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Mitochondria

AICAR

An AMPK activator and exercise-mimetic candidate from research, with impressive animal data but unclear use in humans.

2 min read 9 sources

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AICAR vial with white powder and the black TPD label on a white round podium, next to a blue and white 3D molecule model with a ring structure in a bright lab
As an infusion up to phase 3, without benefit · not approved

Summary

At a glance

Sources checked on 26 Oct 2026

Running endurance (mice)
+44 %

untrained mice after four weeks of AICAR, injected into the abdominal cavity1

Half-life (humans)
1.4 hours

after an infusion in healthy men, levels fell quickly in two phases2

Sugar uptake into muscle
2.1 -fold

healthy men, AICAR as an infusion, cycling reached 4.7-fold3

Phase 3 without benefit
3,080 participants

bypass surgery, infusion, stopped after an interim analysis4

  • AICAR, known as the drug acadesine, activates the enzyme AMPK, the energy sensor of the cell. It became known as an exercise mimetic candidate.89
  • Untrained mice ran 44 percent longer after four weeks of AICAR without training. The animals received high doses, injected into the abdominal cavity.1
  • In humans AICAR was given as an infusion: in healthy men the half-life was 1.4 hours and sugar uptake into muscle rose 2.1-fold.23
  • A phase 3 trial with 3,080 participants in bypass surgery was stopped without benefit. In leukaemia studies very high infusions strained the kidneys.45
  • There is no study of AICAR under the skin for performance or metabolism. Everything here is research, not a recommendation.7
Profile

Updated May 2026

Class
AMPK activator

exercise mimetic

Use
Subcutaneous

in mg

Half-life
short
Status
Tested as an infusion

acadesine, up to phase 3, no benefit, not approved

Sizes
50 to 100 mg

2 sizes in the shop

Contents 15 sections
  1. At a glance
  2. What is AICAR?
  3. How it works
  4. What you need
  5. Reconstitution
  6. Dosing
  7. Injection
  8. What the research shows
  9. Research status
  10. Side effects
  11. Storage
  12. Related compounds
  13. FAQ
  14. Glossary
  15. Sources

What is AICAR?

AICAR is a small molecule that activates the enzyme AMPK, the cell's central energy sensor. It is seen as an exercise-mimetic candidate: part of the metabolic signals otherwise produced by endurance training is meant to be triggered without training.

Up front: the spectacular effects come from animal models, there is no established, sensible human dose.

Comparison

Exercise mimetic candidates compared

Compounds from the TPD lexicon meant to mimic training signals, as described there. Tap a card to open its entry.

AMPK activator for injection AICAR AMPK
AMPK activator as a tablet AICAR Oral AMPK PPAR delta agonist Cardarine (GW-501516) PPAR-delta ERR agonist SLU-PP-332 ERR

Simplified: AICAR acts on AMPK, cardarine on the PPAR delta receptor. Both routes were tested in the 2008 mouse study. There is no comparison in humans. 1

How it works

By activating AMPK, AICAR switches on programs tied to energy expenditure, fat burning and endurance. In mice AICAR markedly increased running endurance even without training (Narkar, 2008). But the effect in humans at reasonable doses is unclear.

Where it acts

Where AICAR acted in studies

Tap a point or a card. Colour = AMPK, grey = observed. Only tested in humans as an infusion.

  1. Skeletal muscle

    More endurance in mice, more sugar uptake into muscle of healthy men (infusion)3

    AMPK
  2. Blood

    Rapid uptake into red blood cells and conversion to the monophosphate, half-life 1.4 hours2

    Observed in trials
  3. Heart

    No protection against complications in bypass surgery (phase 3)4

    Observed in trials
  4. Kidney

    Kidney problems with very high infusions in leukaemia studies5

    Observed in trials

Targets in the ChEMBL database8

Compound CHEMBL1551724 (Acadesin): one recorded mechanism, Activator according to ChEMBL.

AMP-activated protein kinase
Gene
PRKAA1, PRKAA2
UniProt
Q13131, P54646
ChEMBL
CHEMBL2096907
Action
Activator according to ChEMBL
Transparent glass muscle fibres with glowing orange mitochondria, a glass sensor shape in the middle lights up as small blue ring molecules dock onto it
AMPK as the energy sensor in muscle. Symbolic image.

What you need

Supplies

2 things, numbered as in the picture

Tick off what you already have. Vial and BAC water are our real shop photos at the same size.

AICAR vial and bacteriostatic water at the same size with the black TPD label, next to two U-100 insulin syringes, two alcohol swabs and a sharps container with a blue lid

  1. AICAR vial

    The AICAR vial (lyophilized powder).

    In the shop

  2. Water and supplies

    Bacteriostatic water, U-100 insulin syringes, alcohol swabs.

    In the shop

Reconstitution

Use the peptide calculator. A 50mg vial with 2ml water gives 25mg per ml. Just add the water to the vial and let it dissolve.

Step by step

Dissolving the powder

Four steps, the same for every vial size.

  1. 1Wipe the cap

    Clean the rubber stopper with an alcohol swab.

  2. 2Add BAC water

    Just add it, it does not matter if it hits the powder directly.

  3. 3Swirl or shake

    Until everything has dissolved, both are fine.

  4. 4Draw up

    With the U-100 insulin syringe.

Less water higher concentration fewer units on the syringe Example: 50 mg + 2 ml = 25 mg/ml

Dosing

Dosing

Dosing, titration and syringe

Loading the dosing information …

  • Getting started and stepping up, drawn as a staircase
  • Units on the U-100 syringe for every step
  • How long one vial lasts

Injection

The injection is subcutaneous, into the fat layer under the skin. Common spots are the abdomen (keep about two finger-widths clear of the navel), the front and the inner side of the thigh, or the back of the upper arm.

The short version:

Injection

Where and at what angle

Pick a spot or switch the angle. Subcutaneous means: into the fat layer, not the muscle.

Rotate the spot each time, never the same one twice in a row.

90°More fat under the skin

Rule of thumb: where there is more fat under the skin, insert straight at 90 degrees. In lean people with little fat, 45 degrees, so the needle stays in the fat layer. Simplified diagram.

  1. Clean the spot with an alcohol swab and let it dry

  2. Pinch up a small fold of skin

  3. Insert the needle: at 90 degrees where there is more fat under the skin, at 45 degrees in lean people with little fat

  4. Inject slowly, wait a moment, then withdraw

  5. Put the needle straight into the sharps container

Rotate the site each time so the tissue does not get irritated. Never the same spot twice in a row.

What the research shows

The well-known study (Narkar, 2008) showed in mice that AICAR alone, without training, raised running endurance by 44 percent after 4 weeks, a classic exercise-mimetic result. The combination with training was tested there with a different compound (a PPAR-delta agonist). That is impressive but animal research at high doses. AICAR is also on the WADA list.

In humans AICAR, under the name acadesine, went as an infusion into a phase 3 study in heart bypass surgery (RED-CABG, Newman 2012). It was stopped early after 3,080 patients because no benefit was expected. There is no approval.

Study results

What the trials measured

Interactive: switch tabs, tap points, show or hide arms. Arms are named relative to each other, no dosing advice.

Running endurance of untrained mice after four weeks1

Change compared with mice without AICAR, in percent

Treadmill running endurance1
Without AICAR (comparison) 0%
With AICAR 44%

Value from the abstract, daily dosing into the abdominal cavity according to the full text. The mice did not train, AICAR switched on metabolic genes in muscle. The animals received high doses. Mouse model, not tested in humans.

Sugar uptake into muscle of healthy men3

Rise after three hours compared with baseline, as a multiple

Uptake of labelled sugar3
Acadesine as infusion 2.1-fold
Cycling (comparison) 4.7-fold

Values from the abstract, 29 healthy men. AICAR was given as an infusion into a vein, not under the skin. Whole-body glucose disposal rose by only 7 percent and AMPK activity in muscle did not change measurably.

Death, stroke or severe heart failure up to day 284

Share of participants in percent, 1,493 per group

Primary endpoint4
Placebo 5.0%
Acadesine as infusion 5.1%

Values from the abstract. The trial was stopped after 3,080 of a planned 7,500 participants because an interim analysis made a benefit unlikely. The key secondary endpoints showed no difference either.

Glass block of muscle tissue with reddish fibres and many small glowing mitochondria against a light background
Endurance effect only shown in mice so far. Symbolic image.

Research status

Where the research stands

The registry lists five trials with AICAR or acadesine, all using the compound as an infusion or lab tool, none with injections under the skin. Shown are the three acadesine trials with a start and end date in the registry. As of 26 Oct 2026. 7

  1. Preclinical Cell assays and mouse models, exercise mimetic study 2008
  2. Phase 1 no registered trial
  3. Phase 2 2 trials, 1 completed, 1 stopped early
  4. Phase 3 1 trial, 0 completed, 1 stopped early
  5. Approval not yet
3,080 participants in phase 3 Not approved. As an infusion, development ended after phase 3 without benefit. AICAR has never been tested under the skin in a study.7
Show all 3 phase 2 and 3 trials on a timelineHide timeline 1 completed 0 running 2 stopped early 2 with results
Phase 2
Phase 3

Bar: start to primary endpoint (planned for running trials). Green = completed, blue = progress until 26 Oct 2026, grey = stopped early.

Side effects

  • Solid human data are largely missing.
  • Local reactions at the injection site.
  • Banned in official competition.

Storage

Before mixing the powder is robust, normal room temperature (around 20 to 25 degrees) is fine, ideally kept in the dark. After mixing, keep in the fridge (2 to 8 degrees), do not freeze. It stays good there for at least 4 to 6 months with barely any loss of potency, in practice considerably longer. Swirl or shake to mix, both are fine.

Shelf life

How long it keeps

Undissolved (powder) Room temperature, around 20 to 25 degrees, dark

Robust, no fridge needed. Best kept in the dark.

Dissolved (mixed) Fridge, 2 to 8 degrees, do not freeze

At least 4 to 6 months with barely any loss of potency. The bacteriostatic water brings a preservative.

  • Keep it dark
  • Dissolved: 2 to 8 degrees
  • Note the mixing date on the vial
Nine vials with white powder and blue caps in the door shelf of a bright fridge
Powder dark at room temperature, once dissolved into the fridge (2 to 8 degrees), stable there for at least 4 to 6 months. Symbolic image.

Related

Related compounds

Blends with AICAR or a different path: all in the TPD lexicon.

AICAR
AICAR Oral The same compound as a tablet Cardarine (GW-501516) PPAR delta agonist, tested in the same mouse study SLU-PP-332 ERR agonist, also an exercise mimetic candidate MOTS-c Peptide from the mitochondria, a different metabolic approach SR9009 (Stenabolic) Rev-erb agonist, a different route Metformin (Glucophage) Biguanide, a different metabolic approach

FAQ

Common questions about AICAR

Short answers, each backed by the sources below.

Where does the exercise mimetic reputation come from?

From a 2008 mouse study: untrained mice ran 44 percent longer after four weeks of AICAR and their muscles switched on metabolic genes. The animals received high doses injected daily into the abdominal cavity. AICAR did not need training for this, the combination with training was tested there with the PPAR delta agonist.1

Has AICAR been tested in humans?

Yes, as an infusion under the name acadesine. A phase 3 trial in bypass surgery was stopped after 3,080 participants: death, stroke or severe heart failure occurred in 5.1 percent, as often as with placebo at 5.0 percent. There were also small studies in blood cancer. There is no study with injections under the skin.457

What happens in human muscle?

In 29 healthy men an AICAR infusion raised sugar uptake into muscle 2.1-fold after three hours, cycling reached 4.7-fold. Whole-body glucose disposal rose by only 7 percent and AMPK activity in muscle did not change measurably.3

How long does AICAR stay in the blood?

Not long. After an infusion levels in healthy men fell quickly in two phases, with a half-life of 1.4 hours. Red blood cells took up AICAR rapidly and converted it to the monophosphate. Only 8 percent was excreted unchanged by the kidneys.2

Which side effects are known?

Healthy men tolerated AICAR well in the early study, with mild and short-lived complaints. With very high infusions in a leukaemia study raised uric acid, temporary blood count changes, kidney problems and drops in blood pressure occurred. Another trial was stopped because of kidney problems. There are no data on dosing under the skin.257

Is AICAR allowed in sport?

No. AICAR is on the WADA prohibited list. Because it also occurs naturally in the body, doping labs tell the body's own AICAR from added AICAR by the make-up of the carbon isotopes.6

Glossary

Terms explained briefly

Dotted words in the text open these explanations directly.

Acadesine
The drug name of AICAR. Clinical development as an infusion ran under this name.
AMPK
The energy sensor of the cell. When energy runs short, AMPK switches the cell to burning sugar and fat.
Bypass surgery
Heart surgery in which narrowed coronary arteries are bridged with a piece of vessel.
Exercise mimetic
A substance meant to trigger part of the signals of training without any training.
Half-life
The time until the amount in the blood has fallen by half.
Infusion
Giving a solution directly into a vein over a longer time.
Interim analysis
A planned look at the data before a trial is finished. If it shows no prospect of benefit, the trial is stopped.
Lyophilisate
Freeze-dried powder. Without water a compound keeps much longer.
Subcutaneous
Into the fat layer just under the skin.
Uric acid
The end product of purine breakdown. If it rises sharply it can strain the kidneys and joints.
WADA
World Anti-Doping Agency. It keeps the list of substances banned in sport.

Evidence

Sources

Show all 9 sourcesHide sources 6 Studies1 Trial registry2 Database checked 26 Oct 2026

Studies

  1. AMPK and PPAR delta agonists as exercise mimetics (mice)

    Narkar et al., Cell, 2008

    DOI 10.1016/j.cell.2008.06.051 PMID 18674809
    Checked 26 Oct 2026 via doi.org, Crossref, PubMed, PMC (Volltext)
  2. Safety and pharmacokinetics in healthy men, infusion and oral

    Dixon et al., Journal of Clinical Pharmacology, 1991

    DOI 10.1002/j.1552-4604.1991.tb03715.x PMID 2037706
    Checked 26 Oct 2026 via doi.org, Crossref, PubMed
  3. AICAR infusion and muscle sugar uptake in healthy men

    Cuthbertson et al., Diabetes, 2007

    DOI 10.2337/db06-1716 PMID 17513706
    Checked 26 Oct 2026 via doi.org, Crossref, PubMed
  4. RED-CABG: acadesine in bypass surgery, phase 3

    Newman et al., JAMA, 2012

    DOI 10.1001/jama.2012.7633 PMID 22782417 NCT00872001
    Checked 26 Oct 2026 via doi.org, Crossref, PubMed
  5. Acadesine in chronic lymphocytic leukaemia, phase 1/2

    Van Den Neste et al., Cancer Chemotherapy and Pharmacology, 2013

    DOI 10.1007/s00280-012-2033-5 PMID 23228986
    Checked 26 Oct 2026 via doi.org, Crossref, PubMed
  6. Detecting added AICAR in doping control

    Buisson et al., Drug Testing and Analysis, 2017

    DOI 10.1002/dta.2322 PMID 29032594
    Checked 26 Oct 2026 via doi.org, Crossref, PubMed

Trial registry

  1. Trials with acadesine on ClinicalTrials.gov

    ClinicalTrials.gov, U.S. National Library of Medicine

    Checked 26 Oct 2026 via ClinicalTrials.gov API v2

Database

  1. Acadesine in ChEMBL (mechanism and highest phase)

    ChEMBL, EMBL-EBI (CHEMBL1551724)

    Checked 26 Oct 2026 via ChEMBL
  2. Structure of AICAR (acadesine) in PubChem

    PubChem, U.S. National Library of Medicine (CID 17513)

    Checked 26 Oct 2026 via PubChem

In the shop

AICAR in the catalog

Sizes, prices and shipping times are on the product page.

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