AICAR

Human clinical Weight Loss & Metabolism In 1 protocol 3 sources

AICAR (Acadesine) is an AMP analog that directly activates AMP-activated protein kinase (AMPK), a master regulator of cellular energy metabolism. Research indicates it can mimic the metabolic effects of exercise, enhancing endurance, increasing fatty acid oxidation, and improving glucose uptake in muscle tissues.

01Dosing reference

Amount

10-50 mg/day (highly variable in research)

Frequency

Daily or pre-workout

Cycle

4-8 weeks on, 4 weeks off

Reference figures, not a recommendationThese values reflect amounts described in the literature and vendor documentation this database indexes. Use the reconstitution calculator to convert them into syringe units.

02Mechanism of action

AMPK Activation

AICAR enters cells and is phosphorylated to ZMP, which mimics AMP and directly activates AMPK.

Metabolic Shift

Activated AMPK stimulates glucose uptake, lipid oxidation, and mitochondrial biogenesis while inhibiting energy-consuming processes.

Exercise Mimetic Effects

This leads to enhanced endurance, reduced body fat, and improved metabolic markers without actual physical exertion.

03Human evidence

Improved outcomes in cardiac surgery

Clinical trials (e.g., CABG surgery) showed acadesine (AICAR) reduced the incidence of early cardiac death and myocardial infarction, though phase III trials had mixed results.

Potential in metabolic disorders

Early human studies explored its use in metabolic conditions, showing it can decrease hepatic glucose production, though poor oral bioavailability limits its clinical use.

04Preclinical evidence

Enhanced endurance in sedentary mice

Mouse models demonstrated that AICAR administration increased running endurance by 44% without prior training, highlighting its 'exercise in a pill' potential.

Reversal of metabolic syndrome

Animal studies showed AICAR improved insulin sensitivity, reduced adiposity, and lowered inflammation in diet-induced obese mice.

05What is known vs. unknown

Reasonably established

Directly activates AMPK, the body's cellular energy sensor.
Promotes mitochondrial biogenesis and fatty acid oxidation.
Often referred to as an 'exercise mimetic' due to its ability to replicate metabolic benefits of training.
Has been investigated clinically under the name Acadesine for cardiovascular protection during surgery.

Unknowns & limits

Poor oral bioavailability requires high doses or intravenous/subcutaneous administration.
Long-term safety of chronic AMPK activation in humans is not fully understood.
Extremely short half-life necessitates frequent dosing in research settings.

06Safety & regulatory context

Regulatory statusAICAR is not FDA-approved for general use or metabolic disorders, though it was investigated clinically (as Acadesine) for cardiac surgery. It is banned by the World Anti-Doping Agency (WADA) due to its performance-enhancing effects. Potential side effects in research include changes in blood flow, potential heart tissue enlargement with chronic use, and uric acid accumulation. It remains strictly a research chemical for most applications.

07Compared with GW501516 (Cardarine)

AICAR vs. GW501516 (Cardarine)

Key difference

AICAR directly activates AMPK, whereas Cardarine is a PPAR-delta receptor agonist.

When researchers discuss each

Both are studied as exercise mimetics and endurance enhancers, but AICAR works on the energy-sensing pathway (AMPK) while Cardarine works on gene transcription related to lipid metabolism.

08Appears in protocols

⚡ Advanced Metabolic Protocol

50 mg/day5 days on / 2 days off

09Glossary

AMPK

AMP-activated protein kinase, an enzyme that plays a crucial role in cellular energy homeostasis.

Exercise Mimetic

A compound that replicates the physiological benefits of exercise without physical exertion.

Mitochondrial Biogenesis

The process by which cells increase their mitochondrial mass, improving energy production.

10Knowledge check

Q1By what primary mechanism does AICAR exert its metabolic effects?

Q2Why is AICAR often referred to as an 'exercise mimetic' in preclinical research?

Q3Considering the human clinical data on AICAR for cardiac surgery, which interpretation is best supported by the dossier?

Q4Which statement best describes how AICAR and GW501516 (Cardarine) differ in their primary biochemical target?

Q5Which statement about AICAR's regulatory or safety status is supported by the dossier?

11Sources

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Research and educational use onlyNothing on this site is medical advice, a prescription, or a recommendation for human use. Compounds documented here are research chemicals. Consult a qualified clinician before making any health decision.