Generic and Brand Names: AICAR, which is also known as Acadesine or 5-Aminoimidazole-4-Carboxamide Ribonucleotide. There are currently no approved brands for the use of this drug for its therapeutic purposes. AICAR is primarily seen as an investigational agent, therefore the drug is referred to by its generic name by professionals working in labs on preclinical studies.
Drug classification: AICAR belongs to the class of AMPK Activator, Purine Nucleoside Analog Metabolic Modulator, Cellular Energy Homeostasis Regulator and Insulin Sensitizing Research Agent
Chemical information: AICAR is a synthetic purine nucleoside analogue that has the following molecular formula, C9H14N4O5, and molecular weight 258.23 Da. This drug is a ribonucleotide derivative that works as a pro-drug metabolized in a cell into ZMP. Like the other amino acid peptides, AICAR exhibits great water solubility, permeability and biochemical stability in physiological conditions.
Mechanism of action
- Activation of receptors and enzymes
The biological mechanism of AICAR action is based on indirect allosteric activation of the Adenosine Monophosphate-Activated Protein Kinase (AMPK) by this agent. After intracellular conversion of AICAR into ZMP, ZMP imitates the AMP and binds to the regulatory domain thus activating the kinase. Due to this mechanism, the agent does not interact with GLP-1, GIP and melanocortin and does not bind to other metabolic receptors.1.2 Metabolic and Physiological Effects
The activation of AMPK that occurs because of AICAR is thought to improve overall human metabolism, which is important for research involving metabolism-related disorders. The stimulation effects include an increase in insulin sensitivity and glucose uptake in muscles and fat tissues, as well as a decrease in glucose production by the liver, which leads to the stabilization of glucose levels in the blood leading to improvements in the symptoms of type 2 diabetes. This compound enhances the process of fat burning, prevents fat production, and contributes to increased total energy expenses of the organism, which helps to control the weight problems of a person. What is more, the compound can reduce metabolic abnormalities caused by intermittent hypoxia.
- Indications and Usage (Research Only)
The use of AICAR is limited to scientific research only, as there is no permission for its application in medical procedures.
Type 2 Diabetes Mellitus Research: It is used in the experiments concerning insulin resistance, impaired glucose tolerance, and liver metabolism in terms of the effects of AMPK.
Chronic Weight Management Research: It is applied in studies involving obesity in terms of fat burning process and energy balance regulation.
Obstructive Sleep Apnea Research: Aicarm use in research helps improve metabolicCore Energy Metabolism Study: It is considered a highly recommended research method in studying the AMPK biochemical pathway, cellular energy homeostasis and the mechanisms of metabolic adaptations during physical exercise.
- Dosage and administration (research laboratory standards)
3.1 Routes and frequencies
AICAR Peptide is for research use only and academic experimental purposes. It is not registered as a pharmaceutical drug, dietary supplement or an over-the-counter medicine and has no clinical use approval from the FDA, EMA or other regional medical regulatory body. The product cannot be used for human clinical diagnosis, treatment of disease, oral or intravenous administration as well as commercial off-label usage. All of the product details and research data is academic in nature and not intended as medical advice or to be construed as therapeutic claims. Local laws, institutional laboratory-management requirements, and ethical-research standards must be followed by all purchasers and researchers. We shall not be liable for any unauthorized illegal use, improper operation or non-research application of the product.
The laboratory administration routes for AICAR include subcutaneous and intraperitoneal injections, as well as supplementation with the drug in vitro cell culture medium. In the case of investigational studies, an intraperitoneal injection is preferred to a subcutaneous one owing to better drug delivery. AICAR is administered to the subjects in compliance with the research study protocols according to one of the two routes mentioned.
3.2 Titration schedule
In the field of animal research, the dosage levels that can be used in primary AMPK activation experiments are established before the commencement of the animal study. Thus, the first dose is 50 mg/kg daily, and a medium dosage of 100-150 mg/kg daily can be administered to achieve the necessary metabolic effect. Maximum dosage level allowed in the preclinical studies is not more than 200 mg/kg daily in order not to exceed the safety limits of AMPK activation.
3.3 Missed dose management
In all standardized laboratory protocols, missed doses of AICAR do not imply any corrective dosages to be administered after that. Cancelled doses are reported by researchers, and no additional laboratory procedures are carried out after that. Giving overdoses is forbidden in order to avoid receiving unreliable outcomes in the course of preclinical studies.
- Dosage forms
AICAR is available in the form of a pure crystalline powder for laboratory purposes. It can be diluted with sterile saline prior to its insertion into the biological object. No capsules and tablets with AICAR are produced.
- FDA classification of AICAR
AICAR has been classified as a drug meant only for research purposes according to FDA classification system. No researches have been conducted in humans so far.
10 Common FAQs About Peptides
- What is a peptide?
Answer: A peptide is a short chain of amino acids linked together by peptide bonds. It is smaller and more easily absorbed by the human body than proteins, serving as a fundamental functional substance in biological organisms.
- What is the difference between peptides and proteins?
Answer: The core difference lies in molecular length and structure. Peptides are short amino acid chains (usually consisting of 2–50 amino acids), while proteins are long, complex amino acid chains with stable three-dimensional structures. Peptides have stronger permeability and faster absorption efficiency than proteins.
- What are the main types of peptides?
Answer: Peptides are mainly classified by the number of amino acids: dipeptides, tripeptides, oligopeptides (2–10 amino acids) and polypeptides (10–50 amino acids). They can also be divided into natural peptides and synthetic peptides according to their sources.
- What are the biological functions of peptides?
Answer: Peptides have diverse biological activities, including regulating human metabolism, improving immune function, promoting cell repair, anti-oxidation, anti-aging, and adjusting hormone levels. They act as key signaling molecules and regulatory factors in the body.
- Are peptides safe for human use?
Answer: Most natural and medically approved synthetic peptides are highly safe. They have small molecular weight, low toxicity, and will not accumulate in the body. However, unstandardized high-dose peptide products or impure synthetic peptides may cause mild discomfort.
- What are the common applications of peptides?
Answer: Peptides are widely used in multiple fields. In biomedicine, they are made into therapeutic drugs for endocrine and immune diseases; in cosmetics, they are used for anti-aging and skin repair; in health products, they serve as nutritional supplements to improve physical fitness.
- Can the human body absorb exogenous peptides directly?
Answer: Yes. Unlike proteins that need to be decomposed before absorption, small-molecule peptides can be directly absorbed by the intestinal tract and skin with high absorption rate and utilization efficiency, and can quickly exert biological effects in the body.
- What are synthetic peptides used for?
Answer: Synthetic peptides are artificially customized amino acid chains. They are mainly used for scientific research, clinical drug development, targeted skin care ingredient production, and precise nutritional supplementation, with higher purity and targeted activity than some natural peptides.
- Do peptide products have side effects?
Answer: Standard peptide products have almost no obvious side effects for most people. Individual groups may experience mild gastrointestinal discomfort or skin sensitivity due to physical differences or excessive intake. Long-term excessive use may disrupt the body’s metabolic balance.
- What is the difference between collagen peptides and ordinary peptides?
Answer: Collagen peptides are a specific type of functional peptide extracted and decomposed from collagen, mainly targeting skin moisturizing, anti-wrinkle and joint care. Ordinary peptides cover a broader range with more diverse regulatory functions including immunity and metabolism, while collagen peptides have more focused skincare and anti-aging effects.
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