AICAR

What it is

AICAR is not a peptide. It is a nucleoside, a small molecule related to a building block of DNA, that the body also makes in tiny amounts. Inside cells it is converted to a compound that mimics AMP and switches on AMPK, the cellular energy sensor that is turned on by exercise and fasting.

It became known after a 2008 mouse study reported improved endurance in sedentary mice given AICAR, which led to it being called an exercise mimetic. It is sold in the research chemical market and has a reputation in endurance sport, which is why the World Anti-Doping Agency bans it.

Its drug name is acadesine. It has been tested in people in other settings, such as protecting the heart during bypass surgery and in leukaemia, but it was never approved for metabolic or performance use.

History

AICAR has been used in research since the 1980s. Acadesine was developed as a heart-protection drug during bypass surgery and ran through late-stage trials that did not deliver an approved indication. The 2008 mouse endurance work is what brought it to wider attention. It has been on the WADA prohibited list for years.

How it works

AICAR is taken up by cells and converted to ZMP, which looks like AMP to the cell. That activates AMPK, which pushes cells toward burning fat and glucose, making new mitochondria and taking up more sugar. In mice that translates into more endurance and better glucose handling. Whether the same happens in people at the doses used outside of research is unproven.

Dosage

• There is no established human dose for fat loss, endurance or any grey-market use. Human trials gave it intravenously for heart surgery and other conditions.
• Community reports vary widely, with doses in the tens of milligrams per injection, because the mouse studies used large doses per kilogram. Scaling mouse doses to people is unreliable.
• Typical courses reported are a few weeks, then a break. These come from forums, not trials.

How it is taken

• Subcutaneous injection with a 29-31G insulin syringe is the usual route. Because the doses are large compared with real peptides, injection volumes can be sizeable.
• Rotate sites and watch for irritation.

How to reconstitute

• For a 50 mg vial, adding 2.5 ml of bacteriostatic water gives 20 mg/ml. On a 1 ml (100-unit) insulin syringe, 25 units (0.25 ml) is 5 mg and 50 units (0.5 ml) is 10 mg.
• AICAR can be slower to dissolve than short peptides. Gentle swirling, and sometimes slight warming to room temperature, helps. Do not shake or heat strongly. If it will not fully dissolve, more water gives a lower concentration.
• Check the label on your own vial and work from that.

How it should arrive

A sealed vial containing white to off-white powder or a solid cake. As a small molecule it can look more crystalline than a fluffy peptide cake.

How it should look once reconstituted

A clear, colourless solution. Any cloudiness or particles that do not clear with gentle swirling are a bad sign.

What to expect, and when

• No reliable human timeline exists for performance or fat-loss use.
• Animal effects on endurance appeared after a few weeks of daily dosing.
• If you see nothing in a few weeks, that is consistent with the human evidence.

Side effects

• Injection-site pain or irritation.
• Nausea, tiredness or low blood sugar-type symptoms have been reported.
• Raised uric acid is a known effect of the drug in clinical work, which can matter for gout.
• Headache and lightheadedness reported anecdotally.

Risks

• Banned by WADA at all times for competitive athletes, and it is readily detected in tests.
• Very limited human data for this kind of use. The exercise-mimetic promise comes mainly from mice.
• It can raise uric acid, which is a concern for anyone with gout or kidney problems.
• It can lower blood glucose, relevant if you take diabetes medication.
• It acts on a fundamental cell energy pathway, and chronic activation has not been studied for safety in healthy people.
• Quality varies like any grey-market chemical.

Potential gains

• In mice, improved endurance and metabolic markers.
• In people, no strong evidence that it improves performance or helps fat loss at doses used outside research.
• As a research tool it is useful for studying AMPK.

Other useful information

AICAR gets lumped in with peptides because it is sold alongside them, but it is a different kind of compound, so do not assume peptide handling or safety knowledge applies. If the aim is better metabolic health, the most reliable AMPK activators are exercise and fasting-type changes, and metformin (prescription) is the best-studied drug that nudges the same pathway.