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AICAR
5-Aminoimidazole-4-carboxamide-1-β-D-ribofuranoside; purine nucleoside analogue (not a peptide).
AICAR FAQ
What is AICAR?
AICAR (5-aminoimidazole-4-carboxamide ribonucleoside, also called acadesine) is a purine nucleoside analogue. Inside cells it is converted to ZMP, which mimics AMP and activates AMP-activated protein kinase (AMPK), so it is used as an AMPK activator in laboratory research.
Is AICAR a peptide?
No. AICAR is a nucleoside: an imidazole base attached to a ribose sugar. It contains no amino acids.
Why is AICAR banned in sport?
The World Anti-Doping Agency lists AMPK activators, naming AICAR, among the metabolic modulators in class S4 of its Prohibited List, banned at all times. WADA prohibits it because it is not approved for human therapeutic use and is considered capable of enhancing performance.
AICAR vs. 5-Amino-1MQ
Both are small molecules (neither is a peptide) used in metabolism research, but they act at different points. AICAR is a nucleoside that cells convert to ZMP, an AMP mimic that activates AMP-activated protein kinase (AMPK). 5-Amino-1MQ is a quinolinium compound that inhibits the enzyme nicotinamide N-methyltransferase (NNMT), which sits in the NAD+ salvage and methylation pathways.
5-Amino-1MQ vs. SLU-PP-332
They are different small molecules with different targets. 5-Amino-1MQ inhibits the enzyme nicotinamide N-methyltransferase (NNMT). SLU-PP-332 is a synthetic agonist of the estrogen-related receptors (ERRα, β and γ), nuclear receptors involved in mitochondrial gene programs, developed at Saint Louis University. Neither is a peptide, and neither is FDA approved. MOTS-c, by contrast, is a peptide, and AICAR acts through AMPK.
AICAR vs. MOTS-c
Both are studied in connection with AMPK, but they are different kinds of molecule. AICAR is a synthetic nucleoside that cells convert to ZMP, an AMP mimic that activates AMPK directly. MOTS-c is a 16-amino-acid peptide encoded in mitochondrial DNA; research links it to AMPK indirectly, through the folate cycle and a build-up of the AICAR-related intermediate in cells. Only MOTS-c is a peptide.
What has AICAR been studied for in research?
AICAR is widely used in cell culture and rodent studies as a pharmacological AMPK activator, in research on glucose and lipid metabolism, skeletal muscle and cancer cell biology. Researchers note that ZMP also interacts with other AMP-sensitive enzymes, so controls are needed to attribute findings to AMPK. Under the name acadesine it was investigated in clinical trials, including in people undergoing heart bypass surgery. Findings in cells or animals do not establish effects in people.
Is AICAR FDA approved?
No. AICAR (acadesine) was investigated in clinical trials, including a large trial in people undergoing coronary artery bypass surgery that was stopped early, but it has never been approved by the FDA or any other drug regulator. It is sold here strictly as a research compound.
How does AICAR activate AMPK?
AICAR enters cells through nucleoside transporters and is phosphorylated by adenosine kinase to ZMP (AICAR monophosphate). ZMP resembles AMP and binds the regulatory γ-subunit of AMP-activated protein kinase (AMPK), promoting phosphorylation and activation of the kinase without changing the cell's actual AMP-to-ATP ratio. ZMP is also a normal intermediate of purine biosynthesis.
What does AICAR stand for?
AICAR stands for 5-aminoimidazole-4-carboxamide ribonucleoside (also written as 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside). It is also known by the nonproprietary name acadesine. Its phosphorylated form, ZMP, is sometimes called AICAR ribotide or AICA ribonucleotide. It is a purine nucleoside analogue, not a peptide.
How do you pronounce AICAR?
AICAR is usually pronounced as one word, "AY-car", although some researchers spell out the letters. Its formal nonproprietary name, acadesine, is pronounced "uh-CAD-uh-seen". The abbreviation comes from the compound's chemical name, 5-aminoimidazole-4-carboxamide ribonucleoside. AICAR is a nucleoside, not a peptide, despite being sold alongside peptides.
AICAR vs. ALCAR (acetyl-L-carnitine)
They are unrelated compounds with similar-looking abbreviations. AICAR is a purine nucleoside analogue used in research as an AMPK activator. ALCAR is acetyl-L-carnitine, an acetylated form of L-carnitine, a small amino-acid-derived molecule involved in transporting fatty acids into mitochondria. Neither is a peptide.
AICAR vs. cardarine
They act on different targets. AICAR is a nucleoside that activates AMP-activated protein kinase (AMPK) through its metabolite ZMP. Cardarine (GW501516) is a synthetic agonist of the nuclear receptor PPARδ; its clinical development was abandoned. Neither is FDA approved, and both appear among the metabolic modulators on the World Anti-Doping Agency's Prohibited List.
Does methotrexate inhibit AICAR transformylase?
Yes. In biochemical studies, methotrexate polyglutamates (the forms that build up inside cells) inhibit AICAR transformylase (ATIC), the enzyme that converts ZMP to the next intermediate in purine biosynthesis. This causes ZMP, the phosphorylated form of AICAR, to accumulate in cells, which is why AICAR and its metabolites appear in mechanistic research on methotrexate.
What are the identifiers for AICAR?
AICAR: molecular formula C9H14N4O5; molecular weight 258.23 g/mol; CAS number 2627-69-2. Match these identifiers against the Certificate of Analysis for the lot.
Does AICAR come with a Certificate of Analysis?
Yes. Each lot has its own Certificate of Analysis, linked on this page for the current lot of each size: 50mg (99.52% HPLC purity). Past certificates are archived in the COA library; contact us with the lot number on the vial label if a certificate is missing.
What purity is AICAR?
99.52% (HPLC, current lot). Purity is measured by high-performance liquid chromatography (HPLC) and reported on the lot's Certificate of Analysis.
What sizes of AICAR are available?
AICAR is supplied as lyophilized powder in a sealed vial: 50mg. In stock and dispatched in 1–2 business days. Quantity pricing applies automatically at 5+ and 10+ vials of the same size.
How should AICAR be stored?
Store sealed at −20 °C, dry and protected from light.
More on testing, storage and handling in the full FAQ.
