AICAR (Acadesine)
5-Aminoimidazole-4-carboxamide Ribonucleotide | AMPK Activator
Community Research
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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.
Molecular Data
Research Indications
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.
Dosing Protocols
Subcutaneous injection once daily. Progressive dosing protocols are common to assess tolerance.
| Goal | Dose | Frequency | Route |
|---|---|---|---|
| Standard Protocol | 1-3mg | Daily | SubQ |
| Gradual Introduction | 1mg → 2mg → 3mg | Daily, titrating over 4 weeks | SubQ |
| Advanced Protocol | 3-5mg | Daily for 8-12 weeks | SubQ |
Reconstitution Instructions
- AICAR lyophilized powder (typically 50mg vial)
- Bacteriostatic water (3.0mL recommended)
- Insulin syringes (29-31 gauge)
- Alcohol swabs
- 1 Allow vial to reach room temperature
- 2 Clean rubber stopper with alcohol swab
- 3 Add 3.0mL bacteriostatic water for ~16.7mg/mL concentration
- 4 Inject slowly along vial wall to avoid foaming
- 5 Gently swirl to dissolve; never shake
- 6 Label with date and store refrigerated at 2-8°C
- 7 Use within 4 weeks of reconstitution
Interactions
What to Expect
Side Effects & Safety
Common Side Effects
- Injection site reactions
- Mild fatigue during adaptation
- Potential hypoglycemia
Stop Signs - Discontinue if:
- Severe hypoglycemia symptoms
- Lactic acidosis symptoms (muscle pain, weakness, difficulty breathing)
- Unusual cardiac symptoms
- Severe fatigue or weakness
Contraindications
- Diabetes (risk of hypoglycemia)
- Cardiac conditions
- Pregnancy or breastfeeding
- Competitive athletes (WADA prohibited)
Quality Checklist
Good Signs
- White to off-white lyophilized powder
- Clear solution after reconstitution
- Certificate of Analysis with purity testing
Warning Signs
- Slight yellowing may occur but should dissolve clearly
Bad Signs
- Discolored or clumped powder
- Cloudy solution after reconstitution
- Particulate matter visible
Frequently Asked Questions
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.
References
- AMPK and Exercise: Glucose Uptake and Insulin Sensitivity(2012)
Review of AMPK role in exercise-induced metabolic adaptations and AICAR as pharmacological activator.
- AICAR Mouse Endurance Study(2008)
Mice treated with AICAR showed 44% increase in running endurance without training.
Disclaimer
This information is for educational and research purposes only. Consult a healthcare professional before use.