AICAR
5-Aminoimidazole-4-carboxamide Ribonucleotide · AMPK Activator
AICAR is a cell-permeable nucleoside analog that activates AMP-activated protein kinase (AMPK), a key regulator of cellular energy homeostasis. Originally studied for cardiac ischemia protection, it gained attention as an 'exercise mimetic' due to its metabolic effects.
Overview
AICAR is a cell-permeable nucleoside analog that activates AMP-activated protein kinase (AMPK), a key regulator of cellular energy homeostasis. Originally studied for cardiac ischemia protection, it gained attention as an 'exercise mimetic' due to its metabolic effects.
Once inside cells, AICAR is phosphorylated to ZMP, which mimics AMP and activates AMPK. This triggers metabolic pathways typically activated during exercise: increased glucose uptake, fatty acid oxidation, and mitochondrial biogenesis.
Research indications
What the compound has been studied for, grouped by body system. Effect size is the reported magnitude where it was measured — not a recommendation.
Directly activates the master metabolic regulator through ZMP accumulation.
Increases fat burning through AMPK-mediated pathways.
Enhances glucose uptake independent of insulin in some tissues.
Animal studies showed increased running endurance; human data limited.
AMPK activation promotes new mitochondria formation over time.
Original clinical interest; may protect heart tissue during reduced blood flow.
A large effect in a weak study and a small effect in a strong one are different things. Effect size is never evidence of use in people.
- Class
- Nucleoside analog
- Molecular weight
- 338.21 Da
- Half-life
- ~2.5 h
- Typical dose
- 1-5mg daily
- Frequency
- Once daily
- Cycle length
- 8-12 weeks
- Storage
- Lyophilized: -20°C; Reconstituted: 2-8°C for 4 weeks
Molecular data
- Type
- Nucleoside analog
- Molecular weight
- 338.21 Da
- Half-life
- 150 min
Dosing reference
Doses reported in the literature and by suppliers. These are a record of what has been used in research — reference, never instruction.
| Context | Route | Amount | Frequency |
|---|---|---|---|
| Standard Protocol | SubQ | 1-3mg | Daily |
| Gradual Introduction | SubQ | 1mg → 2mg → 3mg | Daily, titrating over 4 weeks |
| Advanced Protocol | SubQ | 3-5mg | Daily for 8-12 weeks |
Interactions
Both activate AMPK through different mechanisms. Combined use may have additive effects on glucose metabolism.
Different pathways (AMPK vs PPARδ) that may complement metabolic effects. Popular research combination.
Rev-ErbA agonist with complementary metabolic effects.
Quality checklist
- ✓White to off-white lyophilized powder
- ✓Clear solution after reconstitution
- ✓Certificate of Analysis with purity testing
- !Slight yellowing may occur but should dissolve clearly
- ×Discolored or clumped powder
- ×Cloudy solution after reconstitution
- ×Particulate matter visible
What to expect
Safety
- Injection site reactions
- Mild fatigue during adaptation
- Potential hypoglycemia
- Severe hypoglycemia symptoms
- Lactic acidosis symptoms (muscle pain, weakness, difficulty breathing)
- Unusual cardiac symptoms
- Severe fatigue or weakness
- Diabetes (risk of hypoglycemia)
- Cardiac conditions
- Pregnancy or breastfeeding
- Competitive athletes (WADA prohibited)
FAQ
Does AICAR actually work as an 'exercise mimetic' in humans?
Animal studies show AICAR increased running endurance by 44% without training. However, this was mice, not humans. Humans have never been adequately tested for AICAR's endurance effects, so calling it an exercise mimetic is speculative. The compound does activate AMPK and increase fat oxidation, but real-world performance gains in people are unproven.
Is AICAR banned in sports and why?
Yes, AICAR is WADA prohibited. While it's not anabolic per se, it provides competitive advantage through enhanced metabolic efficiency and endurance. Athletes competing under WADA rules must avoid it entirely due to testing likelihood and strict liability regulations.
What's the risk of hypoglycemia on AICAR if I'm not diabetic?
AICAR increases glucose uptake independent of insulin in some tissues, creating theoretical hypoglycemia risk especially in non-diabetics with normal insulin sensitivity. Diabetics face more serious risk, which is why AICAR is contraindicated in diabetes. Monitor blood glucose closely, particularly during initial doses.
How does AICAR differ from GW501516 for metabolic enhancement?
AICAR activates AMPK, the master metabolic regulator, increasing fatty acid oxidation and glucose uptake. GW501516 is a PPARδ agonist with different downstream effects. They're often stacked because they target complementary pathways—AMPK plus PPARδ activation produces synergistic metabolic effects.