AICAR (acadesine)
MetabolicPhase 3Also known as: Acadesine, AICA riboside, AICA ribonucleoside, 5-aminoimidazole-4-carboxamide riboside, GP-1-110, NSC-105823
AICAR is a nucleoside analog of adenosine. Under the drug name acadesine it was developed by Gensia Pharmaceuticals as an adenosine-regulating agent meant to protect the heart during bypass surgery, and the rights later moved through several companies including Schering-Plough for the cardiac program and Advancell and Protherics for a separate blood-cancer program, which received European orphan drug status for B-cell chronic lymphocytic leukemia (PMID: 18457469).
Overview
At A Glance
AICAR enters cells through nucleoside transporters and is phosphorylated by adenosine kinase to ZMP, an AMP mimetic. ZMP reproduces both activating effects of AMP on AMP-activated protein kinase, allosteric activation and promotion of phosphorylation by upstream AMPK kinase, with…
Overview
AICAR is a nucleoside analog of adenosine. Under the drug name acadesine it was developed by Gensia Pharmaceuticals as an adenosine-regulating agent meant to protect the heart during bypass surgery, and the rights later moved through several companies including Schering-Plough for the cardiac program and Advancell and Protherics for a separate blood-cancer program, which received European orphan drug status for B-cell chronic lymphocytic leukemia (PMID: 18457469). It has never been approved for sale as a medicine in any country. Inside a cell, AICAR is phosphorylated to a molecule called ZMP that looks enough like AMP to switch on AMP-activated protein kinase, the enzyme that acts as a low-energy sensor. In isolated rat liver cells this happened without changing the actual ATP, ADP or AMP content of the cell, which is why AICAR became a standard laboratory tool for turning AMPK on (PMID: 7744080). Switching AMPK on pushes cells toward burning glucose and fat and away from making fat and cholesterol. The reputation AICAR has in fitness circles comes from one mouse experiment. Sedentary mice given AICAR by daily intraperitoneal injection for four weeks ran 44 percent longer on a treadmill than untreated mice, and the authors described the AMPK and PPAR-delta pathway as a target for exercise-mimicking drugs (PMID: 18674809). AICAR also improved muscle function in dystrophin-deficient mdx mice (PMID: 22908954). Human work looks different. In healthy men, intravenous AICAR roughly doubled glucose uptake into leg muscle but raised whole-body glucose disposal by only about 7 percent (PMID: 17513706). In men with type 2 diabetes, an intravenous infusion lowered liver glucose output and circulating free fatty acids (PMID: 18709353). A follow-up study found the muscle response is blunted with older age rather than by diabetes itself (PMID: 19190259). None of these were exercise or body-composition studies, and no published human trial has measured endurance or muscle mass after AICAR. Where large human trials do exist, they were negative. RED-CABG randomized 3080 bypass surgery patients to acadesine or placebo and was stopped early for futility, with no reduction in death, stroke or severe left ventricular dysfunction (PMID: 22782417). A phase I/II study in relapsed leukemia established a maximum tolerated intravenous dose and reported hyperuricemia, transient anemia and thrombocytopenia, renal impairment and infusion-related hypotension (PMID: 23228986). What sells online as AICAR is a lyophilized powder in a vial. The studied product was a hospital intravenous infusion made to pharmaceutical standards, which is not the same thing as vialed powder from a research chemical supplier.
Potential Research Fields
Chemical Information
IUPAC Name
Not yet available
CAS Number
2627-69-2
Molecular Formula
C9H14N4O5
Molecular Mass
258.23 g/mol
Dosing & Protocols
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Interactions
Contraindications
Mechanism-based: because acadesine is metabolized mainly to uric acid in humans, it is a poor fit for anyone with gout, hyperuricemia or impaired kidney function (PMID: 8227467; PMID: 23228986). Infusion-related hypotension was reported in the leukemia study, so people on blood pressure lowering therapy face an additive effect. Prohibited in tested sport under WADA section S4.4. No pregnancy, lactation or pediatric safety data exist.
Research Disclaimer
This interaction data is compiled from published research and community reports. It may not be exhaustive. Always consult a healthcare professional before combining compounds.
$49.99
$0.9998
1
1
vial
| Vendor | Product | Form | Qty | Price | $/mg | Coupon | |
|---|---|---|---|---|---|---|---|
 |
AICAR 50 mg | vial | 1 vial (50 mg)● In Stock | $49.99BEST | $1.000 | — |
Tracking since Sep 7, 2026 · 1 data point
Vendors Selling AICAR (acadesine)
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View Full Dosage Guide →
Protocols, calculator & safety for AICAR (acadesine)
Research Score
0 PubMed studies
Quality Indicators
Data Completeness
63%Quick Facts
Half-Life
Intact acadesine was measurable in plasma for only about 2 hours after a short intravenous infusion in four healthy men, with total plasma clearance of 2.2 L/h/kg and negligible protein binding; radiolabeled drug-derived material had an apparent terminal half-life of about one week, reflecting metabolites rather than parent compound (PMID: 8227467)
Molecular Weight
258.23 g/mol
Administration
Intravenous infusion (human trials), Intraperitoneal injection (rodent studies)
CAS Number
2627-69-2
Trial Phase
Phase 3
Research Disclaimer
This information is for educational and research purposes only. Not intended as medical advice. Consult a healthcare professional before use.
Frequently Asked Questions
What is AICAR (acadesine) used for in research?
AICAR is a nucleoside analog of adenosine. Under the drug name acadesine it was developed by Gensia Pharmaceuticals as an adenosine-regulating agent meant to protect the heart during bypass surgery, and the rights later moved through several companies including Schering-Plough for the cardiac program and Advancell and Protherics for a separate blood-cancer program, which received European orphan drug status for B-cell chronic lymphocytic leukemia (PMID: 18457469). It has never been approved for sale as a medicine in any country.
Inside a cell, AICAR is phosphorylated to a molecule called ZMP that looks enough like AMP to switch on AMP-activated protein kinase, the enzyme that acts as a low-energy sensor. In isolated rat liver cells this happened without changing the actual ATP, ADP or AMP content of the cell, which is why AICAR became a standard laboratory tool for turning AMPK on (PMID: 7744080). Switching AMPK on pushes cells toward burning glucose and fat and away from making fat and cholesterol.
The reputation AICAR has in fitness circles comes from one mouse experiment. Sedentary mice given AICAR by daily intraperitoneal injection for four weeks ran 44 percent longer on a treadmill than untreated mice, and the authors described the AMPK and PPAR-delta pathway as a target for exercise-mimicking drugs (PMID: 18674809). AICAR also improved muscle function in dystrophin-deficient mdx mice (PMID: 22908954).
Human work looks different. In healthy men, intravenous AICAR roughly doubled glucose uptake into leg muscle but raised whole-body glucose disposal by only about 7 percent (PMID: 17513706). In men with type 2 diabetes, an intravenous infusion lowered liver glucose output and circulating free fatty acids (PMID: 18709353). A follow-up study found the muscle response is blunted with older age rather than by diabetes itself (PMID: 19190259). None of these were exercise or body-composition studies, and no published human trial has measured endurance or muscle mass after AICAR.
Where large human trials do exist, they were negative. RED-CABG randomized 3080 bypass surgery patients to acadesine or placebo and was stopped early for futility, with no reduction in death, stroke or severe left ventricular dysfunction (PMID: 22782417). A phase I/II study in relapsed leukemia established a maximum tolerated intravenous dose and reported hyperuricemia, transient anemia and thrombocytopenia, renal impairment and infusion-related hypotension (PMID: 23228986).
What sells online as AICAR is a lyophilized powder in a vial. The studied product was a hospital intravenous infusion made to pharmaceutical standards, which is not the same thing as vialed powder from a research chemical supplier.
What forms does AICAR (acadesine) come in?
AICAR (acadesine) is available in vial form.
How much does AICAR (acadesine) cost?
Prices start at $49.99 across 1 verified vendor.
How do I compare AICAR (acadesine) vendors?
Compare prices, payment methods, shipping, and COA scores across 1 vendor.
Research Tools
Related Compounds
View AllAmlexanox
MetabolicFDA ApprovedAmlexanox is an old anti-inflammatory drug with a second life.
Berberine
MetabolicPreclinicalBerberine is an isoquinoline alkaloid — a naturally occurring plant secondary metabolite with a characteristic yellow color — extracted from the roots, rhizomes, stems, and bark of several plant genera including Berberis (barberry, Oregon grape), Coptis (goldthread), Hydrastis (goldenseal), Phellodendron (Amur cork tree), and Tinospora (guduchi).
Cardarine (GW501516)
MetabolicDiscontinuedCardarine is the market name for GW501516, a synthetic agonist of the nuclear receptor PPAR-delta developed by GlaxoSmithKline as a treatment for low HDL cholesterol and the lipid problems that travel with metabolic syndrome.
Metformin
MetabolicPreclinicalMetformin is a biguanide-class oral antihyperglycemic medication that has been in continuous clinical use since 1957 (in France under the brand name Glucophage) and is now the most-prescribed diabetes medication worldwide with over 150 million prescriptions annually.
SLU-PP-915
MetabolicPreclinicalSLU-PP-915 is an experimental agonist of the estrogen-related receptors, a family of three orphan nuclear receptors called ERR-alpha, ERR-beta and ERR-gamma that control genes for mitochondrial biogenesis, oxidative phosphorylation, fatty acid oxidation and the Krebs cycle.
Sobetirome (GC-1)
MetabolicDiscontinuedSobetirome, also called GC-1 and later QRX-431, is a synthetic analog of thyroid hormone made in Thomas Scanlan laboratory and first described in 1998 as a high-affinity, subtype-selective agonist for the thyroid hormone receptor (PMID: 9653548).
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