AICAR INJECTOR PEN 3ML 50MG

AICAR Injector Pen: The AMPK Peptide Activator for Metabolic Signaling, Cellular Energy, and “Exercise-Mimetic” Research. (Now Available in UAE)

In the fast-evolving field of metabolic and performance physiology research, AICAR (also known as Acadesine; 5-aminoimidazole-4-carboxamide ribonucleoside) stands out as a widely used small-molecule tool for studying cellular energy sensing and metabolic adaptation. AICAR is taken up by cells and converted into ZMP, an AMP-analog that can influence AMP-activated protein kinase (AMPK) signaling an intracellular “fuel gauge” that coordinates pathways involved in glucose handling, lipid metabolism, and mitochondrial energetics. Foundational work in skeletal muscle demonstrated that AICAR can activate AMPK-linked signaling with downstream changes consistent with increased substrate utilization and energy regulation, making it a staple reagent in studies of metabolic flexibility and exercise biology.

Unlike stimulants or hormones, AICAR’s core appeal is its ability to probe central metabolic control nodes helping researchers model aspects of energy stress and training adaptation in controlled settings. Importantly, AICAR has also demonstrated AMPK-independent biology in certain contexts (including immune-cell transcriptional regulation), reinforcing the need for careful experimental design and interpretation when attributing effects solely to AMPK.

AICAR has been evaluated in both preclinical models and limited human clinical research primarily via controlled infusion protocols to characterize its acute effects on glucose metabolism and related pathways. However, it is not approved for therapeutic use in humans, and anti-doping authorities explicitly prohibit AICAR in sport due to its potential performance-enhancing effects and lack of established clinical safety for non-medical use.

Below, we explore five key benefits of AICAR as a research compound, each supported by scientific studies from reputable sources such as PubMed/PMC and peer-reviewed journals.

1. Acute Stimulation of Skeletal Muscle Glucose Uptake in Humans AICAR is frequently cited for its ability to increase skeletal muscle glucose uptake in controlled human research settings—one of the most direct translational datapoints supporting its use as a metabolic research tool. In a controlled clinical study in healthy men, AICAR administration increased skeletal muscle 2-deoxyglucose uptake (with a comparatively modest change in whole-body glucose disposal), supporting its use in studies of insulin-independent glucose transport pathways and muscle substrate handling. This effect has also been examined across age and type 2 diabetes cohorts, with findings suggesting that the magnitude of response is influenced more by age than diabetic status per se—an important nuance for designing studies in older or metabolically impaired populations.

2. Reduction of Hepatic Glucose Output and Improvements in Systemic Glucose Flux in Type 2 Diabetes Research AICAR has been studied in vivo in type 2 diabetes to evaluate whether pharmacologic activation of energy-sensing pathways can acutely shift glucose kinetics. In a clinical trial involving male patients with type 2 diabetes, intravenous AICAR reduced hepatic glucose output (lowering the plasma glucose rate of appearance), increased glucose disposal as a fraction of appearance, and was associated with a greater decline in plasma glucose concentration versus control conditions. The same study reported reductions in plasma NEFA kinetics and concentration, consistent with altered lipid mobilization/oxidation dynamics in response to AICAR.

3. Exercise-Mimetic Endurance Adaptation and Oxidative Gene Programming in Animal Models One of the most widely referenced “exercise-mimetic” findings comes from rodent research exploring whether pathway-specific agents can replicate aspects of endurance training adaptation. In a landmark study in mice, AICAR administration in sedentary animals for four weeks induced metabolic gene expression and enhanced running endurance (reported as a 44% increase), supporting its role as a tool for investigating AMPK-linked training biology and oxidative capacity remodeling.

4. Investigated Cardioprotection in Ischemia-Reperfusion and Cardiac Surgery With Mixed Clinical Outcomes AICAR (acadesine) was also investigated as an adenosine-regulating agent in cardiac surgery contexts where ischemia-reperfusion injury contributes to postoperative morbidity and mortality. A meta-analysis pooling individual patient data from five randomized, placebo-controlled trials in CABG surgery reported reductions in perioperative myocardial infarction and early cardiac death with acadesine versus placebo. However, a later large multicenter randomized controlled trial (RED-CABG) was stopped early for futility and did not find a reduction in a composite endpoint of all-cause mortality, nonfatal stroke, or severe left ventricular dysfunction through postoperative day 28. For researchers and clinicians, this “mixed evidence” pattern highlights both the historical promise of AICAR in cardiometabolic stress biology and the importance of large, well-powered clinical validation.

5. Modulation of Inflammatory Transcriptional Responses in Human Macrophages Beyond classic metabolic readouts, AICAR has demonstrated notable effects on inflammatory gene expression in primary human immune cells—useful for investigators studying immunometabolism and transcriptional control during innate immune activation. In primary human macrophages, AICAR potently suppressed LPS-induced inflammatory gene expression and interfered with NFκB (and STAT3) DNA-binding activity, with evidence indicating the effect occurred independently of conversion to the AMPK-activating monophosphate (ZMP). This underscores a critical point for experimental design: AICAR can produce biologic effects that may not be fully explained by AMPK activation alone.

Why Choose Our High-Quality AICAR Research Reagent?

If you are sourcing AICAR for laboratory work, prioritize suppliers that provide: documented purity (e.g., HPLC/LC-MS), lot-specific Certificates of Analysis (COA), appropriate storage/shipping conditions, and clear labeling for research use. Given AICAR’s potential for AMPK-dependent and AMPK-independent effects, rigorous controls (vehicle controls, orthogonal AMPK modulation, genetic knockdown/knockout where feasible, and pathway readouts beyond a single biomarker) materially improve interpretability.

Note: These statements are based on scientific studies and are not intended to diagnose, treat, or cure any disease.

Scientific Studies:

5-aminoimidazole-4-carboxamide 1-beta-D-ribofuranoside acutely stimulates skeletal muscle 2-deoxyglucose uptake in healthy men
Blunting of AICAR-induced human skeletal muscle glucose uptake in type 2 diabetes is dependent on age rather than diabetic status
Intravenous AICAR administration reduces hepatic glucose output and inhibits whole body lipolysis in type 2 diabetic patients
AMPK and PPARdelta agonists are exercise mimetics
Effects of acadesine on myocardial infarction, stroke, and death following surgery (meta-analysis of 5 RCTs)
Effect of adenosine-regulating agent acadesine on morbidity and mortality associated with CABG: the RED-CABG randomized controlled trial
AICAR inhibits NFκB DNA binding independently of AMPK to attenuate LPS-triggered inflammatory responses in human macrophages 

Disclaimer: The summaries above describe findings from published scientific studies and are provided for educational and research‑discussion purposes only. They are not intended to diagnose, treat, cure, or prevent any disease, and they are not a substitute for medical advice. Therefore this product is not intended to be for human consumption!