{"id":71431,"date":"2026-05-20T11:00:00","date_gmt":"2026-05-20T11:00:00","guid":{"rendered":"https:\/\/medsbase.com\/aicar-acadesine\/"},"modified":"2026-05-21T07:14:08","modified_gmt":"2026-05-21T07:14:08","slug":"aicar-acadesine","status":"publish","type":"product","link":"https:\/\/medsbase.com\/cs\/product\/aicar-acadesine\/","title":{"rendered":"AICAR (Acadesine \/ AICA-Riboside)"},"content":{"rendered":"<p><!-- medsbase-tldr-answer --><\/p>\n<div style=\"background: #fff8e1; border-left: 4px solid #f5a623; padding: 18px 22px; margin: 18px 0; border-radius: 4px;\">\n<h3 style=\"margin: 0 0 8px 0; font-size: 16px; color: #1a4a6b;\">Rychl\u00e1 odpov\u011b\u010f \u2014 Co je AICAR?<\/h3>\n<p style=\"margin: 0;\"><strong>AICAR<\/strong> (Acadesine \/ AICA-Ribosid \/ 5-aminoimidazol-4-karboxamid-1-\u03b2-D-ribofuranosid, CAS 2627-69-2) je kanonick\u00e1 mal\u00e1 molekula <strong>aktiv\u00e1tor AMPK (AMP-activated protein kinase)<\/strong> pou\u017e\u00edvan\u00fd v metabolick\u00e9m, fyziologick\u00e9m v\u00fdzkumu cvi\u010den\u00ed, sval\u016f a v\u00fdzkumu rakoviny. AICAR je bun\u011b\u010dn\u011b prostupn\u00fd ribosid; uvnit\u0159 bun\u011bk je fosforylov\u00e1n adenosin kin\u00e1zou na aktivn\u00ed nukleotid <strong>ZMP<\/strong> (5-aminoimidazol-4-karboxamid ribonukleotid), AMP-mimetikum, kter\u00e9 alostericky aktivuje AMPK. Aktivovan\u00fd AMPK podporuje inzulin-nez\u00e1visl\u00fd p\u0159\u00edjem gluk\u00f3zy do kostern\u00edho svalstva, zvy\u0161uje oxidaci mastn\u00fdch kyselin, potla\u010duje jatern\u00ed glukoneogenezi a de-novo lipogenezi a inhibuje mTORC1 \u2014 kanonick\u00e1 farmakologie \u201ccvi\u010den\u00ed v pilulce\u201d. Dod\u00e1v\u00e1 se jako lyofilizovan\u00fd pr\u00e1\u0161ek (\u226599% HPLC) pouze pro laboratorn\u00ed v\u00fdzkum. <em>Nen\u00ed peptid.<\/em><\/p>\n<\/div>\n<div class=\"medsbase-trust-strip\" style=\"background: #f4f8fb; border: 1px solid #d8e3eb; padding: 12px 16px; margin: 16px 0; border-radius: 4px; font-size: 14px;\"><strong>Co z\u00edsk\u00e1te s MedsBase:<\/strong> Lyofilizovan\u00fd pr\u00e1\u0161ek \u226599% HPLC-verifikovan\u00fd \u00b7 COA dostupn\u00fd na vy\u017e\u00e1d\u00e1n\u00ed \u00b7 Diskr\u00e9tn\u00ed teplotn\u011b stabiln\u00ed balen\u00ed \u00b7 Celosv\u011btov\u00e1 dod\u00e1vka v\u00fdzkumn\u00fdch materi\u00e1l\u016f \u00b7 1,400+ ov\u011b\u0159en\u00fdch <a href=\"https:\/\/medsbase.com\/cs\/reviews\/\">recenz\u00ed z\u00e1kazn\u00edk\u016f<\/a><\/div>\n<p class=\"medsbase-reship-line\" style=\"font-size: 14px; color: #444; margin: 8px 0 18px;\">\ud83d\udce6 Ka\u017ed\u00e1 objedn\u00e1vka je pokryta na\u0161\u00ed <a href=\"https:\/\/medsbase.com\/cs\/medsbase-re-shipment-assurance-policy\/\"><strong>Z\u00e1rukou op\u011btovn\u00e9ho odesl\u00e1n\u00ed<\/strong><\/a> \u2014 pokud va\u0161e z\u00e1silka nedoraz\u00ed do 20 pracovn\u00edch dn\u016f, p\u0159epos\u00edl\u00e1me ji.<\/p>\n<table class=\"medsbase-spec-table\" style=\"width: 100%; border-collapse: collapse; margin: 18px 0; font-size: 14px;\">\n<thead>\n<tr style=\"background: #2c7cb0; color: #fff;\">\n<th style=\"padding: 8px 12px; text-align: left; width: 30%;\">Specifikace<\/th>\n<th style=\"padding: 8px 12px; text-align: left;\">Detail<\/th>\n<\/tr>\n<\/thead>\n<tbody>\n<tr style=\"background: #f9f9f9;\">\n<td style=\"padding: 8px 12px; border-bottom: 1px solid #e0e0e0; width: 30%;\"><strong>T\u0159\u00edda slou\u010denin<\/strong><\/td>\n<td style=\"padding: 8px 12px; border-bottom: 1px solid #e0e0e0;\">Mal\u00e1 molekula purin-nukleosidov\u00e9ho analogu; bun\u011b\u010dn\u011b prostupn\u00e9 AMP-mimetikum; aktiv\u00e1tor AMPK; <em>nen\u00ed peptid<\/em><\/td>\n<\/tr>\n<tr style=\"background: #fff;\">\n<td style=\"padding: 8px 12px; border-bottom: 1px solid #e0e0e0; width: 30%;\"><strong>Chemick\u00fd n\u00e1zev<\/strong><\/td>\n<td style=\"padding: 8px 12px; border-bottom: 1px solid #e0e0e0;\">5-Aminoimidazol-4-karboxamid-1-\u03b2-D-ribofuranosid (synonyma: Acadesine, AICA-Ribosid, NSC 105823, Z-Ribosid)<\/td>\n<\/tr>\n<tr style=\"background: #f9f9f9;\">\n<td style=\"padding: 8px 12px; border-bottom: 1px solid #e0e0e0; width: 30%;\"><strong>CAS \u010d\u00edslo<\/strong><\/td>\n<td style=\"padding: 8px 12px; border-bottom: 1px solid #e0e0e0;\">2627-69-2<\/td>\n<\/tr>\n<tr style=\"background: #fff;\">\n<td style=\"padding: 8px 12px; border-bottom: 1px solid #e0e0e0; width: 30%;\"><strong>item2<\/strong><\/td>\n<td style=\"padding: 8px 12px; border-bottom: 1px solid #e0e0e0;\">C<sub>9<\/sub>H<sub>14<\/sub>N<sub>4<\/sub>O<sub>5<\/sub><\/td>\n<\/tr>\n<tr style=\"background: #f9f9f9;\">\n<td style=\"padding: 8px 12px; border-bottom: 1px solid #e0e0e0; width: 30%;\"><strong>item7<\/strong><\/td>\n<td style=\"padding: 8px 12px; border-bottom: 1px solid #e0e0e0;\">258.23 g\/mol<\/td>\n<\/tr>\n<tr style=\"background: #fff;\">\n<td style=\"padding: 8px 12px; border-bottom: 1px solid #e0e0e0; width: 30%;\"><strong>Mechanismus \u00fa\u010dinku<\/strong><\/td>\n<td style=\"padding: 8px 12px; border-bottom: 1px solid #e0e0e0;\">Bun\u011b\u010dn\u011b prostupn\u00fd AICA ribosid je p\u0159ij\u00edm\u00e1n prost\u0159ednictv\u00edm adenosinov\u00fdch transport\u00e9r\u016f a fosforylov\u00e1n adenosin kin\u00e1zou na aktivn\u00ed intracelul\u00e1rn\u00ed monofosf\u00e1t <strong>ZMP<\/strong> (5-aminoimidazol-4-karboxamid ribonukleotid). ZMP napodobuje AMP na \u03b3-podjednotce AMPK v Batemanov\u011b dom\u00e9n\u011b, co\u017e vede k alosterick\u00e9 aktivaci AMPK nez\u00e1visle na zm\u011bn\u00e1ch bun\u011b\u010dn\u00e9ho pom\u011bru AMP:ATP. Aktivovan\u00e1 AMPK n\u00e1sledn\u011b spou\u0161t\u00ed downstream metabolick\u00fd p\u0159ep\u00edna\u010d (katabolick\u00e9 \u2191, anabolick\u00e9 \u2193).<\/td>\n<\/tr>\n<tr style=\"background: #f9f9f9;\">\n<td style=\"padding: 8px 12px; border-bottom: 1px solid #e0e0e0; width: 30%;\"><strong>item9<\/strong><\/td>\n<td style=\"padding: 8px 12px; border-bottom: 1px solid #e0e0e0;\">n\/a (mal\u00e1 molekula purinov\u00e9ho ribonukleosidu \u2014 nikoli peptid)<\/td>\n<\/tr>\n<tr style=\"background: #fff;\">\n<td style=\"padding: 8px 12px; border-bottom: 1px solid #e0e0e0; width: 30%;\"><strong>item11<\/strong><\/td>\n<td style=\"padding: 8px 12px; border-bottom: 1px solid #e0e0e0;\">Lyofilizovan\u00fd b\u00edl\u00fd a\u017e sv\u011btle b\u00e9\u017eov\u00fd krystalick\u00fd pr\u00e1\u0161ek; jednor\u00e1zov\u00e9 v\u00fdzkumn\u00e9 lahvi\u010dky<\/td>\n<\/tr>\n<tr style=\"background: #f9f9f9;\">\n<td style=\"padding: 8px 12px; border-bottom: 1px solid #e0e0e0; width: 30%;\"><strong>item13<\/strong><\/td>\n<td style=\"padding: 8px 12px; border-bottom: 1px solid #e0e0e0;\">\u226599% (HPLC ov\u011b\u0159eno, COA na vy\u017e\u00e1d\u00e1n\u00ed)<\/td>\n<\/tr>\n<tr style=\"background: #fff;\">\n<td style=\"padding: 8px 12px; border-bottom: 1px solid #e0e0e0; width: 30%;\"><strong>Rozpustnost<\/strong><\/td>\n<td style=\"padding: 8px 12px; border-bottom: 1px solid #e0e0e0;\">Rozpustn\u00fd ve vod\u011b (~50 mg\/ml p\u0159i m\u00edrn\u00e9m zah\u0159\u00e1t\u00ed a prot\u0159ep\u00e1v\u00e1n\u00ed), PBS a DMSO (\u2265100 mM z\u00e1sobn\u00ed roztok). Vodn\u00e9 roztoky mohou vy\u017eadovat kr\u00e1tk\u00e9 zah\u0159\u00e1t\u00ed na 37 \u00b0C pro \u00fapln\u00e9 rozpu\u0161t\u011bn\u00ed. Pracovn\u00ed roztoky pro bun\u011b\u010dn\u00e9 kultury se obvykle p\u0159ipravuj\u00ed v koncentraci 0,5\u20132 mM v r\u016fstov\u00e9m m\u00e9diu.<\/td>\n<\/tr>\n<tr style=\"background: #f9f9f9;\">\n<td style=\"padding: 8px 12px; border-bottom: 1px solid #e0e0e0; width: 30%;\"><strong>Skladov\u00e1n\u00ed<\/strong><\/td>\n<td style=\"padding: 8px 12px; border-bottom: 1px solid #e0e0e0;\">Lyofilizovan\u00fd: 2\u20138 \u00b0C pro kr\u00e1tkodob\u00e9 pracovn\u00ed z\u00e1soby; \u221220 \u00b0C pro dlouhodob\u00e9 skladov\u00e1n\u00ed neotev\u0159en\u00fdch lahvi\u010dek (stabilita \u226536 m\u011bs\u00edc\u016f p\u0159i \u221220 \u00b0C). Rekonstituovan\u00e9 vodn\u00e9 roztoky: 2\u20138 \u00b0C, pou\u017e\u00edt do ~30 dn\u016f. Z\u00e1sobn\u00ed roztoky v DMSO: \u221220 \u00b0C, jednor\u00e1zov\u00e9 rozmrazen\u00ed. Chr\u00e1nit p\u0159ed dlouhodob\u00fdm vystaven\u00edm sv\u011btlu. Vyvarovat se opakovan\u00e9ho zmrazov\u00e1n\u00ed a rozmrazov\u00e1n\u00ed pracovn\u00edch roztok\u016f.<\/td>\n<\/tr>\n<tr style=\"background: #fff;\">\n<td style=\"padding: 8px 12px; border-bottom: 1px solid #e0e0e0; width: 30%;\"><strong>Pouze pro v\u00fdzkum<\/strong><\/td>\n<td style=\"padding: 8px 12px; border-bottom: 1px solid #e0e0e0;\">Pouze pro laboratorn\u00ed v\u00fdzkumn\u00e9 \u00fa\u010dely. Nen\u00ed ur\u010deno pro diagnostick\u00e9 nebo terapeutick\u00e9 pou\u017eit\u00ed u lid\u00ed nebo zv\u00ed\u0159at. AICAR \/ Acadesin je na Seznamu zak\u00e1zan\u00fdch l\u00e1tek Sv\u011btov\u00e9 antidopingov\u00e9 agentury (WADA) (t\u0159\u00edda S4.5, Metabolick\u00e9 modul\u00e1tory) a je ve sportu zak\u00e1z\u00e1n za v\u0161ech okolnost\u00ed \u2014 v\u00fdzkumn\u00edci pracuj\u00edc\u00ed s lidsk\u00fdmi subjekty by m\u011bli b\u00fdt v\u011bdomi tohoto regula\u010dn\u00edho statusu.<\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n<p><!-- \/medsbase-tldr-answer --><\/p>\n<h2>Co je AICAR?<\/h2>\n<p><strong>AICAR<\/strong> (5-Aminoimidazol-4-karboxamid-1-\u03b2-D-ribofuranosid, tak\u00e9 zn\u00e1m\u00fd jako Acadesin, AICA-Ribosid, NSC 105823 nebo Z-Ribosid; CAS 2627-69-2) je mal\u00e1 molekula analogu purinov\u00e9ho ribonukleosidu a nej\u010dast\u011bji citovan\u00fd farmakologick\u00fd n\u00e1stroj pro aktivaci <strong>AMP-aktivovan\u00e9 protein kin\u00e1zy (AMPK)<\/strong> v bun\u011b\u010dn\u00fdch kultur\u00e1ch, prim\u00e1rn\u00edch bu\u0148k\u00e1ch a in vivo v\u00fdzkumu na hlodavc\u00edch. Jedn\u00e1 se <em>nen\u00ed peptid<\/em> \u2014 jde o syntetick\u00fd ribonukleosid s molekul\u00e1rn\u00edm vzorcem C<sub>9<\/sub>H<sub>14<\/sub>N<sub>4<\/sub>O<sub>5<\/sub> a molekulovou hmotnost\u00ed 258,23 g\/mol. MedsBase jej skladuje ve stejn\u00e9m lyofilizovan\u00e9m form\u00e1tu vial jako na\u0161e katalogov\u00e9 v\u00fdzkumn\u00e9 peptidy pro snadnou rekonstituci a d\u00e1vkov\u00e1n\u00ed ve sm\u00ed\u0161en\u00fdch protokolech AMPK \/ metabolick\u00e9ho \/ mitochondri\u00e1ln\u00edho v\u00fdzkumu.<\/p>\n<p>AICAR byl p\u016fvodn\u011b vyvinut v 90. letech spole\u010dnost\u00ed Acadesine Inc. (pozd\u011bji Schering-Plough) jako kandid\u00e1tn\u00ed kardioprotektivn\u00ed l\u00e1tka pro koron\u00e1rn\u00ed bypass \u2014 slou\u010denina dokon\u010dila f\u00e1zi III klinick\u00fdch studi\u00ed, ale nez\u00edskala regula\u010dn\u00ed schv\u00e1len\u00ed. Jej\u00ed farmakologick\u00e1 vyu\u017eitelnost se v\u0161ak od t\u00e9 doby pouze roz\u0161\u00ed\u0159ila: AICAR je nyn\u00ed standardn\u00ed referen\u010dn\u00ed slou\u010deninou pro aktivaci AMPK v publikovan\u00e9m v\u00fdzkumu a AMPK dr\u00e1ha, kterou ovliv\u0148uje, byla spojov\u00e1na s t\u00e9m\u011b\u0159 ka\u017edou v\u00fdznamnou oblast\u00ed metabolick\u00e9 biologie \u2014 inzulinovou senzitivitou, diabetem 2. typu, oxidac\u00ed mastn\u00fdch kyselin, fyziologi\u00ed cvi\u010den\u00ed, svalovou hypertrofi\u00ed \/ atrofi\u00ed, mitochondri\u00e1ln\u00ed biogenez\u00ed, metabolismem n\u00e1dor\u016f, autofagi\u00ed a st\u00e1rnut\u00edm.<\/p>\n<p>V publikovan\u00e9m v\u00fdzkumu je AICAR popisov\u00e1n jako \u201cexercise mimetic\u201d (napodobitel cvi\u010den\u00ed), proto\u017ee chronick\u00e9 pod\u00e1v\u00e1n\u00ed sedav\u00fdm my\u0161\u00edm podle studi\u00ed vyvol\u00e1v\u00e1 genovou expresn\u00ed signaturu kostern\u00edho svalstva, program mitochondri\u00e1ln\u00ed biogeneze a fenotyp vytrvalostn\u00edho v\u00fdkonu, kter\u00fd v \u0161ir\u0161\u00edm smyslu napodobuje \u00fa\u010dinky dobrovoln\u00e9ho b\u011bhu na kole\u010dku \u2014 p\u016fvodn\u00ed publikace Narkar et al. z roku 2008 v <em>Cell<\/em> (\u201cAMPK and PPAR\u03b4 Agonists Are Exercise Mimetics\u201d) je nejcitovan\u011bj\u0161\u00ed prac\u00ed v t\u00e9to oblasti. AICAR je tak\u00e9 na seznamu zak\u00e1zan\u00fdch l\u00e1tek WADA (t\u0159\u00edda S4.5, metabolick\u00e9 modul\u00e1tory) a je ve sportu trvale zak\u00e1z\u00e1n kv\u016fli tomuto potenci\u00e1lu zvy\u0161ov\u00e1n\u00ed v\u00fdkonu.<\/p>\n<h2>Mechanismus \u00fa\u010dinku \u2014 bun\u011b\u010dn\u00e1 aktivace AMPK prost\u0159ednictv\u00edm ZMP<\/h2>\n<p>Mechanismus AICAR je nejl\u00e9pe prozkouman\u00fd ze v\u0161ech farmakologick\u00fdch aktiv\u00e1tor\u016f AMPK:<\/p>\n<ul>\n<li><strong>Vstup do bun\u011bk pomoc\u00ed adenosinov\u00fdch transport\u00e9r\u016f<\/strong> \u2014 AICAR (ribosid) je s\u00e1m o sob\u011b biologicky inertn\u00ed. Do bun\u011bk je p\u0159ij\u00edm\u00e1n stejn\u00fdmi equilibrativn\u00edmi a koncentra\u010dn\u00edmi adenosinov\u00fdmi transport\u00e9ry (ENT1, ENT2, CNT2, CNT3), kter\u00e9 p\u0159en\u00e1\u0161ej\u00ed endogenn\u00ed adenosin a dal\u0161\u00ed purinov\u00e9 nukleosidy p\u0159es plazmatickou membr\u00e1nu. Distribuce ve tk\u00e1n\u00edch a kinetika koncentrace in vivo jsou \u0159\u00edzeny t\u011bmito transport\u00e9ry.<\/li>\n<li><strong>Intracelul\u00e1rn\u00ed fosforylace na ZMP adenosin kin\u00e1zou<\/strong> \u2014 Po vstupu do bu\u0148ky je AICAR fosforylov\u00e1n <strong>adenosin kin\u00e1zou (AK)<\/strong> na sv\u00e9 5\u2032-hydroxylov\u00e9 skupin\u011b, \u010d\u00edm\u017e vznik\u00e1 aktivn\u00ed metabolit ZMP (5-aminoimidazol-4-karboxamid ribonukleotid). ZMP je p\u0159\u00edm\u00fdm analogem AMP a je to pr\u00e1v\u011b tato molekula, kter\u00e1 skute\u010dn\u011b aktivuje AMPK. Aktivita adenosin kin\u00e1zy je tedy limituj\u00edc\u00edm krokem farmakologie AICAR v dan\u00e9 tk\u00e1ni \u2014 v\u00fdzkumn\u00e9 protokoly vyu\u017e\u00edvaj\u00edc\u00ed bu\u0148ky s deficitem AK nebo inhibitory AK potvrzuj\u00ed, \u017ee aktivn\u00ed formou je ZMP, nikoli samotn\u00fd AICAR.<\/li>\n<li><strong>Alersterick\u00e1 aktivace AMPK na \u03b3-podjednotce<\/strong> \u2014 ZMP v\u00e1\u017ee stejn\u00e9 Batemanovy dom\u00e9ny CBS na \u03b3-podjednotce AMPK, kter\u00e9 za podm\u00ednek n\u00edzk\u00e9 energie obsazuje endogenn\u00ed AMP. Vazba ZMP vyvol\u00e1v\u00e1 t\u0159i konvergentn\u00ed alosterick\u00e9 \u00fa\u010dinky na AMPK: (1) alosterickou stimulaci katalytick\u00e9 aktivity, (2) ochranu fosforylace Thr172 na \u03b1-podjednotce AMPK p\u0159ed defosforylac\u00ed PP2C a (3) zv\u00fd\u0161enou fosforylaci Thr172 pomoc\u00ed upstream kin\u00e1z LKB1 a CaMKK2. V\u00fdsledkem je trval\u00e1, vysok\u00e1 aktivace AMPK, kter\u00e1 je nez\u00e1visl\u00e1 na zm\u011bn\u00e1ch skute\u010dn\u00e9ho bun\u011b\u010dn\u00e9ho pom\u011bru AMP:ATP.<\/li>\n<li><strong>Downstream metabolic switch \u2014 katabolick\u00e1 upregulace<\/strong> \u2014 Aktivovan\u00e1 AMPK fosforyluje velk\u00e9 mno\u017estv\u00ed metabolick\u00fdch efektor\u016f, kter\u00e9 spou\u0161t\u011bj\u00ed katabolick\u00fd\/energetick\u00fd program: ACC (acetyl-CoA karboxyl\u00e1za, na Ser79 a Ser212) \u2014 uvol\u0148uje inhibici malonyl-CoA na CPT-I a umo\u017e\u0148uje vstup dlouh\u00fdch mastn\u00fdch kyselin do mitochondri\u00ed pro \u03b2-oxidaci; HSL (hormon-senzitivn\u00ed lip\u00e1za) \u2014 zvy\u0161uje lipol\u00fdzu v adipocytech; TBC1D1 \u2014 podporuje inzulin-nez\u00e1visl\u00fd p\u0159esun GLUT4 a p\u0159\u00edjem gluk\u00f3zy do kostern\u00edho svalstva; PGC-1\u03b1 \u2014 podporuje mitochondri\u00e1ln\u00ed biogenezi. Efekt p\u0159\u00edjmu gluk\u00f3zy v kostern\u00edm svalstvu je nej\u010dast\u011bji citovan\u00fdm funk\u010dn\u00edm v\u00fdstupem ve v\u00fdzkumu AMPK.<\/li>\n<li><strong>Downstream metabolic switch \u2014 anabolick\u00e1 suprese<\/strong> \u2014 Aktivovan\u00e1 AMPK sou\u010dasn\u011b potla\u010duje anabolick\u00e9\/energeticky n\u00e1ro\u010dn\u00e9 dr\u00e1hy: fosforylace TSC2 a Raptoru inhibuje mTORC1, potla\u010duje synt\u00e9zu b\u00edlkovin a spou\u0161t\u00ed autofagii; fosforylace HMG-CoA redukt\u00e1zy potla\u010duje synt\u00e9zu cholesterolu; fosforylace SREBP1c potla\u010duje jatern\u00ed de-novo lipogenezi; fosforylace PFKFB3 a ACC potla\u010duje synt\u00e9zu glykogenu a mastn\u00fdch kyselin. Kombinovan\u00fd p\u0159ep\u00edna\u010d katabolick\u00e9 up\/anabolick\u00e9 down je kanonickou farmakologi\u00ed AMPK.<\/li>\n<\/ul>\n<p>Farmakokinetick\u00fd profil AICAR je obecn\u011b p\u0159\u00edzniv\u00fd pro v\u00fdzkumn\u00e9 pou\u017eit\u00ed \u2014 peror\u00e1ln\u00ed biologick\u00e1 dostupnost je m\u00edrn\u00e1, ale pou\u017eiteln\u00e1, intraperitone\u00e1ln\u00ed pod\u00e1n\u00ed u hlodavc\u016f poskytuje spolehlivou syst\u00e9movou expozici do 30 minut a plazmatick\u00fd polo\u010das rodi\u010dovsk\u00e9ho ribosidu je \u0159\u00e1dov\u011b 90 minut (polo\u010das intracelul\u00e1rn\u00edho metabolitu ZMP je del\u0161\u00ed, udr\u017euje aktivaci AMPK po dobu n\u011bkolika hodin po jedn\u00e9 bolusov\u00e9 d\u00e1vce). Typick\u00e9 in-vivo protokoly pro hlodavce pou\u017e\u00edvaj\u00ed 250\u2013500 mg\/kg pod\u00e1van\u00e9 IP denn\u011b; vysok\u00e9 d\u00e1vky (1 g\/kg) byly pou\u017eity v n\u011bkter\u00fdch publikovan\u00fdch v\u00fdzkumech svalov\u00e9 fyziologie. In-vitro pr\u00e1ce s bun\u011b\u010dn\u00fdmi kulturami obvykle pou\u017e\u00edv\u00e1 0,5\u20132 mM v r\u016fstov\u00e9m m\u00e9diu.<\/p>\n<h2>Publikovan\u00e9 v\u00fdzkumn\u00e9 aplikace<\/h2>\n<p>AICAR se pou\u017e\u00edv\u00e1 v laboratorn\u00edm v\u00fdzkumu ke studiu:<\/p>\n<ul>\n<li><strong>Farmakologie AMPK \u2014 kanonick\u00fd referen\u010dn\u00ed aktiv\u00e1tor<\/strong> \u2014 zdaleka nej\u010dast\u011bji citovan\u00fd malomolekul\u00e1rn\u00ed aktiv\u00e1tor AMPK v publikovan\u00e9 literatu\u0159e; standardn\u00ed n\u00e1strojov\u00e1 slou\u010denina pro jak\u00fdkoli nov\u00fd v\u00fdzkum dr\u00e1hy AMPK; referen\u010dn\u00ed slou\u010denina, v\u016f\u010di kter\u00e9 jsou porovn\u00e1v\u00e1ny v\u0161echny nov\u011bj\u0161\u00ed p\u0159\u00edm\u00e9 aktiv\u00e1tory AMPK (A769662, MK-8722, PF-739, O304, t\u0159\u00edda metforminu)<\/li>\n<li><strong>Inzulinov\u00e1 senzitivita a p\u0159\u00edjem gluk\u00f3zy v kostern\u00edm svalstvu<\/strong> \u2014 AICAR podporuje inzulin-nez\u00e1visl\u00fd p\u0159esun GLUT4 a p\u0159\u00edjem gluk\u00f3zy do kostern\u00edho svalstva prost\u0159ednictv\u00edm osy AMPK-TBC1D1; \u0161iroce pou\u017e\u00edv\u00e1n ve v\u00fdzkumu diabetu 2. typu, reverze inzulinov\u00e9 rezistence a metabolick\u00e9 flexibility kostern\u00edho svalstva<\/li>\n<li><strong>Exercise mimetic a v\u00fdzkum vytrvalosti<\/strong> \u2014 r\u00e1mec Narkar et al. (2008) \u201eAMPK a PPAR\u03b4 Agonists Are Exercise Mimetics\u201c z\u016fst\u00e1v\u00e1 nej\u010dast\u011bji citovanou prac\u00ed o AICAR; publikovan\u00e9 protokoly pro hlodavce dokumentuj\u00ed zv\u00fd\u0161enou vytrvalost, p\u0159em\u011bnu pomal\u00fdch (Typ I) vl\u00e1ken a zlep\u0161enou oxida\u010dn\u00ed kapacitu po 4t\u00fddenn\u00edm pod\u00e1v\u00e1n\u00ed AICAR u sedav\u00fdch my\u0161\u00ed, <em>Cell<\/em>) \u201cAMPK and PPAR\u03b4 Agonists Are Exercise Mimetics\u201d r\u00e1mec z\u016fst\u00e1v\u00e1 nejcitovan\u011bj\u0161\u00edm \u010dl\u00e1nkem o AICAR; publikovan\u00e9 protokoly na hlodavc\u00edch dokumentuj\u00ed zv\u00fd\u0161enou vytrvalost, p\u0159em\u011bnu na pomal\u00e1 vl\u00e1kna (typ I) a zlep\u0161enou oxida\u010dn\u00ed kapacitu po 4t\u00fddenn\u00edm pod\u00e1v\u00e1n\u00ed AICAR u sedav\u00fdch my\u0161\u00ed.<\/li>\n<li><strong>Potla\u010den\u00ed jatern\u00ed glukoneogeneze a lipogeneze<\/strong> \u2014 AICAR potla\u010duje jatern\u00ed produkci gluk\u00f3zy prost\u0159ednictv\u00edm AMPK-zprost\u0159edkovan\u00e9 fosforylace transkrip\u010dn\u00edch koaktiv\u00e1tor\u016f (CRTC2, HNF4\u03b1); tak\u00e9 potla\u010duje jatern\u00ed de-novo lipogenezi fosforylac\u00ed SREBP1c; pou\u017e\u00edv\u00e1 se v preklinick\u00e9m v\u00fdzkumu nealkoholick\u00e9ho ztukovat\u011bn\u00ed jater (NAFLD) a metabolicky asociovan\u00e9 steatohepatitidy (MASH)<\/li>\n<li><strong>V\u00fdzkum oxidace mastn\u00fdch kyselin<\/strong> \u2014 AICAR fosforyluje ACC, uvol\u0148uje inhibici malonyl-CoA na CPT-I a poh\u00e1n\u00ed dlouh\u00e9 \u0159et\u011bzce mastn\u00fdch kyselin do mitochondri\u00ed pro \u03b2-oxidaci; kanonick\u00e1 farmakologick\u00e1 intervence pro zv\u00fd\u0161en\u00ed oxidace mastn\u00fdch kyselin v prim\u00e1rn\u00edch hepatocytech, kardiomyocytech a myotubech kostern\u00edho svalstva<\/li>\n<li><strong>V\u00fdzkum metabolismu n\u00e1dor\u016f<\/strong> \u2014 mnoho n\u00e1dorov\u00fdch bun\u011bk vykazuje zv\u00fd\u0161enou lipogenezi (prost\u0159ednictv\u00edm SREBP1c) a zv\u00fd\u0161enou signalizaci mTORC1; AICAR potla\u010duje oboj\u00ed aktivac\u00ed AMPK a byl zkoum\u00e1n v publikovan\u00fdch v\u00fdzkumech akutn\u00ed lymfoblastick\u00e9 leuk\u00e9mie (p\u016fvodn\u00ed indikace pro Acadesin), karcinomu prostaty, prsu a dal\u0161\u00edch n\u00e1dorov\u00fdch modelech<\/li>\n<li><strong>V\u00fdzkum autofagie a inhibice mTORC1<\/strong> \u2014 AICAR spou\u0161t\u00ed autofagii dvojitou fosforylac\u00ed TSC2 (Ser1387) a Raptoru (Ser792), kter\u00e9 oba inhibuj\u00ed mTORC1; pou\u017e\u00edv\u00e1 se jako farmakologick\u00e1 intervence ve v\u00fdzkumu indukce autofagie spolu s rapamycinem a modely hladov\u011bn\u00ed<\/li>\n<li><strong>V\u00fdzkum mitochondri\u00e1ln\u00ed biogeneze<\/strong> \u2014 AICAR podporuje expresi a aktivitu PGC-1\u03b1, zvy\u0161uje mitochondri\u00e1ln\u00ed biogenezi v kostern\u00edm svalu a hn\u011bd\u00e9 tukov\u00e9 tk\u00e1ni; komplement\u00e1rn\u00ed k <a href=\"https:\/\/medsbase.com\/cs\/mots-c\/\">MOTS-c<\/a> (mitochondri\u00e1ln\u011b odvozen\u00fd AMPK-aktivuj\u00edc\u00ed peptid) v protokolech zkoumaj\u00edc\u00edch redundanci AMPK dr\u00e1hy<\/li>\n<li><strong>V\u00fdzkum kardioprotekce<\/strong> \u2014 p\u016fvodn\u00ed klinick\u00e1 indikace; AICAR byl pou\u017e\u00edv\u00e1n v modelech isch\u00e9mie-reperf\u00fazn\u00edho po\u0161kozen\u00ed a paradigmatu kardioprotekce v kardiochirurgii; preklinick\u00fd v\u00fdzkum pokra\u010duje navzdory tomu, \u017ee f\u00e1ze III nez\u00edskala schv\u00e1len\u00ed<\/li>\n<\/ul>\n<p>Pro \u0161ir\u0161\u00ed kontext v\u00fdzkumn\u00fdch slou\u010denin AMPK \/ NAD<sup>+<\/sup> \/ metabolick\u00e9 osy v tomto katalogu viz <a href=\"https:\/\/medsbase.com\/cs\/mots-c\/\">MOTS-c<\/a> (mitochondri\u00e1ln\u011b odvozen\u00fd peptidov\u00fd aktiv\u00e1tor AMPK \u2014 nejbli\u017e\u0161\u00ed peptidov\u00fd analog), <a href=\"https:\/\/medsbase.com\/cs\/5-amino-1mq\/\">5-Amino-1MQ<\/a> (inhibitor NNMT; komplement\u00e1rn\u00ed p\u0159\u00edstup \u0161et\u0159\u00edc\u00ed NAD<sup>+<\/sup>-prekurzor), <a href=\"https:\/\/medsbase.com\/cs\/nad\/\">NAD<sup>+<\/sup><\/a> (oxidovan\u00fd dinukleotidov\u00fd koenzym, centr\u00e1ln\u00ed substr\u00e1t elektronov\u00e9ho transportu), a <a href=\"https:\/\/medsbase.com\/cs\/l-carnitine\/\">L-Karnitin<\/a> (mitochondri\u00e1ln\u00ed transport\u00e9r dlouh\u00fdch mastn\u00fdch kyselin). Proch\u00e1zejte cel\u00fd <a href=\"https:\/\/medsbase.com\/cs\/peptides\/\">katalog v\u00fdzkumn\u00fdch peptid\u016f a slou\u010denin<\/a> pro souvisej\u00edc\u00ed slou\u010deniny, nebo se pod\u00edvejte na kur\u00e1torsk\u00fd <a href=\"https:\/\/medsbase.com\/cs\/best-longevity-peptides\/\">v\u00fdzkumn\u00e9 slou\u010deniny pro dlouhov\u011bkost<\/a> a <a href=\"https:\/\/medsbase.com\/cs\/best-peptides-for-fat-loss\/\">hub v\u00fdzkumn\u00fdch peptid\u016f pro \u00fabytek tuku<\/a> huby.<\/p>\n<h2>Dostupn\u00e9 s\u00edly a koncentrace<\/h2>\n<p>MedsBase nab\u00edz\u00ed AICAR v jedn\u00e9 velikosti lyofilizovan\u00e9 lahvi\u010dky kalibrovan\u00e9 pro typick\u00e9 in-vivo a vysokokapacitn\u00ed in-vitro v\u00fdzkumn\u00e9 protokoly. Lahvi\u010dka je dostupn\u00e1 v balen\u00ed po 10 nebo 20 kusech:<\/p>\n<table style=\"width: 100%; border-collapse: collapse; margin: 16px 0;\">\n<thead>\n<tr style=\"background: #2c7cb0; color: #fff;\">\n<th style=\"padding: 10px; border: 1px solid #ddd; text-align: left;\">S\u00edla vialky<\/th>\n<th style=\"padding: 10px; border: 1px solid #ddd; text-align: left;\">Typick\u00fd v\u00fdzkumn\u00fd p\u0159\u00edpad u\u017eit\u00ed<\/th>\n<th style=\"padding: 10px; border: 1px solid #ddd; text-align: left;\">Velikosti balen\u00ed<\/th>\n<\/tr>\n<\/thead>\n<tbody>\n<tr>\n<td style=\"padding: 10px; border: 1px solid #ddd;\"><strong>50 mg<\/strong><\/td>\n<td style=\"padding: 10px; border: 1px solid #ddd;\">Standardn\u00ed v\u00fdzkumn\u00e1 s\u00edla \u2013 d\u00e1vkov\u00e1n\u00ed pro jednu kohortu hlodavc\u016f in-vivo (250\u2013500 mg\/kg IP denn\u011b po dobu 2\u20134 t\u00fddn\u016f pokryje 30g my\u0161\u00ed kohortu s jednou 50mg lahvi\u010dkou na ~2\u20133 d\u00e1vky), vysokokapacitn\u00ed panely aktivace AMPK in-vitro (pracovn\u00ed koncentrace 0,5\u20132 mM), pr\u00e1ce s rekonstituc\u00ed a titrac\u00ed d\u00e1vek, panely oxidace mastn\u00fdch kyselin v prim\u00e1rn\u00edch hepatocytech\/myotubech<\/td>\n<td style=\"padding: 10px; border: 1px solid #ddd;\">10 nebo 20 vialek<\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n<p>Form\u00e1t 50mg lahvi\u010dky poskytuje vhodnou d\u00e1vkovac\u00ed jednotku pro v\u011bt\u0161inu publikovan\u00fdch in-vivo protokol\u016f pro hlodavce a podporuje pracovn\u00ed koncentrace 0,5\u20132 mM pou\u017e\u00edvan\u00e9 ve v\u00fdzkumu aktivace AMPK v bun\u011b\u010dn\u00fdch kultur\u00e1ch. Balen\u00ed po 20 lahvi\u010dk\u00e1ch je ekonomi\u010dt\u011bj\u0161\u00ed n\u00e1kup na mg pro protokoly s prodlou\u017een\u00fdm cyklem nebo velk\u00fdmi kohortami (chronick\u00e9 d\u00e1vkov\u00e1n\u00ed 4\u20138 t\u00fddn\u016f, studie s v\u00edce kohortami napodobuj\u00edc\u00ed cvi\u010den\u00ed). V\u00fdzkumn\u00edci by m\u011bli ur\u010dit konkr\u00e9tn\u00ed d\u00e1vkov\u00e9 rozsahy z recenzovan\u00e9 literatury vhodn\u00e9 pro protokol.<\/p>\n<h2>Srovn\u00e1n\u00ed \u2013 AICAR vs MOTS-c<\/h2>\n<p>AICAR a <a href=\"https:\/\/medsbase.com\/cs\/mots-c\/\">MOTS-c<\/a> jsou dva nejstudovan\u011bj\u0161\u00ed v\u00fdzkumn\u00e9 slou\u010deniny aktivuj\u00edc\u00ed AMPK v tomto katalogu a c\u00edl\u00ed na AMPK dr\u00e1hu mechanisticky odli\u0161n\u00fdmi cestami. AICAR je mal\u00e1 molekula napodobuj\u00edc\u00ed AMP, kter\u00e1 pronik\u00e1 do bun\u011bk a p\u0159\u00edmo aktivuje AMPK na \u03b3-podjednotce. MOTS-c je mitochondri\u00e1ln\u00ed peptid o 16 aminokyselin\u00e1ch, kter\u00fd se p\u0159i metabolick\u00e9m stresu translokuje do j\u00e1dra a aktivuje AMPK nep\u0159\u00edmo prost\u0159ednictv\u00edm intermedi\u00e1tu fol\u00e1tov\u00e9 dr\u00e1hy\/metioninov\u00e9ho cyklu (AICAR-like zv\u00fd\u0161en\u00ed bun\u011b\u010dn\u00fdch hladin AICAR\/ZMP). Tyto dv\u011b slou\u010deniny jsou mechanisticky komplement\u00e1rn\u00ed v publikovan\u00fdch kombinovan\u00fdch v\u00fdzkumech a toto srovn\u00e1n\u00ed ilustruje jeden z nejstudovan\u011bj\u0161\u00edch \u201cdy\u00e1d mal\u00e1 molekula vs peptid\u201d v biologii AMPK.<\/p>\n<table style=\"width: 100%; border-collapse: collapse; margin: 16px 0;\">\n<thead>\n<tr style=\"background: #2c7cb0; color: #fff;\">\n<th style=\"padding: 10px; border: 1px solid #ddd; text-align: left;\">Krit\u00e9rium<\/th>\n<th style=\"padding: 10px; border: 1px solid #ddd; text-align: left;\">AICAR<\/th>\n<th style=\"padding: 10px; border: 1px solid #ddd; text-align: left;\">MOTS-c<\/th>\n<\/tr>\n<\/thead>\n<tbody>\n<tr>\n<td style=\"padding: 10px; border: 1px solid #ddd;\"><strong>Chemick\u00e1 t\u0159\u00edda<\/strong><\/td>\n<td style=\"padding: 10px; border: 1px solid #ddd;\">Mal\u00e1 molekula purinov\u00e9ho ribonukleosidu (bun\u011b\u010dn\u011b pronikaj\u00edc\u00ed analog AMP)<\/td>\n<td style=\"padding: 10px; border: 1px solid #ddd;\">Mitochondri\u00e1ln\u00ed peptid o 16 zbytc\u00edch (dr\u00e1ha MTHFD2L \/ mechanismus hromad\u011bn\u00ed podobn\u00fd AICAR)<\/td>\n<\/tr>\n<tr style=\"background: #f9f9f9;\">\n<td style=\"padding: 10px; border: 1px solid #ddd;\"><strong>Molekulov\u00e1 hmotnost<\/strong><\/td>\n<td style=\"padding: 10px; border: 1px solid #ddd;\">258.23 g\/mol<\/td>\n<td style=\"padding: 10px; border: 1px solid #ddd;\">~2 174 g\/mol (16-aminokyselinov\u00fd peptid)<\/td>\n<\/tr>\n<tr>\n<td style=\"padding: 10px; border: 1px solid #ddd;\"><strong>Cesta k AMPK<\/strong><\/td>\n<td style=\"padding: 10px; border: 1px solid #ddd;\">P\u0159\u00edm\u00e1 \u2013 fosforylov\u00e1na na ZMP intracelul\u00e1rn\u011b, v\u00e1\u017ee se na Batemanovu dom\u00e9nu \u03b3-podjednotky AMPK (AMP-mimetikum)<\/td>\n<td style=\"padding: 10px; border: 1px solid #ddd;\">Nep\u0159\u00edm\u00e1 \u2013 naru\u0161uje fol\u00e1tov\u00fd\/methioninov\u00fd cyklus, zvy\u0161uje bun\u011b\u010dnou hladinu AICAR\/ZMP, aktivuje AMPK p\u0159es stejn\u00e9 alosterick\u00e9 m\u00edsto \u03b3-podjednotky<\/td>\n<\/tr>\n<tr style=\"background: #f9f9f9;\">\n<td style=\"padding: 10px; border: 1px solid #ddd;\"><strong>Nejl\u00e9pe prostudovan\u00fd v\u00fdzkumn\u00fd z\u00e1m\u011br<\/strong><\/td>\n<td style=\"padding: 10px; border: 1px solid #ddd;\">Mimetikum cvi\u010den\u00ed, citlivost na inzul\u00edn, jatern\u00ed glukoneogeneze, metabolismus n\u00e1dor\u016f, autofagie, mitochondri\u00e1ln\u00ed biogeneze<\/td>\n<td style=\"padding: 10px; border: 1px solid #ddd;\">Citlivost na inzul\u00edn, mitochondri\u00e1ln\u00ed biologie, metabolick\u00fd \u00fabytek souvisej\u00edc\u00ed s v\u011bkem, dlouhov\u011bkost, farmakologie peptidov\u00e9 osy<\/td>\n<\/tr>\n<tr>\n<td style=\"padding: 10px; border: 1px solid #ddd;\"><strong>Stabilita v plazm\u011b<\/strong><\/td>\n<td style=\"padding: 10px; border: 1px solid #ddd;\">~90 minut polo\u010das v plazm\u011b (mate\u0159sk\u00fd ribosid); intracelul\u00e1rn\u00ed ZMP udr\u017euje \u00fa\u010dinek po n\u011bkolik hodin po bolusov\u00e9 d\u00e1vce<\/td>\n<td style=\"padding: 10px; border: 1px solid #ddd;\">Kr\u00e1tk\u00fd \u2013 minuty polo\u010dasu v plazm\u011b bez ochrany; vhodn\u00fd pro IP\/SC pod\u00e1n\u00ed ve v\u00fdzkumu<\/td>\n<\/tr>\n<tr style=\"background: #f9f9f9;\">\n<td style=\"padding: 10px; border: 1px solid #ddd;\"><strong>Typick\u00e1 v\u00fdzkumn\u00e1 d\u00e1vka<\/strong><\/td>\n<td style=\"padding: 10px; border: 1px solid #ddd;\">250\u2013500 mg\/kg IP denn\u011b u hlodavc\u016f (ob\u010dasn\u011b 1 g\/kg ve svalov\u00fdch fyziologick\u00fdch protokolech); 0,5\u20132 mM v bun\u011b\u010dn\u00e9 kultu\u0159e<\/td>\n<td style=\"padding: 10px; border: 1px solid #ddd;\">0,5\u20135 mg\/kg IP\/SC u hlodavc\u016f<\/td>\n<\/tr>\n<tr>\n<td style=\"padding: 10px; border: 1px solid #ddd;\"><strong>Selektivita \/ profil mimo c\u00edle<\/strong><\/td>\n<td style=\"padding: 10px; border: 1px solid #ddd;\">Nen\u00ed \u010dist\u011b selektivn\u00ed \u2014 ZMP tak\u00e9 ovliv\u0148uje adenosinovou signalizaci, frukt\u00f3za-1,6-bisfosfat\u00e1zu a AMP-deamin\u00e1zu p\u0159i vysok\u00fdch d\u00e1vk\u00e1ch<\/td>\n<td style=\"padding: 10px; border: 1px solid #ddd;\">Selektivita t\u0159\u00eddy peptid\u016f \u2014 m\u00e9n\u011b zdokumentovan\u00fdch \u00fa\u010dink\u016f na mal\u00e9 molekuly receptor\u016f mimo c\u00edle, ale identita receptor\u016f st\u00e1le z\u016fst\u00e1v\u00e1 p\u0159edm\u011btem v\u00fdzkumu<\/td>\n<\/tr>\n<tr style=\"background: #f9f9f9;\">\n<td style=\"padding: 10px; border: 1px solid #ddd;\"><strong>Regula\u010dn\u00ed status<\/strong><\/td>\n<td style=\"padding: 10px; border: 1px solid #ddd;\">\u017d\u00e1dn\u00e9 klinick\u00e9 schv\u00e1len\u00ed (Acadesin f\u00e1ze III pro CABG nez\u00edskal schv\u00e1len\u00ed); WADA zak\u00e1zan\u00fd seznam S4.5 (zak\u00e1z\u00e1n ve sportu za v\u0161ech okolnost\u00ed)<\/td>\n<td style=\"padding: 10px; border: 1px solid #ddd;\">\u017d\u00e1dn\u00e9 klinick\u00e9 schv\u00e1len\u00ed; pouze pro v\u00fdzkum<\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n<p>Pro v\u00fdzkum zam\u011b\u0159en\u00fd na p\u0159\u00edmou, vysokou aktivaci AMPK s kanonickou referen\u010dn\u00ed malou molekulou je AICAR standardn\u00ed slou\u010denina. Pro v\u00fdzkum zam\u011b\u0159en\u00fd na aktivaci AMPK t\u0159\u00eddy peptid\u016f, mitochondri\u00e1ln\u00ed signalizaci nebo farmakologii peptid\u016f dlouhov\u011bkosti, <a href=\"https:\/\/medsbase.com\/cs\/mots-c\/\">MOTS-c<\/a> c\u00edlen\u011bj\u0161\u00edm n\u00e1strojem. Viz tak\u00e9 <a href=\"https:\/\/medsbase.com\/cs\/5-amino-1mq\/\">5-Amino-1MQ<\/a> pro v\u00fdzkum \u0161et\u0159\u00edc\u00ed prekurzory NAD-osy, <a href=\"https:\/\/medsbase.com\/cs\/ss-31-elamipretide\/\">SS-31 (Elamipretide)<\/a> pro v\u00fdzkum c\u00edlen\u00fd na kardiolipin-v\u00e1zaj\u00edc\u00ed mitochondrie, <a href=\"https:\/\/medsbase.com\/cs\/nad\/\">NAD<sup>+<\/sup><\/a> pro p\u0159\u00edmou suplementaci NAD-poolu.<\/p>\n<div style=\"background: #f4f8fb; border-left: 4px solid #2c7cb0; padding: 14px 18px; margin: 18px 0;\"><strong class=\"mb-bac-water-callout\">\ud83d\udca7 Pot\u0159ebujete BAC vodu?<\/strong> Rekonstituce jak\u00e9hokoli lyofilizovan\u00e9ho vialu vy\u017eaduje steriln\u00ed bakteriostatickou vodu. Sp\u00e1rujte tento produkt s na\u0161\u00edm <a href=\"\/cs\/bac-water\/\"><strong>BAC Water (Bakteriostatick\u00e1 voda)<\/strong><\/a> \u2014 30 mL multid\u00e1vkov\u00fdm vialem, 0,9% benzylalkoholem konzervovan\u00fdm, USP-grade.<\/div>\n<h2>Skladov\u00e1n\u00ed a rekonstituce<\/h2>\n<p><strong>P\u0159ed rekonstituci:<\/strong> lyofilizovan\u00e9 lahvi\u010dky skladujte v chladni\u010dce p\u0159i 2\u20138 \u00b0C v p\u016fvodn\u00edm obalu pro kr\u00e1tkodob\u00e9 pracovn\u00ed z\u00e1soby. Pro dlouhodob\u00e9 skladov\u00e1n\u00ed zmrazte neotev\u0159en\u00e9 lahvi\u010dky p\u0159i \u221220 \u00b0C (stabiln\u00ed \u226536 m\u011bs\u00edc\u016f p\u0159i \u221220 \u00b0C; \u226512 m\u011bs\u00edc\u016f p\u0159i 2\u20138 \u00b0C). Lyofilizovan\u00fd AICAR je v\u00fdrazn\u011b stabiln\u011bj\u0161\u00ed ne\u017e v\u011bt\u0161ina lyofilizovan\u00fdch peptid\u016f, proto\u017ee mal\u00e1 molekula ribonukleosidu nem\u00e1 \u017e\u00e1dn\u00e9 amidov\u00e9 vazby nebo disulfidov\u00e9 m\u016fstky, kter\u00e9 by se hydrolyzovaly. Chra\u0148te p\u0159ed dlouhodob\u00fdm vystaven\u00edm p\u0159\u00edm\u00e9mu sv\u011btlu.<\/p>\n<p><strong>Postup rekonstituce:<\/strong> pro lahvi\u010dku 50 mg injikujte 1,0 mL bakteriostatick\u00e9 vody, steriln\u00ed vody nebo steriln\u00edho PBS po bo\u010dn\u00ed st\u011bn\u011b lahvi\u010dky \u2014 t\u00edm z\u00edsk\u00e1te pracovn\u00ed z\u00e1sobu 50 mg\/mL (~193 mM). Pro v\u00edce z\u0159ed\u011bn\u00e9 pracovn\u00ed z\u00e1soby: 2,5 mL poskytne 20 mg\/mL (~77 mM) a 5,0 mL poskytne pracovn\u00ed z\u00e1sobu 10 mg\/mL (~39 mM). AICAR se rychle rozpou\u0161t\u00ed p\u0159i jemn\u00e9m krou\u017een\u00ed p\u0159i pokojov\u00e9 teplot\u011b; kr\u00e1tk\u00e9 zah\u0159\u00e1t\u00ed na 37 \u00b0C urychluje rozpou\u0161t\u011bn\u00ed, pokud jsou p\u0159\u00edtomny zbytkov\u00e9 krystaly z chladn\u00e9ho skladov\u00e1n\u00ed. Pro pr\u00e1ci s bun\u011b\u010dn\u00fdmi kulturami in vitro je DMSO tak\u00e9 vhodn\u00fdm rozpou\u0161t\u011bdlem pro rekonstituci (z\u00e1soba a\u017e 200 mM); pracovn\u00ed roztoky na\u0159e\u010fte do vodn\u00e9ho m\u00e9dia t\u011bsn\u011b p\u0159ed pou\u017eit\u00edm, c\u00edlem je kone\u010dn\u00e1 koncentrace 0,5\u20132 mM v r\u016fstov\u00e9m m\u00e9diu. Po rekonstituci ve vodn\u00e9m pufru skladujte lahvi\u010dku p\u0159i 2\u20138 \u00b0C a pou\u017eijte do 30 dn\u016f. Chra\u0148te p\u0159ed sv\u011btlem. Vyho\u010fte, pokud se objev\u00ed z\u00e1kal, \u010d\u00e1stice nebo v\u00fdrazn\u00e1 zm\u011bna barvy.<\/p>\n<h2>\u010casto kladen\u00e9 dotazy<\/h2>\n<h3>Je AICAR peptid?<\/h3>\n<p>Ne. AICAR je mal\u00e1 molekula analogu purinov\u00e9ho ribonukleosidu (MW 258,23 g\/mol), <em>ne<\/em> peptid. M\u00e1me jej v na\u0161em katalogu v\u00fdzkumn\u00fdch peptid\u016f vedle <a href=\"https:\/\/medsbase.com\/cs\/5-amino-1mq\/\">5-Amino-1MQ<\/a>, <a href=\"https:\/\/medsbase.com\/cs\/nad\/\">NAD<sup>+<\/sup><\/a> a <a href=\"https:\/\/medsbase.com\/cs\/l-carnitine\/\">L-Karnitin<\/a> proto\u017ee pln\u00ed dopl\u0148uj\u00edc\u00ed roli ve v\u00fdzkumu mitochondri\u00e1ln\u00ed \/ metabolick\u00e9 \/ AMPK-osy a je dod\u00e1v\u00e1n ve stejn\u00e9m lyofilizovan\u00e9m form\u00e1tu lahvi\u010dky. \u0158\u00e1dek sekvence v tabulce specifikac\u00ed je z tohoto d\u016fvodu ozna\u010den jako \u201cn\/a\u201d.<\/p>\n<h3>Jak\u00fd je rozd\u00edl mezi AICAR, Acadesinem, AICA-Ribosidem a ZMP?<\/h3>\n<p>AICAR, Acadesine, AICA-Riboside, NSC 105823 a Z-Riboside jsou <em>v\u0161echny stejn\u00e1 slou\u010denina<\/em> \u2014 p\u011bt r\u016fzn\u00fdch n\u00e1zv\u016f pro 5-aminoimidazol-4-karboxamid-1-\u03b2-D-ribofuranosid, bun\u011b\u010dn\u011b prostupn\u00fd ribosid (CAS 2627-69-2). <strong>ZMP<\/strong> je jin\u00e1 slou\u010denina \u2014 intracelul\u00e1rn\u00ed monofosf\u00e1t (5-aminoimidazol-4-karboxamid ribonukleotid), kter\u00fd vznik\u00e1 p\u016fsoben\u00edm adenosin kin\u00e1zy z ribosidu po jeho vstupu do bu\u0148ky. ZMP je skute\u010dn\u00fd AMP-mimetik, kter\u00fd aktivuje AMPK; samotn\u00fd ribosid (AICAR) je bun\u011b\u010dn\u011b prostupn\u00fd prol\u00e9\u010divo. V\u00fdzkumn\u00e9 spole\u010dnosti prod\u00e1vaj\u00ed ribosid, proto\u017ee je bun\u011b\u010dn\u011b prostupn\u00fd; monofosf\u00e1t (ZMP) neproch\u00e1z\u00ed plazmatickou membr\u00e1nou.<\/p>\n<h3>Pro\u010d se AICAR naz\u00fdv\u00e1 \u201cmimetikum cvi\u010den\u00ed\u201d?<\/h3>\n<p>Studie Narkar et al. (2008) <em>Cell<\/em> s n\u00e1zvem \u201cAMPK a PPAR\u03b4 agonist\u00e9 jsou mimetika cvi\u010den\u00ed\u201d popsala, \u017ee 4 t\u00fddny pod\u00e1v\u00e1n\u00ed AICAR sedav\u00fdm my\u0161\u00edm (500 mg\/kg\/den intraperitone\u00e1ln\u011b) vyvolalo genovou expresi ve skelet\u00e1ln\u00edm svalu, profil mitochondri\u00e1ln\u00ed biogeneze, posun typu vl\u00e1ken sm\u011brem k pomal\u00fdm oxidativn\u00edm vl\u00e1kn\u016fm (typ I) a fenotyp vytrvalostn\u00edho v\u00fdkonu, kter\u00fd \u0161iroce napodoboval \u00fa\u010dinky dobrovoln\u00e9ho b\u011bh\u00e1n\u00ed na kole\u010dku u nel\u00e9\u010den\u00fdch my\u0161\u00ed. R\u00e1mec \u201ccvi\u010den\u00ed v pilulce\u201d poch\u00e1z\u00ed z t\u00e9to studie. AICAR je na seznamu zak\u00e1zan\u00fdch l\u00e1tek WADA \u010d\u00e1ste\u010dn\u011b kv\u016fli t\u011bmto zji\u0161t\u011bn\u00edm o zlep\u0161en\u00ed v\u00fdkonu.<\/p>\n<h3>Jak\u00e9 d\u00e1vkov\u00e9 rozsahy byly pou\u017eity ve v\u00fdzkumu na my\u0161\u00edch a potkanech?<\/h3>\n<p>Nej\u010dast\u011bji citovan\u00e1 d\u00e1vka pro my\u0161i je 250\u2013500 mg\/kg intraperitone\u00e1ln\u011b denn\u011b, pod\u00e1van\u00e1 po dobu 2\u20134 t\u00fddn\u016f. Protokol pro fenotyp vytrvalosti podle Narkar et al. pou\u017e\u00edval 500 mg\/kg\/den intraperitone\u00e1ln\u011b po dobu 4 t\u00fddn\u016f. Vy\u0161\u0161\u00ed d\u00e1vky (a\u017e 1 g\/kg) byly pou\u017eity v n\u011bkter\u00fdch v\u00fdzkumech svalov\u00e9 fyziologie. Protokoly pro potkany jsou podobn\u00e9 (250\u2013500 mg\/kg intraperitone\u00e1ln\u011b). Pr\u00e1ce s bun\u011b\u010dn\u00fdmi kulturami in vitro obvykle pou\u017e\u00edv\u00e1 0,5\u20132 mM AICAR v r\u016fstov\u00e9m m\u00e9diu. V\u00fdzkumn\u00edci by se m\u011bli obr\u00e1tit na prim\u00e1rn\u00ed literaturu (Narkar et al. 2008; Corton et al. 1995 p\u016fvodn\u00ed studie o aktivaci AMPK; Merrill et al. 1997 studie o p\u0159\u00edjmu gluk\u00f3zy ve skelet\u00e1ln\u00edm svalu) pro pokyny k d\u00e1vkov\u00e1n\u00ed specifick\u00e9mu pro druh, model a c\u00edl.<\/p>\n<h3>Jak\u00fd je regula\u010dn\u00ed status AICAR podle WADA?<\/h3>\n<p>AICAR \/ Acadesine je uveden na seznamu zak\u00e1zan\u00fdch l\u00e1tek Sv\u011btov\u00e9 antidopingov\u00e9 agentury (WADA) v t\u0159\u00edd\u011b S4.5 (Hormon\u00e1ln\u00ed a metabolick\u00e9 modul\u00e1tory) a je ve sportu zak\u00e1z\u00e1n v\u017edy \u2014 jak v sout\u011b\u017ei, tak mimo sout\u011b\u017e. Z\u00e1kladem je zji\u0161t\u011bn\u00ed o mimetick\u00e9m \u00fa\u010dinku na vytrvalostn\u00ed fenotyp. V\u00fdzkumn\u00edci prov\u00e1d\u011bj\u00edc\u00ed v\u00fdzkum na lidsk\u00fdch subjektech s AICAR mus\u00ed b\u00fdt v\u011bdomi tohoto statusu (krom\u011b regula\u010dn\u00edch po\u017eadavk\u016f pro jak\u00fdkoli neschv\u00e1len\u00fd l\u00e9k). Pro laboratorn\u00ed v\u00fdzkum in vitro a in vivo na hlodavc\u00edch je status WADA pouze informativn\u00ed.<\/p>\n<h3>Jak se AICAR srovn\u00e1v\u00e1 s metforminem jako aktiv\u00e1tor AMPK?<\/h3>\n<p>AICAR i metformin aktivuj\u00ed AMPK, ale zcela odli\u0161n\u00fdmi mechanismy. AICAR (po intracelul\u00e1rn\u00ed p\u0159em\u011bn\u011b na ZMP) je <em>p\u0159\u00edm\u00fd<\/em> AMP-mimetik, kter\u00fd se v\u00e1\u017ee na Batemanovu dom\u00e9nu \u03b3-podjednotky AMPK. Metformin je <em>nep\u0159\u00edm\u00fd<\/em> aktiv\u00e1tor AMPK \u2014 inhibuje mitochondri\u00e1ln\u00ed komplex I, co\u017e sni\u017euje ATP a zvy\u0161uje pom\u011br AMP:ATP, \u010d\u00edm\u017e sekund\u00e1rn\u011b aktivuje AMPK prost\u0159ednictv\u00edm p\u0159irozen\u00e9ho mechanismu vazby AMP. Tyto dv\u011b slou\u010deniny tedy zkoumaj\u00ed r\u016fzn\u00e9 \u00farovn\u011b dr\u00e1hy AMPK: AICAR\/ZMP obch\u00e1z\u00ed pot\u0159ebu skute\u010dn\u00e9ho energetick\u00e9ho stresu, zat\u00edmco metformin zapojuje p\u0159irozenou v\u011btev detekce energie. Nov\u011bj\u0161\u00ed p\u0159\u00edm\u00e9 aktiv\u00e1tory AMPK (A769662, MK-8722, PF-739, O304) se v\u00e1\u017eou na t\u0159et\u00ed m\u00edsto (alosterickou kapsu ADaM \/ \u03b2-podjednotky) a nab\u00edzej\u00ed lep\u0161\u00ed izoformovou selektivitu ne\u017e AICAR nebo metformin.<\/p>\n<h3>Lze AICAR kombinovat s MOTS-c, NAD<sup>+<\/sup>, nebo 5-Amino-1MQ ve v\u00fdzkumn\u00fdch protokolech?<\/h3>\n<p>Ano \u2014 tyto \u010dty\u0159i slou\u010deniny c\u00edl\u00ed na p\u0159ekr\u00fdvaj\u00edc\u00ed se, ale mechanisticky odli\u0161n\u00e9 uzly mitochondri\u00e1ln\u00ed \/ AMPK \/ NAD-osov\u00e9 biologie a b\u011b\u017en\u011b se kombinuj\u00ed ve v\u00fdzkumu, kter\u00fd si klade za c\u00edl odd\u011blit p\u0159\u00edmou aktivaci AMPK (AICAR) od aktivace AMPK t\u0159\u00eddou peptid\u016f (<a href=\"https:\/\/medsbase.com\/cs\/mots-c\/\">MOTS-c<\/a>), od \u0161et\u0159en\u00ed prekurzor\u016f NAD (<a href=\"https:\/\/medsbase.com\/cs\/5-amino-1mq\/\">5-Amino-1MQ<\/a>), od p\u0159\u00edm\u00e9 suplementace poolu NAD (<a href=\"https:\/\/medsbase.com\/cs\/nad\/\">NAD<sup>+<\/sup><\/a>). Ka\u017edou slou\u010deninu nejprve rekonstituujte zvl\u00e1\u0161\u0165, abyste ov\u011b\u0159ili stabilitu a p\u0159esnost koncentrace, a pot\u00e9 je kombinujte t\u011bsn\u011b p\u0159ed pou\u017eit\u00edm, nikoli spole\u010dn\u00fdm skladov\u00e1n\u00edm rekonstituovan\u00fdch vial. Nej\u010dast\u011bji publikovan\u00e9 kombinace jsou AICAR + metformin (dvojit\u00e1 aktivace AMPK, r\u016fzn\u00e9 nad\u0159azen\u00e9 v\u011btve) a AICAR + rapamycin (dvojit\u00e1 inhibice mTORC1, r\u016fzn\u00e9 mechanismy).<\/p>\n<h3>Pro\u010d Acadesine nez\u00edskal klinick\u00e9 schv\u00e1len\u00ed?<\/h3>\n<p>Acadesine (klinick\u00fd n\u00e1zev pro AICAR) dokon\u010dil ve 90. letech dv\u011b velk\u00e9 studie f\u00e1ze III pro kardioprotekci p\u0159i operaci koron\u00e1rn\u00edho bypassu (CABG). Studie neprok\u00e1zaly statisticky v\u00fdznamn\u00e9 sn\u00ed\u017een\u00ed prim\u00e1rn\u00edho kombinovan\u00e9ho koncov\u00e9ho bodu (infarkt myokardu, c\u00e9vn\u00ed mozkov\u00e1 p\u0159\u00edhoda, kardiovaskul\u00e1rn\u00ed \u00famrt\u00ed), a v\u00fdvojov\u00fd program byl ukon\u010den. AICAR z\u016fst\u00e1v\u00e1 v\u00fdzkumnou slou\u010deninou sp\u00ed\u0161e ne\u017e schv\u00e1len\u00fdm l\u00e9kem, i kdy\u017e \u0159ada akademick\u00fdch skupin pokra\u010duje ve zkoum\u00e1n\u00ed paradigmatu kardioprotekce a \u0161ir\u0161\u00ed farmakologie dr\u00e1hy AMPK.<\/p>\n<div class=\"medsbase-trust-strip\" style=\"background: #f4f8fb; border: 1px solid #d8e3eb; padding: 12px 16px; margin: 20px 0 8px; border-radius: 4px; font-size: 14px;\"><strong>Pro\u010d objedn\u00e1vat v\u00fdzkumn\u00e9 slou\u010deniny od MedsBase:<\/strong> Lyofilizovan\u00e9 peptidy a slou\u010deniny HPLC \u226599% \u00b7 COA dostupn\u00e9 na vy\u017e\u00e1d\u00e1n\u00ed \u00b7 Diskr\u00e9tn\u00ed teplotn\u011b stabiln\u00ed balen\u00ed \u00b7 Celosv\u011btov\u00e1 p\u0159eprava \u00b7 <a href=\"https:\/\/medsbase.com\/cs\/medsbase-re-shipment-assurance-policy\/\">Reshipment Assurance<\/a> na ka\u017edou objedn\u00e1vku \u00b7 1,400+ ov\u011b\u0159en\u00fdch <a href=\"https:\/\/medsbase.com\/cs\/reviews\/\">recenz\u00ed z\u00e1kazn\u00edk\u016f<\/a><\/div>\n<p><!-- medsbase-related-alts-v1 --><\/p>\n<h2>Dal\u0161\u00ed v\u00fdzkumn\u00e9 slou\u010deniny pro v\u00fdzkum AMPK a metabolismu<\/h2>\n<ul>\n<li><a href=\"\/cs\/mots-c\/\"><strong>MOTS-c<\/strong><\/a> \u2014 Mitochondri\u00e1ln\u00ed peptidov\u00fd aktiv\u00e1tor AMPK \u2013 nejbli\u017e\u0161\u00ed mechanistick\u00fd peptidov\u00fd analog<\/li>\n<li><a href=\"\/cs\/5-amino-1mq\/\"><strong>5-Amino-1MQ<\/strong><\/a> \u2014 Selektivn\u00ed inhibitor NNMT \u2013 komplement\u00e1rn\u00ed p\u0159\u00edstup \u0161et\u0159\u00edc\u00ed prekurzory NAD<\/li>\n<li><a href=\"\/cs\/nad\/\"><strong>NAD\u207a<\/strong><\/a> \u2014 Oxidovan\u00fd dinukleotidov\u00fd koenzym \u2014 p\u0159\u00edm\u00fd v\u00fdzkum dopl\u0148ov\u00e1n\u00ed NAD poolu<\/li>\n<li><a href=\"\/cs\/ss-31-elamipretide\/\"><strong>SS-31 (Elamipretide)<\/strong><\/a> \u2014 Peptid v\u00e1zaj\u00edc\u00ed kardiolipin s mitochondri\u00e1ln\u00edm c\u00edlen\u00edm<\/li>\n<li><a href=\"\/cs\/l-carnitine\/\"><strong>L-Karnitin<\/strong><\/a> \u2014 Mitochondri\u00e1ln\u00ed transport\u00e9r dlouh\u00fdch mastn\u00fdch kyselin \u2014 doprovodn\u00e1 mal\u00e1 molekula<\/li>\n<li><a href=\"\/cs\/bac-water\/\"><strong>BAC Water (Bakteriostatick\u00e1 voda)<\/strong><\/a> \u2014 Nezbytn\u00e9 pro rekonstituci jak\u00e9hokoli lyofilizovan\u00e9ho vialu \u2014 steriln\u00ed \u0159edidlo s 0,9% konzervantem benzylalkoholu<\/li>\n<\/ul>","protected":false},"excerpt":{"rendered":"<p>\u2705 Kanonick\u00fd aktiv\u00e1tor AMPK mal\u00fdch molekul (bun\u011b\u010dn\u011b prostupn\u00fd AMP-mimetikum p\u0159es ZMP)<br \/>\n\u2705 Podporuje inzulinov\u011b nez\u00e1visl\u00fd p\u0159\u00edjem gluk\u00f3zy do kostern\u00edho svalstva<br \/>\n\u2705 Potla\u010duje jatern\u00ed glukoneogenezi, de-novo lipogenezi, synt\u00e9zu cholesterolu<br \/>\n\u2705 Publikovan\u00fd fenotyp \u2018napodobuj\u00edc\u00ed cvi\u010den\u00ed\u2019 (Narkar et al. 2008, Cell)<br \/>\n\u2705 Referen\u010dn\u00ed slou\u010denina pro farmakologii AMPK \u2014 MW 258,23, CAS 2627-69-2<\/p>\n<p><strong>AICAR<\/strong> obsahuje v\u00fdzkumnou slou\u010deninu 5-aminoimidazol-4-karboxamid-1-\u03b2-D-ribofuranosid.<\/p>","protected":false},"featured_media":71435,"comment_status":"open","ping_status":"closed","template":"","meta":[],"product_brand":[],"product_cat":[5426],"product_tag":[6486,6487,6485,6488,6489,6484,6482],"class_list":{"0":"post-71431","1":"product","2":"type-product","3":"status-publish","4":"has-post-thumbnail","6":"product_cat-peptides","7":"product_tag-acadesine","8":"product_tag-aica-riboside","9":"product_tag-aicar","10":"product_tag-ampk-activator","11":"product_tag-exercise-mimetic","12":"product_tag-metabolic-research","13":"product_tag-research-compound","15":"first","16":"instock","17":"shipping-taxable","18":"purchasable","19":"product-type-variable","20":"has-default-attributes"},"acf":[],"_links":{"self":[{"href":"https:\/\/medsbase.com\/cs\/wp-json\/wp\/v2\/product\/71431","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/medsbase.com\/cs\/wp-json\/wp\/v2\/product"}],"about":[{"href":"https:\/\/medsbase.com\/cs\/wp-json\/wp\/v2\/types\/product"}],"replies":[{"embeddable":true,"href":"https:\/\/medsbase.com\/cs\/wp-json\/wp\/v2\/comments?post=71431"}],"wp:featuredmedia":[{"embeddable":true,"href":"https:\/\/medsbase.com\/cs\/wp-json\/wp\/v2\/media\/71435"}],"wp:attachment":[{"href":"https:\/\/medsbase.com\/cs\/wp-json\/wp\/v2\/media?parent=71431"}],"wp:term":[{"taxonomy":"product_brand","embeddable":true,"href":"https:\/\/medsbase.com\/cs\/wp-json\/wp\/v2\/product_brand?post=71431"},{"taxonomy":"product_cat","embeddable":true,"href":"https:\/\/medsbase.com\/cs\/wp-json\/wp\/v2\/product_cat?post=71431"},{"taxonomy":"product_tag","embeddable":true,"href":"https:\/\/medsbase.com\/cs\/wp-json\/wp\/v2\/product_tag?post=71431"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}