Has it actually been given to humans?

Yes, more than almost anything else on this site — about fifteen hundred patients received it intravenously in a phase 3 trial under the name acadesine. It was stopped early because it made no difference to the outcome it was being tested for. That tells you it is reasonably tolerated for a few hours by infusion. It tells you nothing about taking it daily for months.

Is it really exercise in a pill?

It reproduced part of the metabolic signature of endurance training in mice. It did not reproduce the cardiovascular, skeletal or neurological adaptations of exercising, and it has never been measured for endurance in a person. It is also barely absorbed orally, so "pill" is doing a lot of work in that phrase.

Will it show up on a drug test?

AMPK activators are prohibited at all times under the WADA list and AICAR is named specifically. Because the body makes a small amount naturally, detection works on the ratio to a reference rather than presence alone — but methods are published and in use.

Muscle & performanceWeight loss

AICAR

Acadesine · AICA riboside · 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside · AICA-riboside

Early human trialsReviewed 1 Sept 2026

AICAR sits oddly in a peptide catalogue because it is not a peptide and not a protein. It is a nucleoside — a sugar attached to a base — closely related to an intermediate the body already makes while building purines.

Its reputation comes from one mouse experiment. In 2008 a group reported that sedentary mice given AICAR ran substantially further than untreated ones, without training. The phrase "exercise in a pill" comes from the coverage of that result, and the World Anti-Doping Agency added AMPK activators to the prohibited list the following year.

What is unusual, and worth knowing before buying it, is that AICAR has a real human trial history under another name. As acadesine it was developed as a cardioprotective agent, and the RED-CABG trial gave it intravenously to about fifteen hundred patients undergoing bypass surgery. It was stopped early for futility: the primary outcome occurred in 5.1 per cent of the acadesine group and 5.0 per cent of the placebo group.

So the position is unusually well defined. This compound has been given to a large number of people under proper supervision and was reasonably well tolerated — and it has never once been tested in a human for endurance, fat loss, or anything an athlete would buy it for.

How it works

AICAR is taken into cells and phosphorylated to ZMP, which resembles AMP closely enough to be mistaken for it.

AMP-activated protein kinase is the cell's low-energy sensor: when AMP rises, AMPK reads it as fuel running short and switches the cell from storing energy to spending it — more glucose uptake, more fatty acid oxidation, more mitochondrial biogenesis, less synthesis of fat and cholesterol.

ZMP activates AMPK without the cell ever actually being short of energy. That is the trick, and it is also the objection: the signal is a forgery, and the cell responds to it everywhere rather than only in exercising muscle.

The effects are not confined to the tissue anybody is aiming at. AMPK activation in the wrong place, or too much of it, has been linked to problems with cell division and to neurodegeneration in experimental work, and naturally accumulating AICAR is itself associated with metabolic disorder in humans.

Oral bioavailability is poor. The human trials gave it by continuous intravenous infusion, which is not how anybody is taking material bought as a powder.

Vocabulary on this page

Bioavailability: How much of an administered dose actually reaches the bloodstream. Injection is close to complete; swallowing a peptide is usually close to nothing.
Concentration: How much peptide there is in each millilitre of solution, once the vial has been reconstituted.
Batch number: An identifier for one production run. It is what makes a certificate of analysis mean anything about the vial in your hand.
Evidence level: The category of human evidence behind a compound, from preclinical through to approved. Stated on every profile here as a category, not an adjective.
Peptide: A short chain of amino acids: the same building blocks as a protein, in a chain short enough to behave differently.
Protocol: One compound, with a dose, a frequency and a length: the plan, as opposed to what was actually taken.

The whole glossary →

Quick reference

Commonly described dose: 50 mg–100 mg
How often: Daily
Route: Subcutaneous or Oral
Where: Abdomen
Timing: No basis for a timing recommendation.
Storage once mixed: Refrigerated, 30 days

These describe what sources report, not what you should do. Full detail and provenance in the dosing section below.

Price index

$0.472 – $1.44per mg

Across 5 vendors, normalised per milligram and confirmed by a person.

Confirmed listings for this compound, cheapest per milligram first.
Vendor	Size	Price	Per mg
Peptide Prosout of stock	50 mg × 100 vial	$2,362.50	$0.472
Peptide Prosout of stock	50 mg × 50 vial	$1,653.75	$0.662
Direct Peptides	50 mg	£36.06	$0.721
Peptide Pros	50 mg	$47.25	$0.945
Modern Aminos	50 mg	$54.00	$1.08

Show 3 more vendors

The remaining listings, continuing from cheapest.
Biotech Peptidesout of stock	50 mg	$56.00	$1.12
Core Peptidesout of stock	50 mg	$62.00	$1.24
BulkGLP	50 mg	$72.00	$1.44

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Ranked on price alone. We sell nothing, take no payment for placement, and use no affiliate links — listing a price is not a recommendation to buy. Prices are what the vendor listed when we last looked, not a live quote.

What it is studied for

Each entry states the evidence behind it. We do not rank indications by effectiveness — for most compounds here, that would be a claim nobody can support.

Endurance

Published review

The claim, and where it comes from.

EvidenceSedentary mice given AICAR ran further than untreated mice. No human has been tested for endurance on AICAR in any published trial.

Cardioprotection in bypass surgery

Clinical trial

The only indication it was seriously trialled for.

EvidencePhase 3, roughly 3,000 patients randomised, stopped early for futility. Death, stroke or need for mechanical cardiac support occurred in 5.1 per cent on acadesine against 5.0 per cent on placebo.

Regulatory status — United States

Not approved for any indication. Developed as acadesine and abandoned after a phase 3 trial was stopped for futility. Prohibited in sport at all times by WADA as an AMPK activator, and detectable. Material sold as a research chemical is not the clinical infusion product.

Last reviewed 1 Sept 2026. Regulatory positions in this category change frequently; we date this line so you can see how current it is.

Identity and clearance

Molecule

Class: Nucleoside analogue, not a peptide
Molecular weight: 258.23 Da

Converted inside the cell to ZMP, the AMP mimic that does the actual work. It is the metabolite, not AICAR itself, that activates AMPK.

Dose protocols reported in sources

Displayed for reference only. Every row says where it came from, and a trial protocol and a community convention are not the same kind of information. None of this is fed into the calculator, and none of it is a recommendation.

Dose protocols reported in sources, with the source of each.
Goal	Dose	Frequency	Route	Units, 50 mg vial	Source	Start this protocol
Commonly described community protocol	50 mg – 100 mg	Daily	SubcutaneousNo published human study supports any dose for this purpose. The human trials infused it intravenously and continuously; the doses circulating in community sources are scaled from rodent work by guesswork.	from 100 u	Community practice	Start this

Start this copies a row into a protocol of your own, which you can then edit. Where a source gave a dose range or an ambiguous frequency, those fields arrive empty — we will not pick a number on your behalf.

CheckRows marked community practice describe what people commonly do, drawn from public discussion. They are not derived from any trial and are not evidence that a dose is safe or effective.

Safety

Reported effects

Broadly tolerated by infusion in the surgical trialsClinical trial
Large exposure, short duration
Roughly fifteen hundred patients received it intravenously over hours without a safety signal that stopped the trial. It was stopped because it did not work, not because it hurt anybody.
Effects of chronic AMPK activationPublished review
Unknown, and the specific concern
The trial exposure was hours. Nobody has taken this daily for months under observation. Sustained AMPK activation in tissues that are not exercising is uncharacterised, and experimental work links excessive or misplaced activation to impaired cell division and to neurodegeneration.
Raised uric acidClinical trial
Reported in early studies
AICAR sits on the purine pathway, and purine metabolism ends in uric acid. Relevant to anyone with gout.

When to stop

Joint pain or swelling suggesting gout.
Persistent unexplained fatigue or muscle weakness.
Any allergic response: rash, hives, facial swelling or difficulty breathing. Seek urgent care.

Interactions and situations that need care

Gout or raised uric acidAvoid
It is a purine-pathway compound and uric acid is where that pathway ends.
Competing in a tested sportAvoid
AMPK activators are prohibited at all times by WADA and AICAR is specifically named. Detection methods exist. This is a sanction, not a health warning.
Pregnancy and breastfeedingAvoid
No reproductive or developmental data, for a compound that reprograms cellular energy metabolism.
Any history of cancerUse caution
AMPK's relationship with tumour biology runs both ways depending on context and tissue, and chronic pharmacological activation has not been studied in people.

What to expect

The human evidence is a failed phase 3 in heart surgery, not a study of anything it is sold for.
No human has been tested for endurance or fat loss on AICAR in any published trial.
"Exercise in a pill" describes a mouse result from 2008.
It is a nucleoside, not a peptide — doses are in the tens of milligrams to grams, not micrograms.
Oral absorption is poor and the clinical work used intravenous infusion.
It is prohibited in sport at all times and detectable.

Storage and handling

Freeze-dried powder: Refrigerated, protected from light.
After mixing: Refrigerated. A small molecule rather than a peptide, so the usual peptide stability rules do not transfer.
Long-term, frozen: Stable frozen as a dry powder.

Printable one-pager How to reconstitute a vial, step by step

Checking your vial

Research chemicals carry no manufacturing standard, so what the vial looks like is often the only quality signal available before you use it. More on assessing quality and COAs.

No certificate of analysis
Identity and purity are the only things that separate this from any other white powder, and neither is visible.
Sold in gram quantities
The doses discussed are tens of milligrams to grams rather than the microgram-to-milligram range most of this site covers. A dosing habit carried over from peptides will be wrong by orders of magnitude in both directions.

Questions

Has it actually been given to humans?: Yes, more than almost anything else on this site — about fifteen hundred patients received it intravenously in a phase 3 trial under the name acadesine. It was stopped early because it made no difference to the outcome it was being tested for. That tells you it is reasonably tolerated for a few hours by infusion. It tells you nothing about taking it daily for months.
Is it really exercise in a pill?: It reproduced part of the metabolic signature of endurance training in mice. It did not reproduce the cardiovascular, skeletal or neurological adaptations of exercising, and it has never been measured for endurance in a person. It is also barely absorbed orally, so "pill" is doing a lot of work in that phrase.
Will it show up on a drug test?: AMPK activators are prohibited at all times under the WADA list and AICAR is named specifically. Because the body makes a small amount naturally, detection works on the ratio to a reference rather than presence alone — but methods are published and in use.

References

Effect of the adenosine-regulating agent acadesine on morbidity and mortality associated with coronary artery bypass grafting: the RED-CABG randomized controlled trial
JAMA, 2012 · Randomised, double-blind, placebo-controlled phase 3
Intermediate- to high-risk adults undergoing non-emergency on-pump coronary artery bypass grafting, at 300 sites · n = 3080 · 0.1 mg/kg per minute intravenously for 7 hours · Through postoperative day 28
Stopped early for futility after 3,080 of a planned 7,500 participants. The composite of death, non-fatal stroke or need for mechanical support for severe left ventricular dysfunction occurred in 5.1 per cent on acadesine and 5.0 per cent on placebo, odds ratio 1.01. No differences in key secondary endpoints.
10.1001/jama.2012.7633
AMPK and PPAR-delta agonists are exercise mimetics
Cell, 2008 · Animal study
Sedentary mice
AICAR increased running endurance in untrained mice and induced a transcriptional programme resembling endurance training. This is the origin of the "exercise in a pill" description and of the WADA prohibition that followed in 2009. No human endurance study has been published.
Clinic and community practice, unverified
Research-chemical vendor listings and forums, 2026 · Not a study
Not applicable
Doses circulating in community sources have no published basis for this use. They are reproduced here because people are using them, not because anything supports them.

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Retatrutide

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Keep this page honest

If something here is wrong, out of date, or missing a source, tell us and we will fix it and say that we did.

Suggest a correction

This page is educational. It describes what published research reports, not what you should do. Peptides discussed here are largely not approved for human use, and nothing on Bioalmanac is medical advice. No clinician reviews these pages.

Page last updated 1 Sept 2026