What Is AICAR 50MG?
AICAR stands for 5 aminoimidazole-4- carboxamide ribonucleotide. It is a synthetic analog of adenosine monophosphate that regulates the activity of AMP-dependent protein kinase (AMPK). It is under investigation for its effects on insulin resistance, cancer, weight loss and ischemic damage in cardiac myocytes. At Pinnacle Peptides, AICAR for sale is exclusively available for research and experimentation.
Structure Of AICAR 50MG
From Pubchem
IUPAC Name: 5-amino-1-[3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]imidazole-4-carboxamide
Synonyms: MFCD00869751, 37642-57-2
Molecular Formula: C9H14N4O5
Molecular Weight: 258.23 g/mol
CAS number: 37642-57-2
PubChem CID: 266934
Mechanism Of AICAR 50MG
AICAR is taken up by the cells and is phosphorylated to form ZMP (5-aminoimidazole-4-carboxamide ribonucleotide monophosphate). ZMP mimics the function of AMP, a naturally occurring compound that activates AMPK. This, in turn, leads to several downstream effects.
For a better understanding of AICAR, it is important to understand the role of AMPK in the body. It is a cellular energy sensor that is crucial in regulating energy balance. It gets activated in the presence of low energy levels and stimulates catabolic pathways for ATP generation. Further, it also inhibits energy-consuming pathways, such as fatty acid synthesis for the conservation of ATP.
Pre-Clinical/Clinical Research
1. Cardioprotection
Inflammation plays a significant role in the development of vascular diseases, such as atherosclerosis. One study in the rabbit model of atherosclerosis found that AICAR can inhibit smooth vascular proliferation. Excessive proliferation not only contributes to cardiovascular disease but is one of the major reasons for the failure of cardiac stents over time. Controlling the smooth vascular proliferation through a dependent pathway can improve response to stent and reduce complications without needing medications that increase bleeding risk [1].
Furthermore, activation of AMPK by AICAR can suppress immune reactions that contribute to the build-up of plaque. Preventing the formation of plaque in the coronary arteries can slow the progression of heart diseases [2]. AICAR can also improve scar formation and reduce adverse remodeling following myocardial infarction through AMPK signalling. This leads to the mobilization of mesenchymal stem cells (MSCs) that ultimately mature into myofibroblasts, resulting in the formation and stabilization of scars. Scar formation is important to replace the damaged necrotic heart tissues that maintain structural integrity and prevent the risk of rupture [3].
2. Insulin Sensitivity
Inflammation in adipocytes contributes to insulin resistance and poor blood glucose control. Research shows that AICAR has the ability to suppress inflammation in adipocytes that results in improved insulin sensitivity and glucose homeostasis. This was confirmed by a study in diabetic males, revealing that AICAR reduced the hepatic glucose uptake and lowered the blood glucose concentration [4].
Some studies indicate that the mechanism by which AICAR influences insulin response is similar to that of exercise, i.e., AMPK activation. The activation of AMPK has been shown to increase the expression of GLUT insulin receptors that mediate the uptake of glucose from the blood to the muscles. This results in the effective reduction of blood glucose levels and insulin resistance [5].
3. Cancer
AMPK regulates apoptosis and inhibits cell growth and proliferation [6]. Literature reveals that AICAR exhibits antitumour activity for different kinds of cancer. One study found that AICAR inhibited the growth of cancerous cells in prostate tissues. The effect of AICAR was found to be selective as it didn’t interfere with the growth of non-cancerous cells.
Furthermore, it enhanced the chemosensitivity of docetaxel in prostate cancerous tissues through the regulation of the AMPK/mTOR-dependent pathway [7]. Similarly, it has been shown to inhibit the growth of lung carcinoma and osteosarcoma [8, 9].
4. Obesity
Activation of AMPK influences the metabolic state in a healthier way. Research indicates that AICAR, being an activator of AMPK, might have the potential to treat obesity. One study in mice found that AICAR reduced the inflammation in adipocytes, hepatic stenosis and kidney disease. Further, it decreased the production of TNF-alpha and promoted the switching of M1 to M2 macrophage phenotype in tissue explants from obese human subjects. These findings suggest that it might also prevent/attenuate obesity-related complications [10].
5. Fertility
AICAR has also been extensively studied for its effect on sperm motility and energy metabolism. A study conducted on domestic cats found that AICAR can improve the motility and fertilizing ability of cryopreserved sperm [11]. Literature suggests that it might improve sperm motility by enhancing energy metabolism and regulating the activity of energetic enzymes in spermatozoa [12].
Summary
AICAR is a synthetic analog of adenosine monophosphate. It activates AMPK which is responsible for energy balance and homeostasis. AICAR has the potential to treat/ prevent vascular diseases and reduce the adverse remodeling following myocardial infarction. Further, it has been shown to improve insulin sensitivity, inhibit cancer growth and reduce obesity-related complications. It is classified as an investigational drug and hasn’t been approved by the FDA yet. We don’t support its unwarranted use and offer the option to purchase AICAR solely for research. Only buy AICAR if you are an authorized researcher.
References
- Igata, M., et al., Adenosine monophosphate-activated protein kinase suppresses vascular smooth muscle cell proliferation through the inhibition of cell cycle progression. Circ Res, 2005. 97(8): p. 837-44.
- Rosenfeld, M.E., Macrophage Proliferation in Atherosclerosis. Arteriosclerosis, Thrombosis, and Vascular Biology, 2014. 34(10): p. E21-e22.
- Cieslik, K.A., et al., AICAR-dependent AMPK activation improves scar formation in the aged heart in a murine model of reperfused myocardial infarction. J Mol Cell Cardiol, 2013. 63: p. 26-36.
- Boon, H., et al., Intravenous AICAR administration reduces hepatic glucose output and inhibits whole body lipolysis in type 2 diabetic patients. Diabetologia, 2008. 51(10): p. 1893-1900.
- Pold, R., et al., Long-Term AICAR Administration and Exercise Prevents Diabetes in ZDF Rats. Diabetes, 2005. 54(4): p. 928-934.
- Zhuge, J., Overexpression of CYP2E1 induces HepG2 cells death by the AMP kinase activator 5'-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside (AICAR). Cell Biol Toxicol, 2009. 25(3): p. 253-63.
- Su, C.C., et al., AICAR Induces Apoptosis and Inhibits Migration and Invasion in Prostate Cancer Cells Through an AMPK/mTOR-Dependent Pathway. Int J Mol Sci, 2019. 20(7).
- Aftab, F., et al., An intrinsic purine metabolite AICAR blocks lung tumour growth by targeting oncoprotein mucin 1. British Journal of Cancer, 2023. 128(9): p. 1647-1664.
- Morishita, M., et al., AICAR induces mitochondrial apoptosis in human osteosarcoma cells through an AMPK-dependent pathway. Int J Oncol, 2017. 50(1): p. 23-30.
- Börgeson, E., et al., AICAR ameliorates high-fat diet-associated pathophysiology in mouse and ex vivo models, independent of adiponectin. Diabetologia, 2017. 60(4): p. 729-739.
- Thuwanut, P., et al., Activation of adenosine monophosphate-activated protein kinase (AMPK) enhances energy metabolism, motility, and fertilizing ability of cryopreserved spermatozoa in domestic cat model. J Assist Reprod Genet, 2019. 36(7): p. 1401-1412.
- Zhu, Z., et al., 5'-AMP-Activated Protein Kinase Regulates Goat Sperm Functions via Energy Metabolism In Vitro. Cell Physiol Biochem, 2018. 47(6): p. 2420-2431.
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Got my Aicar in 3 days.My research began with this... will post results later
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