Metabolic
AICAR Dosage Protocol
An AMPK activator and exercise mimetic studied for metabolic endurance and mitochondrial biogenesis. Complete dosing guide, mechanism overview, and peer-reviewed references.
Last reviewed March 2025 · 2 cited sources
Reconstitution
Add 5.0 mL BAC water → 10 mg/mL
Daily dose range
50–150 mg (titrated)
Unit math (U-100 syringe)
1 unit = 0.01 mL ≈ 100 mcg
Storage (lyophilized)
Freeze at −4 °F · Reconstituted: 36–46 °F · Use within 28 days
Dosing & Reconstitution Guide
The protocol below uses a 5.0 mL reconstitution volume to keep injection units comfortably above 10 on a standard U-100 insulin syringe, reducing measurement error. Doses are titrated as shown below.
| Phase |
Daily dose |
U-100 units |
Injection volume |
| Standard | 50–150 mg IV/SC | Variable | Variable |
Route: IV / Subcutaneous · Frequency: Daily · Cycle: 4–8 weeks
Reconstitution steps
01
Draw 5.0 mL of bacteriostatic water into a sterile syringe.
02
Inject the water slowly down the interior wall of the peptide vial -never directly onto the powder -to prevent foaming and denaturation.
03
Swirl or roll gently until fully dissolved. Do not shake. The lyophilized powder should dissolve completely within 30–60 seconds.
04
Label the vial with the reconstitution date and concentration (10 mg/mL). Refrigerate at 36–46 °F, protected from light. Use within 28 days.
Research use only. This protocol is derived from published preclinical and early-phase clinical literature. AICAR is not FDA-approved for human use. This information is not medical advice, diagnosis, or treatment. Consult a qualified healthcare professional before beginning any peptide protocol.
Supplies Needed
Estimates below assume the titration schedule listed above.
AICAR vials (50 mg each)
Per cycleAs needed per titration
U-100 insulin syringes
8 weeks56 syringes
12 weeks84 syringes
16 weeks112 syringes
Bacteriostatic water (10 mL bottles)
Alcohol swabs (100-count boxes)
8 weeks2 boxes (~112 swabs)
12 weeks2 boxes (~168 swabs)
16 weeks3 boxes (~224 swabs)
Storage Instructions
Lyophilized (dry powder)
−4 °F
Store frozen in dry, dark conditions. Minimize humidity exposure. Stable for 12–24 months when properly stored.
Reconstituted (in solution)
36–46 °F
Refrigerate after reconstitution. Use within 28 days. Do not refreeze reconstituted solution -freeze-thaw cycles degrade peptide integrity.
Allow refrigerated vials to reach room temperature before opening to minimize condensation uptake. Always inspect for cloudiness or particulates before use -discard if present.
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How AICAR Works
AICAR (5-aminoimidazole-4-carboxamide ribonucleoside) is phosphorylated intracellularly to ZMP, an AMP analog that directly activates AMP-activated protein kinase (AMPK) -the master cellular energy sensor.[1] AMPK activation triggers a cascade of metabolic adaptations including fatty acid oxidation, glucose uptake, and mitochondrial biogenesis through PGC-1α signaling.
In a landmark mouse study, AICAR treatment improved running endurance by 44% in sedentary animals without exercise training, establishing it as one of the first pharmacological exercise mimetics.[2] AICAR is classified as a prohibited substance by WADA due to its performance-enhancing potential. Human clinical data remains limited to metabolic disease contexts.
Observed Effects & Side Effect Profile
The following observations are derived from preclinical literature and limited early-phase human data. They do not constitute clinical claims.
Reported benefits (research literature)
- Direct AMPK activation mimics key metabolic benefits of exercise
- 44% endurance improvement in sedentary mice without training
- Promotes fatty acid oxidation and mitochondrial biogenesis via PGC-1α
- Well-characterized mechanism of action in metabolic research
Known limitations & side effects
- WADA prohibited substance -banned in competitive athletics
- Hypoglycemia risk due to enhanced glucose uptake
- Limited human dosing and safety data for research protocols
- Potential cardiac effects at supraphysiologic AMPK activation levels
- Not FDA-approved for any indication
Lifestyle Considerations
While the following suggestions are not protocol requirements, research on tissue repair and peptide efficacy consistently highlights these as factors that influence outcomes:
01
Protein intake. Collagen synthesis and tissue remodeling require adequate dietary protein. Research generally supports 1.6–2.2 g/kg/day during active recovery periods.
02
Sleep. The majority of tissue repair and growth hormone secretion occurs during deep sleep stages. 7–9 hours of quality sleep per night supports the biological environment in which recovery peptides operate.
03
Activity balance. Avoid complete immobilization (which impedes collagen remodeling) and overuse (which re-injures tissue). Progressive loading appropriate to the injury stage supports functional recovery.
04
Stress management. Elevated cortisol chronically impairs immune function and tissue repair. Evidence-based stress reduction techniques support the recovery environment.
Injection Technique
Standard subcutaneous injection guidance from clinical best-practice references.
01
Wash hands thoroughly. Clean your work surface. Gather all supplies before beginning.
02
Wipe the vial rubber stopper with a fresh alcohol swab. Allow it to dry completely before inserting a needle.
03
Draw the calculated dose volume into a sterile insulin syringe. Invert the syringe and tap to remove air bubbles; expel them before withdrawing the needle from the vial.
04
Select an injection site: abdomen (at least 2 inches from the navel), outer thigh, or upper outer arm. Clean with a fresh alcohol swab and allow to dry.
05
Pinch a fold of skin between thumb and forefinger. Insert the needle at a 45–90° angle depending on body fat thickness -45° for leaner individuals, 90° for more subcutaneous tissue.
06
Do not aspirate. Current clinical guidelines do not recommend aspiration for subcutaneous injections. Inject slowly and steadily over 2–3 seconds.
07
Wait 3–5 seconds after the plunger bottoms out before withdrawing the needle at the same angle. Apply gentle pressure with a clean swab -do not rub vigorously.
08
Rotate injection sites systematically with every dose. Reusing the same site repeatedly causes lipohypertrophy (hardened fat tissue) which reduces absorption consistency.
09
Dispose of used needles and syringes immediately in a puncture-resistant sharps container. Never recap needles by hand.
Important Notes
⚠
Research use only. AICAR is not FDA-approved for human use. Human clinical data may be limited. Do not use without consulting a qualified healthcare professional.
◎
One syringe per injection. Never reuse needles or syringes. Each injection requires a fresh, sterile syringe to prevent contamination and infection risk.
⚠
WADA prohibited substance -banned in competitive athletics
◎
Document your protocol. Record daily dose, injection site, and any observations. This supports consistency and allows you to identify patterns or issues over the course of the cycle.
◎
Inspect before each use. The reconstituted solution should be clear and colorless. Discard if cloudy, discolored, or if particulates are visible.
References
All dosing recommendations and mechanism descriptions on this page are derived from the following peer-reviewed publications and regulatory documents.
2
PubMed 9435525
Merrill GF et al. AICA riboside increases AMP-activated protein kinase, fatty acid oxidation, and glucose uptake in rat muscle
pubmed.ncbi.nlm.nih.gov/9435525 ↗
