AICAR
AICAR (5-Aminoimidazole-4-carboxamide ribonucleotide) is a synthetic AMP analog investigated for its ability to activate AMPK, a master regulator of cellular energy metabolism. It is studied in research models focused on endurance capacity, glucose uptake, fatty acid oxidation, and mitochondrial biogenesis, with particular interest in metabolic and exercise physiology applications.
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Description
AICAR (5-Aminoimidazole-4-carboxamide ribonucleotide) is a cell-permeable nucleotide analog and a direct activator of AMP-activated protein kinase (AMPK), a master regulator of cellular energy homeostasis. It is widely studied as a research compound for its ability to mimic the metabolic state of exercise and caloric restriction in experimental models.
In preclinical studies, AICAR has been observed to enhance fatty acid oxidation, stimulate mitochondrial biogenesis, and increase glucose uptake in skeletal muscle independently of insulin signaling. Through activation of AMPK, it modulates downstream pathways including PGC-1α, ACC, and mTOR, shifting cellular metabolism toward catabolic, energy-producing processes.
AICAR has also been investigated for its effects on endurance capacity, muscle fiber-type transition, and metabolic adaptation in rodent models, often referred to in literature as an “exercise mimetic.” Additional research has explored its role in cardioprotection, anti-inflammatory signaling, and glucose regulation in models of metabolic dysfunction.
Supplied as a lyophilized powder for reconstitution, AICAR is intended for in vitro and in vivo laboratory applications under controlled experimental conditions.
Clinical Status:
AICAR is a research compound studied extensively in animal models and in vitro systems for AMPK activation, metabolic modulation, and exercise mimetic effects. It is not approved for human medical or therapeutic use and remains restricted to experimental and laboratory research. AICAR is listed on the WADA Prohibited List as a metabolic modulator in competitive sport.
Evidence type:
Human RCT ☐ | Observational ☐ | Animal ✔ | In vitro ✔ | Regulatory ✔
Mechanism of Action
AICAR works by mimicking adenosine monophosphate (AMP), the cellular signal of low energy. Once inside the cell, it is phosphorylated into ZMP, which directly activates AMP-activated protein kinase (AMPK). This activation shifts metabolism toward fatty acid oxidation, glucose uptake, and mitochondrial biogenesis, while suppressing anabolic pathways and enhancing endurance-related gene expression in experimental models.
Benefits
- AMPK Pathway Activation:
AICAR is one of the most widely used pharmacological activators of AMP-activated protein kinase (AMPK), a master regulator of cellular energy homeostasis. By mimicking AMP, AICAR allosterically activates AMPK without altering ATP levels directly. This mechanism has positioned AICAR as a foundational research tool for studying metabolic stress responses, nutrient sensing, and energy-deficient cellular states in laboratory models. - Enhanced Fatty Acid Oxidation:
In experimental models, AICAR has been observed to stimulate fatty acid oxidation in skeletal muscle and hepatic tissue through inhibition of acetyl-CoA carboxylase (ACC). This shift toward lipid utilization has been studied in models of obesity, hepatic steatosis, and metabolic dysfunction. Researchers frequently use AICAR to investigate substrate-switching mechanisms relevant to metabolic flexibility. - Glucose Uptake Modulation:
AICAR has been reported to promote insulin-independent glucose uptake in skeletal muscle through GLUT4 translocation. This effect, mediated via AMPK activation, mirrors aspects of contraction-induced glucose transport and makes AICAR a key compound in research focused on insulin resistance, type 2 diabetes mechanisms, and exercise-mimetic pathways. - Endurance and Exercise-Mimetic Effects:
Animal studies have shown that AICAR can induce a shift toward oxidative muscle fiber phenotypes and increase endurance capacity even in sedentary subjects. This “exercise-in-a-pill” property has made AICAR a major focus in research on muscle metabolism, mitochondrial adaptation, and the molecular basis of training adaptations. - Mitochondrial Biogenesis:
Research models indicate that AICAR upregulates PGC-1α expression, a transcriptional coactivator that drives mitochondrial biogenesis. Increased mitochondrial density and oxidative capacity have been documented in skeletal muscle following AICAR administration, supporting its use as a probe for studying mitochondrial dynamics and energy metabolism. - Anti-Inflammatory Modulation:
AICAR has been investigated for its anti-inflammatory properties in models of autoimmune and inflammatory disease. By modulating NF-κB signaling and reducing pro-inflammatory cytokine production, AICAR has shown effects in experimental models of multiple sclerosis, colitis, and ischemia-reperfusion injury. These observations support its broader role as a metabolic-immune crosstalk research tool. - Cardioprotective Research Applications:
In preclinical cardiovascular studies, AICAR has been reported to reduce ischemic injury and improve recovery following reperfusion. The compound has been evaluated for its ability to preserve myocardial ATP levels, reduce infarct size, and modulate apoptotic signaling. These properties make AICAR a relevant compound in cardioprotection and metabolic stress research. - Cellular Stress Response and Autophagy:
AICAR has been observed to induce autophagy through AMPK-mTOR signaling crosstalk, supporting cellular cleanup mechanisms and protein quality control. This effect has been investigated in research models of neurodegeneration, cancer metabolism, and aging, where dysregulated autophagy plays a central role. AICAR remains a standard reference compound for autophagy induction studies.
Research Data
| Study / Model | Reported effect |
|---|---|
| Sedentary mice (4-week oral administration) | ↑ endurance capacity by ~44% without exercise training |
| Skeletal muscle (rodent models) | ↑ AMPK phosphorylation, ↑ PGC-1α expression, enhanced mitochondrial biogenesis |
| Diet-induced obese mice | ↓ adiposity, improved glucose tolerance, ↑ fatty acid oxidation |
| Insulin-resistant rat models | ↑ GLUT4 translocation, improved insulin sensitivity in skeletal muscle |
| Ischemia-reperfusion cardiac models | Reduced infarct size and improved post-ischemic recovery |
| In vitro myocyte culture | ↑ glucose uptake and mitochondrial oxidative capacity |
| Aged rodent models | Partial restoration of mitochondrial function and metabolic flexibility |
Stack Suggestions
AICAR is often combined in research with:
- AICAR + GW501516 → Synergistic activation of AMPK and PPARδ pathways for enhanced endurance and fatty acid oxidation models.
- AICAR + Metformin → Complementary AMPK activation for studies on glucose uptake and insulin sensitivity.
- AICAR + MOTS-c → Combined mitochondrial biogenesis and metabolic regulation in cellular energy research.
- AICAR + 5-Amino-1MQ → Parallel modulation of NAD+ and AMPK pathways for metabolic and fat-loss models.
⚠ Stacks are for experimental design only; not safety or efficacy guidance.
Pen Dosage Chart
| AICAR Pen 100 mg | |
| Volume | 3 mL |
| mg/mL | 33.333 mg/mL |
| Click-to-Dose | 1 click = 0.333 mg |
| Example(s) | 10 clicks = 3.333 mg |
Dosage & Protocols Variations
Standard Research Protocol
- Dose: 0.5 – 1.0 mg/kg
- Duration: 4 – 6 weeks
- Frequency: Daily
- Cycle Interval: 2 – 4 weeks off before repeating
- Goal / Description: Baseline AMPK activation models for metabolic and endurance research.
Therapeutic Research Protocol
- Dose: 1.0 – 2.0 mg/kg
- Duration: 4 – 8 weeks
- Frequency: Daily
- Cycle Interval: 4 weeks off before repeating
- Goal / Description: Higher-dose studies targeting glucose uptake and lipid oxidation.
Biohacker Protocol (experimental)
- Dose: 0.25 – 0.5 mg/kg
- Duration: 6 – 8 weeks
- Frequency: 3 – 5× per week
- Cycle Interval: 2 weeks off
- Goal / Description: Microdose continuous mitochondrial and endurance research.
Possible Side Effects
AICAR is generally well-tolerated in animal studies and limited human research settings.
Reported side effects are infrequent and typically mild:
- Transient elevation in plasma lactate and uric acid levels.
- Mild hypoglycemia or fluctuations in blood glucose during administration.
- Headache or dizziness observed in early infusion studies.
- Localized irritation at injection site in subcutaneous research models.
- Reduced heart rate and mild hemodynamic changes in cardiovascular research protocols.
No evidence of hepatotoxic, nephrotoxic, or hormonal adverse effects has been observed in available preclinical data.
Product Attributes
- CAS #: 2627-69-2
- Molecular Formula: C9H14N4O8P
- Sequence (AA): N/A (nucleotide analog, not a peptide)
- Molecular Weight: 338.21 g/mol
- PubChem CID: 65110
- Half-Life: ~30 minutes (plasma)
- Synonyms: Acadesine, ZMP precursor, 5-Aminoimidazole-4-carboxamide-1-β-D-ribofuranoside, AICA riboside, AICA ribonucleotide
- Type: Synthetic AMP analog / AMPK activator (small molecule)
- Research Focus: Metabolism & Energy, Recovery & Performance
Scientific References
- AMP-activated protein kinase: ancient energy gauge provides clues to modern understanding of metabolism Animal | In vitro
- AMPK and PPARdelta agonists are exercise mimetics Animal | In vitro
- AMPK: a contextual oncogene or tumor suppressor? Animal | In vitro
- 5-aminoimidazole-4-carboxamide riboside increases glucose transport and cell-surface GLUT4 content in skeletal muscle Animal | In vitro
- AICAR and metformin, but not exercise, increase muscle glucose transport through AMPK-, ERK-, and PDK1-dependent activation of atypical PKC Animal | In vitro
- AICAR inhibits adipocyte differentiation in 3T3L1 and restores metabolic alterations in diet-induced obesity mice Animal | In vitro
- WADA Prohibited List – Hormone and Metabolic Modulators (S4) Regulatory
- AMPK activation by AICAR reduces ischemic injury and improves mitochondrial function Animal | In vitro
Included In The Box
Every product arrives in a premium, custom-designed PEPTIDE.Power box, engineered for convenience, hygiene, and safe storage in your refrigerator. Inside, you will find everything needed for your full research protocol:
- 1× Disposable Pre-Mixed Injection Pen
- Powered by our proprietary PSM Technology™ – precision stabilization & mixing system for consistent potency
- 10× Ultra-thin Needles (33G, 4 mm)
- 10× Alcohol Pads for sterile preparation
- Internal Stabilizing Foam Insert to prevent shaking during transport
- Instruction Panel printed on the inside of the box for quick reference
- Security Seal Sticker ensuring the package has not been opened or tampered with
Storage
Store the product in a refrigerator at 1 – 8°C immediately upon delivery. To maintain optimal stability, keep the pen away from light, and do not expose it to repeated temperature changes.
Once reconstituted (all our pens come pre-mixed), research compounds remain stable for 6 – 8 weeks under proper refrigeration.
Do not freeze after reconstitution. Always keep the box closed so the pen, needles, and alcohol pads stay clean and protected.
For best results, use the product consistently within the recommended time window and always follow your research protocol.
Delivery
We ship with Next-Day EU Delivery via DHL Express or UPS Express.
All orders are prepared fresh on the day of dispatch, placed in EPS Cold-Chain Transport Boxes, and shipped with cooling elements to maintain a stable temperature throughout the journey.
Our logistics process is designed so the package arrives overnight, avoiding customs delays inside the European Union.
Products are shipped from our EU facility, ensuring no import duties, no customs clearance, and always fast and secure delivery.
Payment
Due to the nature of research peptides and the high-risk category assigned by payment processors, credit card companies do not generally support merchants in this field.
For this reason, we accept mainly Bank Transfers.
We also work with a crypto payment provider, and from time to time, card payments may be available depending on processor availability.
Within the European Union, SEPA transfers are fast, low-cost, and usually arrive within minutes to a few hours, making the payment process smooth and simple.
Once the transfer is received, your order is prepared immediately and dispatched the same day, depending on the daily cut-off time.
Please note that we do not dispatch shipments on Fridays or on days before official public holidays. This is done to ensure that parcels can be delivered on the next working day and are not held in transit over weekends or holidays.
This method ensures compliance, security, and continuity of service for all customers across the EU.
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