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5.  AICAR (acadesine) 

![AICAR (acadesine) molecular structure](/assets/peptide-structure-placeholder-DUmZBF_j.png)

# AICAR (acadesine)

Metabolic Phase 3 

Download  PDF

Also 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).

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) Route:  Intravenous infusion (human trials), Intraperitoneal injection (rodent studies) MW:  258.23 g/mol CAS:  2627-69-2 

Last reviewed: Sep 7, 2026 

[

Metabolic

Category



](/wiki#cat-metabolic)

Phase 3

Research Stage

OverviewChemical InfoDosing & ProtocolsInteractionsResearchCompare Prices1 Related

## Overview

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### At A Glance

Mechanism 

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… 

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)

Routes 

Intravenous infusion (human trials) Intraperitoneal injection (rodent studies) 

Potential Benefits 

Increased treadmill running endurance by 44 percent in sedentary mice given AICAR by daily intraperitoneal injection for four weeks (PMID: 18674809) Roughly doubled skeletal muscle 2-deoxyglucose uptake in healthy men during intravenous infusion (PMID: 17513706) Reduced liver glucose output and plasma non-esterified fatty acids in men with type 2 diabetes during intravenous infusion (PMID: 18709353) Activated AMPK and suppressed fatty acid and sterol synthesis in isolated rat hepatocytes (PMID: 7744080) Improved forelimb and hindlimb strength and reduced muscle damage in dystrophin-deficient mdx mice (PMID: 22908954) 

### 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

AMPK signaling Exercise metabolism Cardioprotection Hematology 

## Chemical Information

IUPAC Name

Not yet available 

CAS Number

2627-69-2

Molecular Formula

C9H14N4O5

Molecular Mass

258.23 g/mol

![AICAR (acadesine) molecular structure](https://pubchem.ncbi.nlm.nih.gov/rest/pug/compound/cid/17513/PNG)

[View on PubChem](https://pubchem.ncbi.nlm.nih.gov/compound/17513)

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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.

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### Vendors Selling AICAR (acadesine)

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### Related Compounds

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[

### Amlexanox

Metabolic FDA Approved 

Amlexanox is an old anti-inflammatory drug with a second life.

t½ Not established in published human pharmacokinetic studies for the oral capsule form; a validated plasma assay has been used for preclinical pharmacokinetics in rats (PMID: 34842293) 

Preclinical View Profile 

](/compound/amlexanox)[

### Berberine

Metabolic Preclinical 

Berberine 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).

Preclinical View Profile 

](/compound/berberine)[

### Cardarine (GW501516)

Metabolic Discontinued 

Cardarine 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.

t½ Not reported in the published human trials; the phase 1 and phase 2 studies described lipid outcomes over two to twelve weeks of oral dosing without publishing a terminal half-life (PMID: 17110604; PMID: 22814748) 

Preclinical View Profile 

](/compound/cardarine)[

### Metformin

Metabolic Preclinical 

Metformin 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.

Preclinical View Profile 

](/compound/metformin)[

### SLU-PP-915

Metabolic Preclinical 

SLU-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.

t½ Not established in humans; in mice it is orally bioavailable and active by both oral and intraperitoneal routes, unlike its predecessor SLU-PP-332 (PMID: 41421047) 

Preclinical View Profile 

](/compound/slu-pp-915)[

### Sobetirome (GC-1)

Metabolic Discontinued 

Sobetirome, 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).

t½ Not established in humans; no peer-reviewed human pharmacokinetic study has been published, and the phase 1 program results were not reported in the peer-reviewed literature (PMID: 19002578) 

Preclinical View Profile 

](/compound/sobetirome)

[

View Full Dosage Guide →

Protocols, calculator & safety for AICAR (acadesine)



](/guides/dosage/aicar)

### Best Price

![Disguised Alpha logo](https://disguisedalpha.com/wp-content/themes/assets/logos/disguised-logo-2x.png)

Disguised Alpha

$49.99

[Buy Now](https://disguisedalpha.com/product/aicar/?coupon=reddit)

1 vendors · 1 listings

### Research Score

30 

0 PubMed studies

### Quality Indicators

Data Completeness

63% 

Description 

Mechanism of Action 

Chemical Data 

Dosing Protocols 

Safety Profile 

PubMed Studies 

Interactions 

Vendor Listings 

### 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

0

[Full Dosage Guide](/guides/dosage/aicar)[Calculate Your Dose](/tools/reconstitution)

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

[

### Peptide Calculator

Reconstitution & syringe units



](/tools/reconstitution)[

### Reconstitution Guide

How to mix, step by step



](/guides/how-to-reconstitute-peptides)[

### Nasal Spray Calc

mL per actuation



](/tools/intranasal)[

### Half-Life Visualizer

Decay curves



](/tools/halflife)

## Related Compounds

[View All](/wiki)

[

### Amlexanox

Metabolic FDA Approved 

Amlexanox is an old anti-inflammatory drug with a second life.

t½ Not established in published human pharmacokinetic studies for the oral capsule form; a validated plasma assay has been used for preclinical pharmacokinetics in rats (PMID: 34842293) 

Preclinical View Profile 

](/compound/amlexanox)[

### Berberine

Metabolic Preclinical 

Berberine 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).

Preclinical View Profile 

](/compound/berberine)[

### Cardarine (GW501516)

Metabolic Discontinued 

Cardarine 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.

t½ Not reported in the published human trials; the phase 1 and phase 2 studies described lipid outcomes over two to twelve weeks of oral dosing without publishing a terminal half-life (PMID: 17110604; PMID: 22814748) 

Preclinical View Profile 

](/compound/cardarine)[

### Metformin

Metabolic Preclinical 

Metformin 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.

Preclinical View Profile 

](/compound/metformin)[

### SLU-PP-915

Metabolic Preclinical 

SLU-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.

t½ Not established in humans; in mice it is orally bioavailable and active by both oral and intraperitoneal routes, unlike its predecessor SLU-PP-332 (PMID: 41421047) 

Preclinical View Profile 

](/compound/slu-pp-915)[

### Sobetirome (GC-1)

Metabolic Discontinued 

Sobetirome, 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).

t½ Not established in humans; no peer-reviewed human pharmacokinetic study has been published, and the phase 1 program results were not reported in the peer-reviewed literature (PMID: 19002578) 

Preclinical View Profile 

](/compound/sobetirome)

Free 2026 Peptide Cheat Sheet — 50 pages, PDF

Reconstitution math, concentration charts, half-lives, and vendor trust tiers. The reference we wish we had on day one.

[Download Free](/guides/peptide-cheat-sheet-download?utm_source=compound-aicar)

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