Cellular energy and oncology
Study
AICA riboside is metabolized to ZMP; energy-sensing experiments are not evidence for athletic use.1
MetabolicSmall molecule
AICAR / acadesine
Acadesine (AICA riboside); intracellular phosphorylation produces ZMP
Investigational acadesine; no FDA-approved weight-loss or exercise indication.
What does it do?
Molecular information
2Amino-acid sequence
Not applicable: this compound is not a single peptide.
LengthNonpeptide
Molecular weight · Da258.23 Da
Molecular formulaC9H14N4O52
This nucleoside is not its intracellular phosphorylated metabolite ZMP.
Pharmacokinetics
Unverified reference estimateNot independently confirmed
Reference half-life1.4 hours13
Route / formulationSource page: Injectable. Exact PK route not verified.
This value is reported by a secondary reference. The stated attribution has not been independently verified as a route- and formulation-matched human PK measurement.
50%of reference level
Illustrative scenario using an unverified reference estimate.
About 3% remaining after 7 h
Five half-lives in this estimated model. This is not a prediction of when effects stop.
About this estimate
Population: Not established by the reference estimate
Source’s stated attribution: Dixon et al. 1991 J Clin Pharmacol (PMID 2037706) - IV PK in healthy volunteers
Source’s reported peak time: 15 min. This has not been independently confirmed and is not used in the elimination curve.
100 × 2−time / half-life. Time zero is a reference level, not the moment of administration. Absorption, repeated dosing, metabolites and clinical effects are not modeled. Five half-lives leaves 3.125%, not zero. This curve cannot determine a dosing interval.
What to expect
Study outcomes
Clinical development encountered renal toxicity
An early MDS/AML study was stopped after serious renal adverse effects at its highest tested dose. Cell activity did not establish a favorable human benefit-risk balance.1
Reported timelines
Reference & communityWeeks 1–2 / 2–4 / 4–8
Reference/community sequence: energy/exercise; fuel shifts; body composition/endurance. No validated oral/SubQ human timeline.14
These are reported timelines, not a prediction of your response.
Doses & schedules
Route
Scroll to compare all columns →
| Route | Dose | Frequency | Goal / evidence | Duration | References |
|---|---|---|---|---|---|
| IVIntravenous (IV) | 500 mg-1 g | Single IV infusion over 60-120 min | Human research protocol (Koistinen et al. 2003, PMID 12716734)Reference report | 4-8 weeks (community); single-session or short course (research) | 14 |
Population Population not independently verified; see the reference and linked research. Context Reported in Pep-Pedia’s educational protocol table. Study attribution and applicability to this exact product are not independently established. Pep-Pedia misattributes an IV protocol to an isolated-muscle experiment and confuses running time with distance in its mouse study summary. Source tabs Injectable | |||||
| SubQSubQ injection | 50-200 mg | Once daily | Community SubQ protocol (anecdotal; no peer-reviewed human data)Reference report | 4-8 weeks (community); single-session or short course (research) | 14 |
Population Population not independently verified; see the reference and linked research. Context Reported in Pep-Pedia’s educational protocol table. Study attribution and applicability to this exact product are not independently established. Pep-Pedia misattributes an IV protocol to an isolated-muscle experiment and confuses running time with distance in its mouse study summary. Source tabs Injectable | |||||
No protocols match these filters.
Study and label doses retain their study context. Reference reports are unvalidated practices, not personal treatment instructions. Ranges remain ranges; escalation stages are labeled.
Reported use periods and breaks. These do not establish a safe cycle or prove that breaks prevent tolerance.
Injectable
- Use period
- 4-8 weeks (community); single-session or short course (research)
- Break
- 4 weeks minimum between cycles (community convention; no human data)
Reported timing
Morning (community practice); pre-exercise timing used in some research contexts
Oral
- Use period
- Not established
- Break
- Not applicable
Reported timing
Not established
Animal and cell protocols 1
Laboratory exposures cannot establish a human dose.
Scroll to compare all columns →
| Route | Dose | Frequency | Goal / evidence | Duration | References |
|---|---|---|---|---|---|
| OtherIntraperitoneal (IP, mice) | 500 mg/kg | Daily IP injection for 4 weeks | Animal reference (Narkar et al. 2008; Winder and Hardie 1996)Reference report | 4-8 weeks (community); single-session or short course (research) | 14 |
Population Population not independently verified; see the reference and linked research. Context Reported in Pep-Pedia’s educational protocol table. Study attribution and applicability to this exact product are not independently established. Pep-Pedia misattributes an IV protocol to an isolated-muscle experiment and confuses running time with distance in its mouse study summary. Source tabs Injectable | |||||
No protocols match these filters.
Side effects & safety
Serious renal adverse effects
Reported at the highest tested dose in the small hematologic clinical program.
1Symptoms
Sweating, confusion, shaking, dizziness may indicate hypoglycemia; muscle pain, weakness, rapid breathing or abdominal symptoms need assessment. Also infection, palpitations, breathlessness and allergy.
Pregnancy
Pregnancy/lactation safety unstudied.
Not a complete safety screen. Discuss health decisions with a qualified clinician.
Combinations & interactions
9 entriesCheck cautions and reported pairings. A compatibility claim does not establish that a combination is safe.
5-Amino-1MQ
Caution reportedGlucose effects.14
Reference report · Pep-Pedia label: Monitor CombinationMetformin
Caution reportedGlucose/lactate concerns.14
Reference report · Pep-Pedia label: Monitor CombinationInsulin / GLP-1 agonists
Caution reportedAdditive glucose lowering.14
Reference report · Pep-Pedia label: Use CautionSemaglutide
Caution reportedGlucose effects.14
Reference report · Pep-Pedia label: Monitor CombinationMOTS-c
Unverified pairingAMPK pathways.14
Reference report · Pep-Pedia label: SynergisticSLU-PP-332
Unverified pairingOxidative metabolism rationale.14
Reference report · Pep-Pedia label: SynergisticNAD+
Unverified pairingSeparate pathways.14
Reference report · Pep-Pedia label: CompatibleAdenosine-related medications
Unverified pairingPurine-metabolism interactions possible.14
Reference report · Evidence context: UnknownOther medicines and research compounds
Not establishedNo clinical interaction study for the exact proposed combination was verified; absence of evidence does not establish compatibility.3
Research contextNo matching interactions. Try another name or filter.
Reconstitution
No universal bacteriostatic-water volume or validated preparation method is established for this entry.3
Reference preparation details
Reported handling information, not a validated formulation or instruction to prepare an injectable product.
Injectable
Pep-Pedia separates subcutaneous preparation from IV preparation.
- Solvents mentioned
- Bacteriostatic water — subcutaneous report / Normal saline — IV report
- Reported parameters
- Subcutaneous report: bacteriostatic water, 2–8°C, 14–28 days. · IV report: normal saline, prepared fresh; the source advises against storing premixed IV bags. · The source describes 1–2 mL as community subcutaneous injection volume.
Oral
The oral section describes capsules or powder but reports no validated human oral bioavailability or established dose.
- Form
- Source describes a prepared product
Appearance & documentation
Appearance and a purity certificate cannot establish sterility, identity, or suitability for injection.
Reported appearanceWhite crystalline powder appearanceReported appearanceThird-party COA with HPLC purity above 98%Reported appearanceClear colorless solution after reconstitutionReported appearanceRefrigerated or frozen storage prior to reconstitutionReported concernClumping, discoloration, or unusual odorReported concernNo COA or unverified purity claims
14Available forms
No verified packaging examples included.
Packaging examples, not a market survey. Approved and research products are not interchangeable.
Storage after mixing
Reconstituted research vials
Refrigerated lifetime not established
The checked sources do not establish how long this research preparation remains stable and sterile after mixing.14
Storage notes
14Refrigerate reconstituted solution at 2-8 degrees C
Room temperature, dry place
Storage depends on the formulation, diluent, container, and handling. Follow the specific product label or pharmacist’s instructions.
Evidence limits
View findings →Research-market product identity, purity and formulation cannot be established from a publication.1
5 distinct primary sources or abstracts checked. Evidence may concern a parent compound, individual blend ingredient, animal, or cell model; it does not necessarily establish a benefit for this exact product.
Evidence definitions →Research findings
Human trialsSource context
Pep-Pedia misattributes an IV protocol to an isolated-muscle experiment and confuses running time with distance in its mouse study summary.
Compound identity & other names
A nucleoside used to investigate cellular energy sensing. Human trials addressed cardiac surgery and hematologic disease; they do not establish an exercise-replacement or self-directed fat-loss treatment.
Other names: AICAR
Investigational acadesine; no FDA-approved weight-loss or exercise indication.
Acadesine / AICA riboside2
Pep-Pedia identity record
N/A · 338.21 g/mol
Reference description; checked chemical identity takes precedence when available.14
How it may work
Intracellular ZMP activates AMPK; some metabolic and cell-cycle effects are AMPK-independent.14
Clinical development encountered renal toxicity
An early MDS/AML study was stopped after serious renal adverse effects at its highest tested dose. Cell activity did not establish a favorable human benefit-risk balance.
1Source checks & newer research
AICAR / acadesine: Isolated human skeletal muscle
Koistinen 2003 exposed isolated skeletal muscle from men with and without type 2 diabetes to AICAR in vitro. It supports tissue glucose-transport/GLUT4 findings, not a 500 mg–1 g human infusion regimen.
Isolated human skeletal muscle; PubMed abstract checked15AICAR / acadesine: Mouse experiment
After four weeks, AICAR alone increased sedentary mouse treadmill running time by about 23% and distance by about 44%. The 44% value was not an AICAR/GW1516 combination result.
Mouse experiment; original Cell paper indexed full text checked16AICAR / acadesine: Placebo-controlled double-blind human PK study
Dixon 1991 actually studied both oral and IV AICA-riboside in healthy men. Oral solution bioavailability was below 5%; post-infusion terminal half-life averaged 1.4 hours. This contradicts the reference claim that no human oral PK study exists.
Placebo-controlled double-blind human PK study; PubMed abstract checked17Research areas and evidence gaps
Cellular energy and oncology research. AICA riboside is metabolized to ZMP; energy-sensing experiments are not evidence for athletic use.1
- Research-market product identity, purity and formulation cannot be established from a publication.
Additional uses listed by Pep-Pedia
Metabolism. Glucose uptake, insulin sensitivity, GLUT4 and fatty-acid oxidation.14
Exercise. Animal endurance, mitochondrial biogenesis and oxidative muscle-gene changes.14
Aging. Caloric-restriction signaling and metabolic-flexibility hypotheses; longevity unproven.14
Route limitations. Human IV research does not validate oral or subcutaneous use.14
Community reports Unvalidated
Performance discussions as described by Pep-Pedia.3
No representative survey, independently verified products, or controlled outcomes.
Search coverage and review status
The targeted check identified relevant additional literature or current regulatory information; checked findings are separated from retained bibliography-only references.
- Checked
- 2026-10-12
- Search
- AICAR acadesine 2025 2026 clinical trial site:pubmed.ncbi.nlm.nih.gov
- Catalog
- Pep-Pedia ↗ · 9 listed references retained
- Targeted search, not an exhaustive systematic review.
- Bibliography-only entries are retained for traceability and are not treated as verified findings.
AI-prepared summaries. Independent medical editorial review is pending.
Community poll 1 topics · Pep-Pedia snapshot
Voluntary, unverified reports. These percentages do not measure effectiveness or safety.
Experience
Number of responses to this question: not disclosed.
Source & limitations
The source displays “3 responses” for this profile. This is not a confirmed participant count or a denominator for individual questions.
- Voluntary self-reports from Pep-Pedia visitors; identity, treatment, outcomes and timing are unverified. These data are not efficacy or safety estimates.
- The source displays a profile-wide response label, not a confirmed unique participant count. It stays unchanged across questions. Question-specific denominators and absolute option counts are not exposed.
- Only the top five categories are displayed for some questions. Extra categories are retained as an undisplayed-category count; their labels and percentages are unavailable.
- Displayed percentages are rounded. They may not total 100%, especially where categories are hidden.
- This is a dated snapshot, not a live survey or current recommendation.
References
Original sources and review status. Open a reference to read its summary.
1Acadesine Circumvents Azacitidine Resistance in Myelodysplastic Syndrome and Acute Myeloid LeukemiaAbstract checked
AI-PREPARED SUMMARY
Small early clinical program stopped after serious renal effects at the highest tested dose; mechanistic cell findings do not establish clinical benefit.
Clinical development encountered renal toxicity
An early MDS/AML study was stopped after serious renal adverse effects at its highest tested dose. Cell activity did not establish a favorable human benefit-risk balance.
Additional research · Checked 2026-10-12
2PubChem: Acadesine / AICA ribosidePrimary source checked
AI-PREPARED SUMMARY
Chemical registry identity, molecular formula and molecular weight; not clinical efficacy evidence.
Additional research · Checked 2026-10-12
3Pep-Pedia: AICAR / acadesine — community referenceCommunity source checked
AI-PREPARED SUMMARY
Accessed October 12, 2026. Secondary descriptions and bibliography; community schedules are unvalidated reports, not recommendations.
4AICAR endurance experiment in sedentary mice (2008)Primary source checked
AI-PREPARED SUMMARY
After four weeks, AICAR alone increased sedentary mouse treadmill running time by about 23% and distance by about 44%. The 44% value was not an AICAR/GW1516 combination result.
Pep-Pedia bibliography; reconciled with an existing checked primary-source record · Checked 2026-10-12
5AICAR and Insulin-Stimulated Glucose Transport - Hayashi et al. (1998)Pep-Pedia report · Primary source not checked
AI-PREPARED SUMMARY
Pep-Pedia reports: Rat muscle experiments linked AICAR to GLUT4 movement and glucose transport without insulin stimulation.
Reported population / model
Rat skeletal muscle
Reported study details
AICAR 2 mM · In vitro / in vivo · GLUT4 translocation
Reported by Pep-Pedia; the linked publication, design, doses and result have not been independently verified here.
Read the Pep-Pedia report ↗Pep-Pedia reference card; original summary of its reported findings · Checked 2026-10-12
6Merrill, Kurth, Hardie, Winder - AMPK Activation by AICAR in Rat Muscle (1997)Pep-Pedia report · Primary source not checked
AI-PREPARED SUMMARY
Pep-Pedia reports: Perfused rat muscle showed AMPK/ACC signaling changes, lower malonyl-CoA and increased fatty-acid oxidation and glucose uptake.
Reported population / model
Rat hindlimb perfusion model
Reported study details
AICAR 0.5-2.0 mM · AMPK activity, fatty acid oxidation, glucose uptake
Reported by Pep-Pedia; the linked publication, design, doses and result have not been independently verified here.
Read the Pep-Pedia report ↗Pep-Pedia reference card; original summary of its reported findings · Checked 2026-10-12
7AICAR in isolated human skeletal muscle (2003)Abstract checked
AI-PREPARED SUMMARY
Koistinen 2003 exposed isolated skeletal muscle from men with and without type 2 diabetes to AICAR in vitro. It supports tissue glucose-transport/GLUT4 findings, not a 500 mg–1 g human infusion regimen.
Pep-Pedia bibliography; reconciled with an existing checked primary-source record · Checked 2026-10-12
8Abbott et al. - AICAR and Fatty Acid Oxidation (2000)Pep-Pedia report · Primary source not checked
AI-PREPARED SUMMARY
Pep-Pedia reports: Rat cardiac metabolism shifted toward fatty-acid use alongside changes in malonyl-CoA decarboxylase activity.
Reported population / model
Rat heart
Reported study details
AICAR IV infusion · Biochemical endpoints · Fatty acid metabolism
Reported by Pep-Pedia; the linked publication, design, doses and result have not been independently verified here.
Read the Pep-Pedia report ↗Pep-Pedia reference card; original summary of its reported findings · Checked 2026-10-12
9Oral and IV AICA-riboside pharmacokinetics in healthy men (1991)Abstract checked
AI-PREPARED SUMMARY
Dixon 1991 actually studied both oral and IV AICA-riboside in healthy men. Oral solution bioavailability was below 5%; post-infusion terminal half-life averaged 1.4 hours. This contradicts the reference claim that no human oral PK study exists.
Pep-Pedia bibliography; reconciled with an existing checked primary-source record · Checked 2026-10-12
10RED-CABG Trial - Newman et al. (2012)Pep-Pedia report · Primary source not checked
AI-PREPARED SUMMARY
Pep-Pedia reports: The 3,080-patient trial stopped for futility: the composite clinical endpoint did not improve. Hypoglycemia was reported in 0.42% versus 0% with placebo.
Reported population / model
Humans
Reported study details
n=3,080 randomized · Acadesine 0.1 mg/kg/min IV for 7 hrs · CABG surgery
Reported by Pep-Pedia; the linked publication, design, doses and result have not been independently verified here.
Read the Pep-Pedia report ↗Pep-Pedia reference card; original summary of its reported findings · Checked 2026-10-12
11AICAr: AMPK-Independent Effects Systematic Review (2021)Pep-Pedia report · Primary source not checked
AI-PREPARED SUMMARY
Pep-Pedia reports: The review separates AMPK-mediated actions from effects on nucleotide metabolism; AICAR activity alone cannot establish an AMPK-specific mechanism.
Reported population / model
Systematic review
Reported study details
Cells, Vol. 10(5) · PMID: 34064363 · Comprehensive mechanistic analysis
Reported by Pep-Pedia; the linked publication, design, doses and result have not been independently verified here.
Read the Pep-Pedia report ↗Pep-Pedia reference card; original summary of its reported findings · Checked 2026-10-12
12WADA Prohibition - AICAR Added to Prohibited ListPep-Pedia report · Primary source not checked
AI-PREPARED SUMMARY
Pep-Pedia reports: The source describes AICAR as prohibited in sport under metabolic modulators. Current rules and exemption eligibility require the governing body's current policy.
Reported population / model
Anti-doping policy
Reported study details
S4 Hormone and Metabolic Modulators · Ongoing
Pep-Pedia supplies no original study link for this card. Study identity, design, doses and result remain unverified.
Read the Pep-Pedia report ↗Pep-Pedia reference card; original summary of its reported findings · Checked 2026-10-12
13Pep-Pedia: AICAR / acadesine — reported pharmacokineticsReference estimate; not independently verified human PKCommunity source checked
AI-PREPARED SUMMARY
Lists a half-life of 1.4 hrs and a peak time of 15 min. Stated attribution: Dixon et al. 1991 J Clin Pharmacol (PMID 2037706) - IV PK in healthy volunteers. This value is reported by a secondary reference. The stated attribution has not been independently verified as a route- and formulation-matched human PK measurement. Five half-lives is not complete clearance, and the source’s “cleared” value is not used as a measured endpoint.
Secondary reference page checked; the underlying quantitative claim is not independently confirmed. · Checked 2026-10-12
14Pep-Pedia: AICAR / acadesine — route-specific referenceReference page checked; underlying claims require separate verification.Community source checked
AI-PREPARED SUMMARY
Source page checked across available routes. Protocols, cycles, storage, mechanisms and pairing claims are secondary reports; checking the page does not independently validate those claims. Original concise summaries are used here.
Content coverage audit · Checked 2026-10-12
15AICAR / acadesine: Isolated human skeletal muscleAbstract checked
AI-PREPARED SUMMARY
Koistinen 2003 exposed isolated skeletal muscle from men with and without type 2 diabetes to AICAR in vitro. It supports tissue glucose-transport/GLUT4 findings, not a 500 mg–1 g human infusion regimen.
AICAR / acadesine: Isolated human skeletal muscle
Koistinen 2003 exposed isolated skeletal muscle from men with and without type 2 diabetes to AICAR in vitro. It supports tissue glucose-transport/GLUT4 findings, not a 500 mg–1 g human infusion regimen.
Additional primary-source check · Checked 2026-10-12
16AICAR / acadesine: Mouse experimentPrimary source checked
AI-PREPARED SUMMARY
After four weeks, AICAR alone increased sedentary mouse treadmill running time by about 23% and distance by about 44%. The 44% value was not an AICAR/GW1516 combination result.
AICAR / acadesine: Mouse experiment
After four weeks, AICAR alone increased sedentary mouse treadmill running time by about 23% and distance by about 44%. The 44% value was not an AICAR/GW1516 combination result.
Additional primary-source check · Checked 2026-10-12
17AICAR / acadesine: Placebo-controlled double-blind human PK studyAbstract checked
AI-PREPARED SUMMARY
Dixon 1991 actually studied both oral and IV AICA-riboside in healthy men. Oral solution bioavailability was below 5%; post-infusion terminal half-life averaged 1.4 hours. This contradicts the reference claim that no human oral PK study exists.
AICAR / acadesine: Placebo-controlled double-blind human PK study
Dixon 1991 actually studied both oral and IV AICA-riboside in healthy men. Oral solution bioavailability was below 5%; post-infusion terminal half-life averaged 1.4 hours. This contradicts the reference claim that no human oral PK study exists.
Additional primary-source check · Checked 2026-10-12