AICAR

AICAR is a research peptide that tricks the body into thinking it has exercised, helping to boost energy use and metabolic activity. It works by activating AMPK, a master regulator of energy balance. AICAR is being studied for its potential roles in fat loss, insulin sensitivity, anti-inflammatory action, and heart health. AICAR (5-Aminoimidazole-4-carboxamide ribonucleotide) is a nucleoside analog that activates AMP-activated protein kinase (AMPK), a critical energy sensor in cells. This mimics the biochemical effects of exercise by promoting energy production and shifting the body to burn fat instead of storing it. In animal models, AICAR has demonstrated improved glucose uptake, enhanced fatty acid oxidation, increased endurance, and reduced inflammation. Notably, it appears most effective in metabolically compromised states, such as obesity or insulin resistance. Beyond metabolic health, AICAR is also being explored for its roles in cardiovascular protection, fertility, and cancer metabolism.

- Mimic benefits of exercise without physical exertion

- Seek improved insulin sensitivity, fat loss, and metabolic flexibility

- Explore anti-inflammatory or cardioprotective research tools

How this peptide works in the body

AMPK Activation:

AICAR is converted into ZMP, an AMP analog that directly activates AMP-activated protein kinase (AMPK), bypassing the need for ATP depletion. AMPK then promotes catabolic processes like fatty acid oxidation while inhibiting anabolic pathways (e.g., lipid synthesis) through phosphorylation of acetyl-CoA carboxylase (ACC) and inhibition of mTOR signaling.

Mitochondrial Enhancement:

Activation of AMPK upregulates PGC-1α (peroxisome proliferator-activated receptor gamma coactivator 1-alpha), stimulating mitochondrial biogenesis and enhancing oxidative phosphorylation. This supports endurance, energy efficiency, and anti-aging pathways.

Anti-Inflammatory Effects:

AICAR downregulates pro-inflammatory mediators like TNF-α and IL-6, partly through SIRT1 activation and inhibition of NF-κB signaling. These actions have been associated with protective effects in colitis, atherosclerosis, and autoimmune conditions.

Insulin Sensitization:

AMPK activation increases GLUT4 translocation to the cell surface, enhancing glucose uptake in skeletal muscle. It also suppresses lipogenesis and reduces inflammation in adipose tissue, improving insulin receptor sensitivity.

Cardioprotection:

In ischemic models, AICAR pre-treatment enhances myocardial ATP availability and reduces infarct size. It inhibits vascular smooth muscle proliferation and protects endothelial function through nitric oxide (NO) regulation.

Anti-Cancer Activity:

AICAR has been shown to suppress mTOR and induce p21-mediated apoptosis in cancer cells. Long-term AMPK activation in tumor cells disrupts metabolic plasticity, potentially impairing survival in nutrient-limited environments.