Onset
Not established for any non-hospital use.
Protocol / Research Dosing Guide
AICAR Dosage Guide: Human Trial History, Animal Research and Safety
An evidence-organized AICAR (acadesine) guide that separates the compound's discontinued human drug program from the animal exercise research that drives most online claims.
Last reviewed September 16, 202616 minute readResearch information only
Level 2 — Fitness claims are animal-onlyExercise claims are animal-onlyProhibited in sport (WADA)
AICAR Quick Start
AICAR (acadesine, 5-aminoimidazole-4-carboxamide ribonucleotide) is a small-molecule AMPK activator, not a peptide. The only AICAR dosing ever recorded in humans is the intravenous acadesine infusion used in cardiac-surgery trials — a program whose definitive Phase 3 trial (RED-CABG) failed its endpoint and was stopped for futility. Its modern endurance reputation traces to a single 2008 mouse study that dosed sedentary mice at roughly 500 mg/kg/day, a figure that does not scale to humans by bodyweight. The World Anti-Doping Agency prohibits AICAR at all times.
Why researchers care
Metabolic, endurance and cellular-energy research
Class
AMPK-activating small molecule (acadesine), not a peptide
Route reported
Human trials used intravenous infusion; vials sold online are research products
Cycle length
Not established for any fitness or wellness use
Regulatory status
Not FDA approved; prohibited at all times under WADA anti-doping rules
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AICAR Dosing Protocol and Schedule
No validated human protocol exists. Human data come from acute intravenous acadesine infusions during cardiac surgery (about 0.1 mg/kg/min), animal data from high-dose mouse studies, and everything else from unverified community anecdote. None of these can be converted into a personal schedule. Every field without direct evidence is marked not established.
| Phase or study | Amount | Frequency / evidence |
|---|---|---|
| Human surgical trials | IV infusion of about 0.1 mg/kg/min during cardiac surgery | Physician-administered hospital context only; failed Phase 3 endpoint |
| Mouse endurance study | Roughly 500 mg/kg/day subcutaneous for about 4 weeks | Sedentary mice only; mg/kg does not scale to humans |
| Research-vial schedule | Not established | No human study of vial-format use exists |
| Cycle or rest interval | Not established | No validated protocol defines one |
Intravenous hospital trial data and milligram-per-kilogram mouse doses cannot be converted into a personal dosing schedule. No validated amount, frequency, cycle, or rest period exists for research-vial AICAR.
AICAR Supplies Needed
Neutral research-material planning only. This does not establish an appropriate amount or route.
Research planning item
Exact labeled research vial
Research planning item
Measured diluent volume
Research planning item
U-100 measurement reference
Research planning item
Alcohol swabs
Research planning item
Appropriate sharps container
Research planning item
Written concentration label
AICAR Reconstitution Calculator
Vial-format concentration math
Concentration
20 mg/mL
Draw volume
0.125 mL
U-100 units
12.5
Mathematical draws
20
Arithmetic only. The entered amount is not a recommendation and does not establish suitability.
Best Time to Take AICAR: Morning or Night?
Morning or evening?
Not established. No human study addresses timing.
Daily or intermittent?
Not established.
With food?
Not applicable to a vial format and not established for any format.
Missed amount?
No validated replacement or doubling procedure exists.
AICAR Route Comparison
| Route | What is reported | Evidence limit |
|---|---|---|
| Intravenous | Human cardiac-surgery trials used IV infusion | Hospital drug-program context only |
| Subcutaneous vial | Route used in rodent studies and described in community anecdote | No human safety or pharmacokinetic study |
| Oral | Poor bioavailability; not a documented delivery method | No exposure data |
| Route conversion | None available | Routes are not interchangeable |
Routes and amounts are not interchangeable unless a verified study explicitly establishes a conversion.
AICAR Half-Life and Dosing Frequency
| Measure | Finding | Evidence limit |
|---|---|---|
| Human half-life (IV) | Reported in drug-program pharmacokinetics | IV data cannot define vial-format behavior |
| Research-vial half-life | Not established | No study of marketed vial format |
| Active metabolite (ZMP) | Cellular accumulation described in lab research | Laboratory context only |
| Frequency | Not established | No studied regimen for vial use |
AICAR Dosage Chart
| Route | Amount | Frequency | Source | Human validation |
|---|---|---|---|---|
| Intravenous (trials) | ~0.1 mg/kg/min infusion | — | Acadesine cardiac-surgery program; failed Phase 3 | No |
| Mouse (Narkar 2008) | ~500 mg/kg/day | — | Sedentary mice ~4 weeks; not scalable to humans | No |
| Community-reported vial use | ~5–10 mg self-reported SubQ | — | Unverified anecdote only; WADA-prohibited | No |
Published study values describe those studies. Community-reported values are not validated dosing recommendations.
AICAR Reconstitution Guide
Concentration: 20 mg/mL
| Entered amount | Volume | U-100 units |
|---|---|---|
| 2.5 mg | 0.125 mL | 12.5 units |
| 5 mg | 0.25 mL | 25 units |
| 7.5 mg | 0.375 mL | 37.5 units |
- 1.Confirm the exact vial label and total quantity.
- 2.Record the measured diluent volume.
- 3.Clean the vial stopper.
- 4.Add liquid slowly along the vial wall.
- 5.Swirl gently; do not shake.
- 6.Inspect for cloudiness, discoloration, or particles.
- 7.Label the calculated concentration and preparation date.
- 8.Use the result only for arithmetic, not as a recommendation.
Reconstitution does not establish identity, purity, sterility, stability, or an appropriate amount.
How AICAR Works
AMPK activation
AICAR converts to ZMP inside cells, which activates AMPK — an enzyme that regulates cellular energy balance.
AICAR Human Trials and FDA Status
Current status · verified September 16, 2026
Not FDA approved; prohibited at all times under WADA anti-doping rules
- Human: an early meta-analysis of five acadesine trials in roughly 4,000 bypass-surgery patients suggested a cardioprotective signal (Mangano 1997).
- Human: the definitive Phase 3 RED-CABG trial infused acadesine at about 0.1 mg/kg/min in roughly 3,000 patients and found no benefit (5.1% vs 5.0% event rates); it was stopped for futility (Newman 2012).
- Animal: the 2008 Narkar et al. mouse study (~500 mg/kg/day) reported sedentary mice ran about 44% farther — the origin of the 'exercise in a pill' headline.
- No controlled human study has tested AICAR for endurance, fat loss, or performance at any dose.
- WADA prohibits AICAR at all times as a metabolic modulator, in and out of competition.
Who Should Avoid AICAR?
This is an evidence-gap and precaution list, not an approved prescribing label.
Competitive athletes
Prohibited at all times under WADA rules; detectable in anti-doping tests
Pregnancy or breastfeeding
No safety data
Children or adolescents
No safety data
Gout or high uric acid
AICAR metabolizes to uric acid; trials documented rises in uric acid
Blood-sugar medication
AMPK activation may interact with glucose control; no interaction studies
Cancer history
AMPK-pathway effects on tumor metabolism are unresolved
Long-term or repeated use
No safety data
AICAR Side Effects, Risks and Safety
Elevated uric acid (hyperuricemia)Documented in human IV trials; AICAR metabolizes to uric acid
Important limitation: Asymptomatic rises; relevant for gout-prone individuals.
Transient kidney effectsReversible creatinine increases reported in trials
Important limitation: Hospital infusion context.
Low blood pressureInfusion-related in surgical trials
Important limitation: Tied to IV route.
AMPK and cancer (unsettled)Most literature is anti-proliferative, but AMPK activation can be context-dependently pro-survival for established tumors
Important limitation: Open research question, not an established human risk or benefit.
Low blood sugarPlausible from mechanism
Important limitation: No controlled incidence data in vial users.
Long-term effectsUnknown — chronic use in healthy people has never been studied
Important limitation: No follow-up evidence.
AICAR Timeline and Monitoring
Peak effect
Not established.
Cycle length
Not established.
Monitoring
No validated monitoring schedule or stopping rule exists.
AICAR Benefits and Results: What the Evidence Shows
| Claim | Evidence level | What research shows | Important limitation |
|---|---|---|---|
| Endurance without training | Not established in humans | Mouse study only (2008) | No human trial |
| Fat loss or metabolic boost | Not established | Animal and cell research | No human trial |
| Heart protection in surgery | Studied, not approved | Human IV drug program | Program discontinued |
AICAR Storage and Handling
Unreconstituted vial
No AICAR-specific consumer stability study was identified; follow the exact product label.
Prepared vial
No validated AICAR storage duration after preparation was identified.
Hospital formulation
IV trial formulations were pharmacy-prepared; conditions do not transfer to research vials.
Appearance
Cloudiness, discoloration, or particles do not establish safe usability.
AICAR Troubleshooting
Solution appears cloudy
Stop and seek qualified product guidance; appearance cannot confirm sterility.
Calculated units look wrong
Recheck vial quantity, diluent volume, target unit, and U-100 conversion.
Conflicting amounts online
No studied human vial amount exists; community figures are not validated.
Unexpected symptoms occur
No AICAR safety protocol exists for vial use; seek licensed clinical review.
A scheduled amount is missed
No validated missed-amount procedure exists.
AICAR Comparisons
| Compound | Class or mechanism | Evidence | FDA status |
|---|---|---|---|
| AICAR | AMPK-activating small molecule (acadesine) | Human IV trials (discontinued); animal endurance research | Not approved; WADA-prohibited |
| 5-Amino-1MQ | NNMT-inhibiting small molecule | Animal and cell research only | Not approved |
| MOTS-c | Mitochondrial-derived peptide | Early human and animal research | Not approved |
AICAR Frequently Asked Questions
What is AICAR?
Acadesine, a small-molecule AMPK activator. It is not a peptide, despite being sold alongside peptides.
Has AICAR been studied in humans?
Yes — intravenous trials in cardiac-surgery patients in the 1990s. The program did not lead to approval.
Does AICAR really replace exercise?
That claim comes from a single 2008 mouse study. It has never been shown in humans.
Is AICAR legal in sport?
No. WADA prohibits it at all times, in and out of competition.
What is the correct human dose from a vial?
Not established — no human study of vial-format use exists.
What is its half-life?
IV pharmacokinetics from the drug program do not define research-vial behavior; a vial-format half-life is not established.
Is AICAR FDA approved?
No.
Is a cycle or rest period established?
No.
What does the calculator do?
It converts entered vial and liquid values into concentration and volume math only.
Sources and Research
Animal study
1. Narkar et al., 2008 — AMPK and PPARδ agonists are exercise mimetics (Cell)
Mouse study behind most endurance claims; animal evidence only.
Open direct sourceHuman trial
2. Newman et al., 2012 — RED-CABG Phase 3 acadesine trial (JAMA)
Definitive human trial in ~3,000 cardiac-surgery patients; no benefit, stopped for futility.
Open direct sourceHuman trial meta-analysis
3. Mangano, 1997 — Acadesine meta-analysis in coronary bypass surgery
Early meta-analysis of five trials in ~4,000 patients suggesting a cardioprotective signal later refuted by RED-CABG.
Open direct sourceRegulatory
4. WADA Prohibited List
AICAR is listed as a prohibited metabolic modulator at all times.
Open direct sourceVendor listing
5. AICAR 50mg product listing
Vendor listing confirming vial size and price; not evidence of effect.
Open direct sourceMissing information flagged for review
- Human trial of research-vial use: Not established
- Human dose, route, and frequency for any non-hospital purpose: Not established
- Vial-format half-life and pharmacokinetics: Not established
- Validated cycle and rest period: Not established
- Compound-specific stability data: Not established
- Long-term safety: Not established
- Drug interactions: Not established
- Human endurance or fat-loss evidence: Not established