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AICAR

AICAR, an analog of adenosine monophosphate, has found clinical application in safeguarding against cardiac ischemia post-heart attack. Its antioxidant attributes make it a potential candidate for retarding the natural aging process. Ongoing investigations explore the potential of AICAR in mitigating the impact of conditions such as diabetes, autoimmune disorders, and various inflammatory ailments.

This PRODUCT IS INTENDED AS A RESEARCH CHEMICAL ONLY. This designation allows the use of research chemicals strictly for in vitro testing and laboratory experimentation only. All product information available on this website is for educational purposes only. Bodily introduction of any kind into humans or animals is strictly forbidden by law. This product should only be handled by licensed, qualified professionals. This product is not a drug, food, or cosmetic and may not be misbranded, misused or mislabled as a drug, food or cosmetic.

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1. Introduction to AICAR

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2. AICAR Structure

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3. AICAR Effects

Introduction

AICAR, or 5-aminoimidazole-4-carboxamide ribonucleoside, is a short peptide that contributes to maintaining energy balance and influencing various metabolic pathways. It plays a crucial role in regulating insulin receptors and their function in muscle cells. AICAR is actively being studied for its potential in combating cancer and protecting cardiovascular tissues. It functions as an activator of AMP kinase (AMPK).

AICAR represents the activated form of the naturally occurring acadesine, presently utilized in treating acute lymphoblastic leukemia. Research indicates that, similar to AICAR, acadesine possesses anti-cancer properties and has also been observed to inhibit platelet activity, thus aiding in preventing the early stages of blood clot formation.v

Structure

aicar

Sequence: 5-aminoimidazole-4-carboxamide ribonucleoside
Molecular Formula: C9H15N4O8P
Molecular Weight: 338.213 g/mol
PubChem CID: 65110
CAS Number: 3031-94-5
Synonyms: AICA ribonucletotide, Z-nucleotide

Effects

AICAR and Insulin Resistance
Studies conducted in mice have demonstrated that even at low doses, AICAR exhibits the ability to diminish inflammation in adipose tissue. Inflammation within fat deposits is associated with heightened insulin resistance, and AICAR’s capacity to reduce inflammation contributes to improved glucose regulation and increased insulin sensitivity, irrespective of changes in body weight. AICAR seems to employ various pathways to impact adipose tissue inflammation, with one of these pathways involving SIRT1 and macrophages.

The influence of AICAR on adipose tissue inflammation aligns with expectations, given that AMPK has been shown to mitigate inflammatory responses in metabolic disorders, both in healthy and diabetic mice. Research conducted in mice indicates that the activation of AMPK, as facilitated by AICAR, enhances insulin sensitivity, maintains energy balance, regulates lipid metabolism, and reduces inflammatory markers.

Physical exercise enhances the presence of GLUT-4 insulin receptors on the surface of muscle cells, making it a highly effective method for increasing glucose uptake by these cells and consequently reducing glucose levels and insulin resistance. Interestingly, AICAR closely replicates the effects of exercise and repeated AICAR administration yields outcomes akin to those seen with long-term exercise.

AICAR and Cancer Research
AMPK’s role in cancer growth and metastasis is multifaceted, exhibiting the potential to either decelerate or hasten tumor growth under different conditions. In a broader context, studies suggest that sustained activation of this enzyme ultimately induces the demise of cancer cells by retarding their metabolic processes and rendering them more vulnerable to external stressors. This phenomenon has been substantiated in both laboratory cell cultures and rat-based experiments

Studies conducted on thyroid cancer cells suggest that AICAR may have a role in triggering apoptosis, a programmed form of cell death. This mechanism seems to involve the buildup of p21 and subsequent activation of caspase 3. Consequently, it results in the suppression of cancer cell growth and their ability to survive.

Source: PubMed
Anti-inflammatory Properties

Activation of AMPK has been revealed to play a crucial role in combating cellular-level inflammation. Research focusing on metformin, a widely used diabetes medication, suggests that one of its key mechanisms of effectiveness lies in reducing inflammation and enhancing pancreatic function. Similarly, AICAR exhibits comparable effects, serving as a protective agent in inflammatory conditions such as acute lung injury, asthma, colitis, atherosclerosis, and hepatitis.

Ongoing investigations are exploring the potential of AICAR to modulate the impact of autoimmune diseases and various other inflammatory disorders. For example, studies conducted in mice suggest that AICAR might effectively reduce inflammation in colitis. It appears that AICAR assumes a central role in inhibiting immune responses in this context by reducing NF-kappaB activation in macrophages and curtailing the production of TH1- and TH17-type cytokines. This research holds promise for novel approaches to managing inflammatory conditions.

Research and the Heart

Inflammation plays a significant role in the development of heart disease, particularly in the progression of vascular conditions like atherosclerosis. The ability to manage inflammation holds the potential to mitigate the advancement of these diseases. Studies conducted on rabbit models of atherosclerosis have indicated that AICAR can effectively inhibit the proliferation of vascular smooth muscle cells. This is a critical factor not only in cardiovascular disease but also in the long-term durability of cardiac stents. By controlling vascular inflammation, we could potentially reduce both immediate and enduring complications associated with stent placement, all without the need for medications that elevate the risk of bleeding.

Furthermore, research suggests that the activation of AMPK can suppress specific immune responses that contribute to the development of atherosclerosis. The accumulation of LDL, commonly known as “bad cholesterol,” triggers the proliferation of macrophages, a process integral to the formation of plaques that can eventually lead to heart attacks. Managing these immune responses through AMPK activation holds promise in preventing atherosclerosis-related complications.

Research and Fertility

A substantial body of research has centered on AICAR’s potential to enhance sperm motility, energy metabolism, and fertilization capabilities. Studies conducted in various animals, including cats, goats, and chickens, suggest that AMPK activators like AICAR can boost sperm motility by improving energy metabolism.

AICAR is known for its minimal side effects and excellent subcutaneous bioavailability in mice. However, it’s important to note that the dosage per kilogram in mice does not directly translate to human dosages. It’s crucial to understand that AICAR available at Peptide Sciences is strictly intended for educational and scientific research purposes and should not be used for human consumption. Therefore, if you are not a licensed researcher, it is advisable not to purchase AICAR.

Article Author

The above literature was researched, edited and organized by Dr. Logan, M.D. Dr. Logan holds a doctorate degree from Case Western Reserve University School of Medicine and a B.S. in molecular biology.

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The product information featured on this website pertains exclusively to in-vitro studies. In-vitro studies, also known as ‘in glass’ studies, are conducted outside of living organisms. It’s important to emphasize that these products do not constitute medicines or drugs and have not received FDA approval for the prevention, treatment, or cure of any medical conditions, ailments, or diseases. It is crucial to note that the introduction of these products into the bodies of humans or animals is strictly prohibited by law.