AICAR
FDA APPROVAL PENDING
Metabolic
AICAR
Performance
0
Amino acids
Molecular weight
Peptide
Type
AICAR (acadesine) is a nucleoside analog small molecule — not a true peptide — that activates AMP-activated protein kinase (AMPK) by accumulating intracellularly as ZMP, mimicking an energy-depleted cellular state. It has been evaluated in human Phase III clinical trials (the RED-CABG trial, 300 sites, 7 countries) for cardioprotection during coronary artery bypass surgery, and is explored in research for exercise mimicry, metabolic modulation, and oncology applications. AICAR is not FDA-approved for any indication and is banned by WADA in competitive sport.
Top researched benefits
Overview of AICAR
AICAR is phosphorylated intracellularly by adenosine kinase to form ZMP, an AMP mimetic that allosterically activates AMPK by binding its gamma subunit. AMPK activation then inhibits acetyl-CoA carboxylase (ACC), reduces malonyl-CoA, increases fatty acid oxidation, upregulates GLUT-4-mediated glucose uptake, and drives mitochondrial biogenesis; additional AMPK-independent effects include inhibition of NF-kB and proteasomal degradation of the G2/M phosphatase cdc25c.
metabolic
- 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.
performance
- Animal studies showed increased running endurance; human data limited.
- AMPK activation promotes new mitochondria formation over time.
cardioprotection
- Original clinical interest; may protect heart tissue during reduced blood flow.
Typical Dose
25mg per day
Frequency
once daily
Cycle Duration
up to 2 weeks, maximum 3 cycles per year with 1–2 month washout
Storage
Lyophilized/powder: -20°C long-term (stable up to 3 years), or 2–8°C for up to 36 months, protected from light. Reconstituted in bacteriostatic water: store at 2–8°C and use within 28 days; aliquots stable at -20°C for 3–6 months.
No visual available
Due to this peptide having no amino acids, there is no molecular chain to display.
Chemical Makeup
Key benefits
Increases running endurance by up to 44% in rodent studies by promoting slow-twitch muscle fiber gene expression and mitochondrial biogenesis
Activates AMPK to inhibit acetyl-CoA carboxylase, reducing malonyl-CoA and increasing mitochondrial fatty acid oxidation without exercise
Upregulates GLUT-4 translocation in skeletal muscle, improving glucose uptake and insulin sensitivity via an insulin-independent pathway
Demonstrated cardioprotective properties in multiple randomized human trials evaluating reduction of myocardial ischemic injury during coronary artery bypass grafting
Community interest
This peptide is still gaining traction in the community.
AMPK Activator | Endurance & Metabolic Research
This overview is informational and based on aggregated descriptions from studies and user reports.
Was it helpful?YesNoAICAR Molecular Information
View the scientifc details of AICAR.
Molecular Weight
258.234DaChain Length
0Amino AcidsType
PeptideAICAR Protocols
Subcutaneous injection is the primary delivery route used in research-community AICAR protocols, targeting systemic AMPK activation for endurance, metabolic health, and insulin sensitivity. Note that research-community SubQ doses (25–50 mg/day) are far lower than the IV infusion doses used in clinical cardiac surgery trials (~42 mg/kg over 7 hours); the SubQ doses represent community-established conventions intended to reduce nephrotoxicity risk rather than clinically validated thresholds. Cycles are strictly limited to 14 days with a 1–2 month washout period. Injection sites are rotated across the abdomen, thighs, and upper arms.
| Goal | Dosage | Frequency | Route |
|---|---|---|---|
| Establish AMPK activation tolerance before escalating; minimize nephrotoxicity and neurological risk in first-time users | 25 | 1 day range | SubQ |
| Simulate exercise-mimetic AMPK activation on non-training days to improve aerobic capacity without interfering with anabolic signaling from resistance training | 50 | 1 day range | SubQ |
| Reduce total weekly AICAR exposure while sustaining AMPK-driven fat oxidation and GLUT4 upregulation across a 14-day cycle | 50 | 3 week range | SubQ |
| Improve skeletal muscle glucose uptake and reduce fasting insulin through sustained low-dose AMPK activation over a 14-day window | 25 | 1 day range | SubQ |
| Achieve greater mitochondrial biogenesis and endurance adaptation by progressively increasing AICAR dose over an 8–12 week research timeline with structured escalation | 50 | 1 day range | SubQ |
| Target AMPK-mediated suppression of inflammatory signaling in a short, conservative cycle to reduce systemic inflammation without exceeding the 14-day neurological safety window | 25 | 1 day range | SubQ |
Reconstitution Instructions
Materials needed:
Steps to reconstitute
- Allow the AICAR lyophilized powder vial to reach room temperature before handling
- Draw 3.0 mL of bacteriostatic water into a sterile syringe
- Insert the needle through the rubber stopper of the AICAR vial at an angle, pointing toward the vial wall
- Inject the bacteriostatic water slowly down the vial wall — never directly onto the powder
- Gently swirl or roll the vial until fully dissolved — do not shake or vortex
- The resulting concentration is approximately 16.7 mg/mL (50 mg per 3.0 mL)
- Label the vial with the date of reconstitution and refrigerate at 2–8°C, protected from light
- Use a fresh insulin syringe to draw the calculated dose volume for injection
- Clean the injection site (abdomen, thigh, or upper arm) with an alcohol swab and allow to dry completely
- Pinch a skinfold and insert the needle at a 45–90° angle into subcutaneous tissue
- Inject steadily without aspiration, then withdraw the needle and apply light pressure with gauze
- Rotate injection sites daily to prevent lipohypertrophy
- Discard reconstituted solution after 4 weeks; do not refreeze after reconstitution
AICAR Cycle
The AICAR Cycle section explains how long a typical cycle lasts and what to expect during each phase. Over time, your body can become less responsive with continuous use.
Taking breaks between cycles may help maintain effectiveness and support better overall results.
- Week 1-2
- Subtle changes in energy levels; body adjusting to AMPK activation
- Week 3-4
- Potential improvements in endurance capacity and metabolic markers
- Week 5-8
- Cumulative metabolic adaptations; enhanced fat oxidation
- Week 8-12
- Full effects on mitochondrial density and metabolic efficiency
Dosing tools
AICAR Peptide Dosage Calculator
Calculate peptide doses with our visual syringe guide.
mg
Enter the total amount of peptide in the vial in milligrams (as stated on the label).
The dose you want to inject per administration, in mcg or mg.
1,000 mcg = 1 mg
1 mL
2 mL
3 mL
5 mL
Custom
Volume of bacteriostatic water you add to reconstitute the powder. Use BAC water for preservation.
Injection Results
Based on your vial and dilution inputs.
AICAR
SINGLE COMPOUNDVolume per injection
0.05
mL
Concentration
10.00
mg/mL
Doses per vial
20
doses
Total injections per vial
20 injections
How it works
Based on a 10 mg AICAR vial diluted with 1 mL of bacteriostatic water, each 500 mcg injection equals 0.05 mL.
1mL / 100 units
5 units
0.050 mL
Reference Guide
Dosing Cycle
- Peptide
- AICAR
- Dosing
- 25mg per day
- Dosing Frequency
- once daily
- Cycle Duration
- up to 2 weeks, maximum 3 cycles per year with 1–2 month washout
- Storage
- Lyophilized/powder: -20°C long-term (stable up to 3 years), or 2–8°C for up to 36 months, protected from light. Reconstituted in bacteriostatic water: store at 2–8°C and use within 28 days; aliquots stable at -20°C for 3–6 months.
Note: Triple agonist; microdose for fewer side effects
Reconstitution Tips
- Use bacteriostatic water (BAC) — contains 0.9% benzyl alcohol for preservation
- Inject water slowly — aim down the vial wall, not directly onto powder
- Never shake — gently swirl or roll the vial until dissolved
- Store properly — refrigerate at 2-8°C after reconstitution
- Use within 28 days — most reconstituted peptides remain stable for about 4 weeks
- Keep sterile — always clean vial tops with alcohol before drawing
Side effects
Contraindications
Diabetes (risk of hypoglycemia)
Cardiac conditions
Pregnancy or breastfeeding
Competitive athletes (WADA prohibited)
Stop signs
Severe hypoglycemia symptoms
Lactic acidosis symptoms (muscle pain, weakness, difficulty breathing)
Unusual cardiac symptoms
Severe fatigue or weakness
Bad signs
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Frequently asked questions
What is a peptide dosage calculator?
A peptide dosage calculator is a free tool that converts your vial size, bacteriostatic water volume, and target dose into an exact syringe draw volume. Instead of doing the reconstitution math by hand, you enter three inputs and instantly get the concentration of your solution and how many milliliters or syringeunits to draw. This calculator works for single peptide compounds and multi-peptide blends.
How do I calculate peptide dosage from a vial?
To calculate your peptide dose, divide the total peptide content of your vial in micrograms by the volume of bacteriostatic water you added in milliliters. This gives you your solution concentration in mcg/mL. Then divide your target dose by that concentration to get your draw volume. For example, a 5mg (5,000 mcg) vial reconstituted with 2mL of BAC water gives a concentration of 2,500 mcg/mL. A 250 mcg dose would require drawing 0.1mL. This calculator automates all of those steps instantly.
How much Bacteriostatic water should I add to a peptide vial?
Most people add 2mL to 3mL of bacteriostatic water per vial, but the right amount depends on the dose you want to draw and the syringe size you are using. Adding 1mL to a 5mg vial gives you a concentration of 5,000 mcg/mL, making each dose very small in volume. Adding 2mL gives you 2,500 mcg/mL, which is easier to measure on a standard insulin syringe. A general guideline is to choose a volume that puts your typical dose somewhere between 10 and 30 units on a U-100 syringe. Use the calculator above to test different water volumes and find what works for your dose.
How are peptides different from proteins?
Both are made of amino acids, but peptides are much smaller than proteins. Because of their tiny size, peptides can act like tiny messengers in the body, sending specific signals to your cells to tell them exactly what to do.
AICARResearch References
AICAR is a phase 3 compound
AICAR
AICAR is a phase 3 compound
AMPK and Exercise: Glucose Uptake and Insulin Sensitivity
Review of AMPK role in exercise-induced metabolic adaptations and AICAR as pharmacological activator.
2012
AICAR Mouse Endurance Study
Mice treated with AICAR showed 44% increase in running endurance without training.
2008
Calculate peptide dosages
Learning how to calculate a peptide dose? Use our beginner-friendly peptide dosage, blend, and accumulation calculators. Enter vial size, reconstitution volume, and target dose to get exact draw volumes instantly. No guesswork, just clear guidance that helps prevent common mistakes.
