AICAR: Reference Overview and Reconstitution Notes

Published by the ✔ Medically reviewed by Bryan Le, PharmD, RPhEditorial standards

AICAR research image

What it is

AICAR (5-aminoimidazole-4-carboxamide ribonucleotide, also called acadesine or AICA-riboside) is a nucleoside analogue, not a peptide. Inside the cell it mimics AMP and activates AMP-activated protein kinase (AMPK), a sensor that responds to low cellular energy.

Quick answer: An AMP-mimetic nucleoside and AMPK activator — not a peptide. It is prohibited in sport at all times under WADA category S4.5, and has been continuously since 2009.

In this article

  1. What it is
  2. Research context
  3. Status
  4. Reconstitution and handling
  5. Status in sport
  6. Related reading
  7. Frequently asked questions
  8. What the community gets wrong
For research and educational reference only. Preppin Peppers sells laboratory hardware and materials (reconstitution pens, cartridges, and bacteriostatic water); it does not sell peptides or any substance for consumption. This is educational content, not medical, health, veterinary, dosing, or compounding advice, has not been evaluated by the FDA, and is not intended to diagnose, treat, cure, or prevent any condition, or for human or animal use. Comply with the laws that apply to you and consult a licensed professional for any health decision.

What it is

Chemical structure of AICAR
The chemical structure of AICAR.

AICAR (5-aminoimidazole-4-carboxamide ribonucleotide, also called acadesine or AICA-riboside) is a nucleoside analogue, not a peptide. Inside the cell it mimics AMP and activates AMP-activated protein kinase (AMPK), a sensor that responds to low cellular energy.

Research context

Grouped under weight and metabolic research because AMPK sits at the centre of cellular energy and metabolic regulation. AICAR drew attention after a 2008 paper reported endurance changes in mice, which is also what prompted its prohibition in sport the following year.

As acadesine it has been investigated clinically in other contexts entirely, including cardiac surgery. Those programmes are separate from the metabolic and endurance research it is usually discussed for.

Status

  • Regulatory status: Not FDA-approved for human use. Investigated clinically as acadesine in unrelated indications.
  • Sport status: Prohibited under the WADA Prohibited List, category S4.5 (hormone and metabolic modulators — AMPK activators), at all times, in and out of competition.

Reconstitution and handling

Reconstitution follows the standard math: concentration equals the milligrams in the vial divided by the millilitres of bacteriostatic water added. There is no single correct concentration — it depends on solubility and how large a draw is wanted. If a mix does not go fully clear, add more water. The reconstitution calculator shows concentration, draw size and portions per vial for any volume.

Refrigerate reconstituted vials at 2–8 °C, keep them out of light, wipe stoppers with alcohol before each puncture, and label with the mix date. Discard anything cloudy, discoloured, or with floaters.

Status in sport

AICAR is prohibited. It falls under WADA category S4.5, hormone and metabolic modulators, as an AMPK activator, and is banned at all times — both in and out of competition. The prohibition has been continuously in effect since 2009.

WADA tests for AICAR and its metabolites. Because the body produces AICA-ribonucleotide endogenously, detection methods were developed specifically to distinguish administered AICAR from what occurs naturally.

Reminder: research and educational reference only. Preppin Peppers sells hardware and materials, not peptides. Not medical, dosing, or health advice, not evaluated by the FDA, and not intended for human or animal use.

Frequently asked questions

Is AICAR banned in sport?

Yes. AICAR is prohibited at all times under WADA category S4.5 (hormone and metabolic modulators, AMPK activators), in and out of competition, and has been since 2009. WADA tests for AICAR and its metabolites.

Is AICAR a peptide?

No. AICAR is a nucleoside analogue that mimics AMP inside the cell. It is included in this reference library as a related research compound, not as a peptide.

What does AICAR act on?

It activates AMP-activated protein kinase (AMPK), a cellular energy sensor that responds to low energy states.

What the research community gets wrong about AICAR

  • Calling it a peptide is wrong. AICAR is a nucleoside analogue. It is grouped here as a related research compound; peptide handling assumptions do not automatically transfer to it.
  • Endogenous production does not make it undetectable. The body makes AICA-ribonucleotide naturally, which is why anti-doping methods were built specifically to separate administered AICAR from endogenous background.
  • Vendor labels are not assays. Identity and purity come from a certificate of analysis on the batch in front of you, not from the name printed on a vial.
  • A reconstituted vial does not stay good forever. Compounds in solution break down over time, and rough handling (shaking hard enough to foam) can damage them. Note the reconstitution date and store as your protocol calls for.

Sources

Macro of AICAR lyophilized powder
Close detail of the lyophilized powder.
  1. WADA — The Prohibited List
  2. USADA — What Athletes Should Know About AICAR and Other Prohibited AMPK Activators
  3. PubChem Compound Summary: Acadesine (AICAR)
  4. Bacteriostatic Water for Injection, USP — FDA/DailyMed label (0.9% benzyl alcohol)
  5. Sigma-Aldrich (Merck) — Handling and Storage Guidelines for Peptides and Proteins

✔ Reviewed by Bryan Le, PharmD, RPh

Bryan is a licensed pharmacist (Doctor of Pharmacy, Registered Pharmacist). Reconstituting lyophilized preparations is core pharmacy practice, so he reviews The Lab’s content for technical accuracy and to keep it within a research-and-education scope, with no medical or dosing advice. View profile on LinkedIn.
Get more of The Lab in your Google results
Browse The Lab by topic