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AICAR

Metabolic & Weight Loss

AICAR (5-Aminoimidazole-4-carboxamide ribonucleotide) is a nucleotide analog and AMPK agonist that mimics cellular energy stress, leading to enhanced fat oxidation, glucose uptake, and endurance capacity. It has been studied in metabolic and athletic contexts for its ability to trigger exercise-like effects without physical activity. AICAR is also used experimentally for improving mitochondrial function and insulin sensitivity. Best suited for short-term cycles with careful monitoring to avoid over-activation of AMPK. All data is based on animal or cellular models.

Reconstitute
3 mL BAC + 50mg vial
167 mcg/unit
Daily Range
30–100 mg Intravenous (IV)
Once
Standard Dose
50 mg
Cycle
4–8 weeks
then reassess
AICARAMPK agonistMetabolic enhancement

Dosing & Reconstitution Guide

In rodent studies, AICAR is typically dosed at 0.5–1.5 mg/g (500–1500 mg/kg) via injection. These studies do not translate to human use or safety.

Standard / Gradual Approach

50mg Vialstandard
PhaseDoseVolume
Weeks 1–21,000 mcg (1 mg)6 units (0.06 mL)
Weeks 3–42,000 mcg (2 mg)12 units (0.12 mL)
Weeks 5–83,000 mcg (3 mg)18 units (0.18 mL)

Standard / Gradual Approach

50mg Vialadvanced
PhaseDoseVolume
Weeks 1–22,000 mcg (2 mg)12 units (0.12 mL)
Weeks 3–63,000 mcg (3 mg)18 units (0.18 mL)
Weeks 7–125,000 mcg (5 mg)30 units (0.30 mL)

Protocol Summary

Intravenous (IV): Once · Dose range 30–100 mg with gradual titration
Cycle Length: 4–8 weeks typical; reassess before extending

Frequency & Cycling

IV

Administer 50 mg/kg IV once daily, commonly in the morning or before exercise. Cycle for 4–8 weeks, followed by an equal or longer off period. Do not exceed 8-week continuous cycles due to potential AMPK desensitization. Often used in metabolic or endurance performance protocols.

🧪 Quick Start

Vial Size
50 mg
BAC Water
3 mL
Concentration
16.7 mcg/unit
Starting Dose
1,000 mcg (1 mg) (6 units (0.06 mL))
Maintenance Dose
3,000 mcg (3 mg) (18 units (0.18 mL))

Potential Benefits & Use Cases

AICAR is not approved for human consumption. Information presented here is for educational and research purposes only.
Increases endurance by 44% in sedentary mice without training, demonstrating exercise-mimetic effects (preclinical)
Increases mitochondrial enzymes, fatty-acid oxidation capacity, and skeletal muscle glucose uptake (preclinical)
Demonstrates cardiac protection — prevents doxorubicin-induced heart failure and blocks cardiac hypertrophy (preclinical)
Promotes conversion from glycolytic to oxidative muscle fibers (preclinical)
Shows tolerable safety up to 210 mg/kg single IV dose in human acadesine trials (human trial)
Clinical data Strong preclinical Limited data

Mechanism of Action

→AMPK Activation
→Mimics exercise-induced energy changes

Lifestyle & Optimization

timing

Administer before exercise to amplify AMPK activation.

diet

Balanced protein-adequate diet. Monitor hydration during endurance activities.

exercise

Structured exercise to amplify AMPK benefits.

sleep

Quality sleep (7–9 hours).

Peptide Research & Preclinical Studies

Evidence-Based Research Findings

Study TitleType
U.S. Anti-Doping Agency (USADA) — What Athletes Should Know About AICAR and Other Prohibited AMPK Activated Protein Kinase Activators (official guidance, 2022)Reference
PubMed — Doping control study of AICAR; endurance enhancement in sedentary animals (Drug Testing and Analysis, 2017)Reference
PMC (PubMed Central) — AICAR treatment for 14 days normalizes obesity-induced dysregulation in skeletal muscle (Am. J. Physiol., 2010)Reference
MDPI (International Journal of Molecular Sciences) — AICAR prevents and reverses diabetic polyneuropathy by regulating mitophagy (2024)Reference
PubMed — Acadesine (AICAR) Phase I/II study; maximum tolerated dose 210 mg/kg IV (Cancer Chemotherapy and Pharmacology, 2013)Reference
Cell Signaling Technology — AICAR (Acadesine) Product Data Sheet; AMPK activation mechanism and cellular effects (2021)Reference
JAMA Network — Effect of adenosine-regulating agent acadesine in cardiac surgery; IV infusion protocol (JAMA, 1997)Reference
Endocrinology (Oxford University Press) — AICAR stimulates fatty acid oxidation via β-adrenergic pathway in skeletal muscleReference
PMC — AICAR enhances glucose transport and mitochondrial function in muscle cellsReference
Biolog Life Science Institute — Technical Information about AICAR-5′-MP (AICA Ribonucleotide); stability and handling (2018)Reference

Side Effects & Safety

Long-Term Safety Data

• Remains experimental; no confirmed clinical benefit in humans established, long-term risks unknown

🧮 Dose Calculator

Concentration
166.7
mcg/unit
Draw Volume
3
units (0.030 mL)
For a 500 mcg dose, draw 3 units on a U-100 insulin syringe
🧬

Bioavailability & Absorption

SubQ Injection
Not typically used.
Oral Administration
Poor bioavailability due to first-pass metabolism.
Half-Life
Approximately 1-1.5 hours IV in animal studies.
Degradation
Metabolized primarily in the liver with renal excretion.
Tissue Specificity
Primarily affects muscle and liver tissues.
⚗️

Peptide Details

Molecular Weight
258.23
Formula
C9H14N4O5
Sequence
Not applicable
⚖️

Legal Status & Regulatory

RegionStatus
FDANot Approved
EUNot Approved
AustraliaNot Approved
CanadaNot Approved

Storage Instructions

Lyophilized (Powder)
freeze at −20 °C (−4 °F); after reconstitution, refrigerate at 2–8 °C (35.6–46.4 °F) for up to 4 weeks; avoid freeze–thaw cycles
Reconstituted (Mixed)
Refrigerate at 2–8 °C (35.6–46.4 °F); use bacteriostatic water; stable ~4 weeks