GrowthMetabolic

AICAR

Nucleotide analogue · AMPK activator · Synthetic

FDA · PRECLINICAL ONLYWADA PROHIBITED

Half-life

~2.5 hours

Short

minsdays

Route

SubQ injection

Evidence

Preclinical only

Risk

Moderate

Overview

Known for

AMPK activator. Mimics exercise at the cellular level by activating AMP-activated protein kinase. Improves endurance, glucose uptake, and fat oxidation. Originally studied for cardiac ischemia protection. Banned in competitive sports.

Mechanism

AMPK activator — "exercise in a pill." Mimics metabolic effects of exercise: fat oxidation, glucose uptake, mitochondrial biogenesis. Also purine synthesis intermediate.

Key facts

Format
Lyophilized powder
Mechanism targets
Classification
Secondary
Supply & nature
Natural / Topping UpNatural
FDA category
Preclinical only

Evidence & standing

Evidence base
Preclinical only
Risk level
Moderate
Best studies
6 references
  • Narkar et al. (2008) Cell 134:405-15 — 'Exercise pill' paper
  • Merrill et al. (1997) J Biol Chem 272:32530-6 — AMPK activation
  • Extensive preclinical literature on AMPK pathway
  • NOT FDA APPROVED
  • WADA prohibited substance
  • No large-scale human clinical trials for performance/aging

Dosage & protocol

Typical dose
150-500mg/day
Research range
25–50 mg
Cycle
2 weeks on / 4 weeks off
Onset
2 days first effects
Full effect
21 days
Half-life
~2-3h
~2-3 hours
Protocol

150-500mg/day SubQ or IV. Often cycled: MAXIMUM 14 days on, 4 weeks off. Some use 50mg daily.

Time to effects

EARLY: 1-3 days

FULL: 2-4 weeks

Day 1-3: Improved exercise endurance — this is one of the faster-acting metabolic peptides. AMPK activation is rapid.

Week 1-2: Significant endurance improvements. Enhanced fat oxidation during exercise. Glucose uptake improved.

Week 2-4: Peak metabolic benefits. Exercise capacity substantially enhanced.

Cycle 4-6 weeks max. Effects are noticeable quickly but compound is expensive and cycles are short. Minimum commitment: 2 weeks.

Recommended vial
  • 50mg (only size)

At 50mg/day = 1 vial per day. Used immediately. No shelf life concern. Expensive at effective doses.

Reference figures only

Dosing reflects published laboratory protocols and is not guidance for use in any living subject.

Safety

Reversibility
Fully Reversible
WADA status
WADA – Prohibited (class to verify)
Side effects

Lactic acidosis (dose-dependent — serious at high doses), hypoglycaemia, GI discomfort, potential cardiac effects at high doses

Interactions

Metformin (additive AMPK — risk of excessive metabolic activation), insulin/anti-diabetics (↑hypoglycaemia risk)

Handle with research caution

  • Caution with diabetes medications (AICAR improves glucose uptake — combined with metformin/insulin = hypoglycaemia risk)

Storage & handling

Lyophilised
12–24 months
2–8°C
Reconstituted
4–6 weeks
2–8°C

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