AICAR

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Product Usage: This PRODUCTS ARE INTENDED FOR 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 mislabeled as a drug, food, or cosmetic.

AICAR

The Endurance Enhancer

Boost Endurance: Unlock the Performance Benefits of AICAR

AICAR, or 5-Aminoimidazole-4-carboxamide ribonucleotide, is a compound with a significant role in cellular metabolism. It functions primarily as an intermediate in the generation of inosine monophosphate, a molecule important for the synthesis of nucleotides, which are the building blocks of DNA and RNA.

In scientific and medical research, AICAR is most noted for its ability to stimulate AMP-activated protein kinase (AMPK). This enzyme plays a crucial role in energy regulation within cells. When activated, AMPK helps cells cope with energy stress by enhancing pathways that generate energy and turning off pathways that consume energy for growth and proliferation.

Beyond its metabolic functions, AICAR has attracted attention in sports and medicine for its potential to mimic the effects of exercise, thus improving endurance and potentially benefiting conditions like diabetes and cardiovascular diseases by improving metabolic

efficiency.

Potential Benefits Under Research

  • Enhancing Exercise Performance and Endurance: Stimulates metabolic pathways similar to those activated by physical exercise, potentially improving physical endurance and performance.
  • Metabolic Regulation and Insulin Resistance: Activates AMPK, which can enhance cellular energy production, increase glucose uptake, and improve insulin sensitivity, offering potential benefits in the treatment of type 2 diabetes and metabolic syndrome.
  • Cardiovascular Health: May protect against ischemia and improve heart function, which is beneficial for cardiovascular health.
  • Weight Management: By improving metabolic efficiency, AICAR could help in managing obesity and related metabolic disorders.
  • Anti-Aging Effects: Potential anti-aging benefits due to its role in enhancing cellular energy and overall cellular health.
  • Cancer Research: Research is exploring AICAR’s ability to inhibit cancer cell growth and proliferation, possibly through its effects on cellular metabolism and energy regulation.
  • Anti-inflammatory Properties: AICAR may have anti-inflammatory effects, which could be beneficial in treating chronic inflammatory diseases.
  • Fertility: Preliminary studies suggest that AICAR could impact fertility through its influence on cellular energy levels and metabolic pathways, although this area requires further research.

Dosing Protocol for Research Purposes

The specific dosage and administration protocols for AICAR in research can vary based on the experimental design, species being studied, and the objectives of the research. General guidelines include:

  • Dosage: Typical research dosages for animal studies range from 0.5 to 1.5 mg/kg per day. Human equivalent doses need careful adjustment and scaling based on body surface area.
  • Administration: AICAR can be administered via intraperitoneal, intravenous, or subcutaneous injections. The route of administration depends on the study’s goals and the species being tested.
  • Duration: The duration of administration can vary widely, from acute single doses to chronic administration over several weeks or months, depending on the research focus.

Overview

AICAR, short for 5-aminoimidazole-4-carboxamide ribonucleoside, is short peptide that plays a role in energy homeostasis and a number of metabolic pathways. AICAR plays a role in the regulation of insulin receptors and how muscle cells function with regards to insulin. AICAR is under active investigation for its cancer-fighting properties and for its ability to protect heart/cardiovascular tissue. AICAR is an AMP kinase (AMPK) activator.

AICAR is the activated form of naturally occurring acadesine, which is currently used in the treatment of acute lymphblastic leukemia. Research shows that acadesine, like AICAR, has anti-cancer properties. It has also been found to play a role in inhibiting platelet function and thus in the prevention of the early stages of blood clotting.

Structure

Sequence: 5-aminoimidazole-4-carboxamide ribonucleoside

Molecular Formula: C9H1sN40sP

Molecular Weight: 338.213 g/mol

PubChem CID: 65110

CAS Number: 3031-94-5

Synonyms: AICA ribonucleotide, z-nucleotide

Most Recent Research

Recent studies on AICAR have focused on its effects on glycogen metabolism in skeletal muscle. One key finding is that short-term AICAR treatment alters the activities of enzymes directly involved in glycogen metabolism, leading to increased glycogen deposition in rat skeletal muscle. This effect seems to be secondary to AICAR’s well-known action on stimulating glucose transport rather than direct effects on glycogen synthase and glycogen phosphorylase. The study suggests that increased glucose uptake by skeletal muscle, indirectly supported by a marked reduction in blood glucose and corresponding increases in muscle glucose-6-phosphate (G-6-P) and blood lactate concentrations, could explain the observed increase in muscle glycogen after AICAR treatment.

Another important aspect of AICAR’s action is its role in activating AMP-activated protein kinase (AMPK), which is crucial for cellular energy homeostasis. AICAR’s ability to stimulate AMPK activity leads to increased fat and carbohydrate catabolism, helping to maintain cellular ATP levels during energy-demanding conditions. The specific pathways through which AICAR influences muscle glycogen content involve complex interactions with various metabolic processes, including glycogen synthesis and breakdown, glucose uptake, and glycolytic flux​.

Source: American Diabetes Association

Reference Link 1

Reference Link 2

Additional Research

AICAR and Insulin Resistance 

Research in mice shows that AICAR, even at low doses, reduces inflammation in adipose tissue. Inflammation in fat is associated with increased insulin resistance and reducing inflammation leads to improved glucose homeostasis and increased insulin sensitivity even without any changes in body weight. It appears that AICAR has several pathways through which it affects inflammation in adipose tissue, with at least one of those pathways involving SIRTl and macrophages.

The impact of AICAR on adipose inflammation is not unexpected. AMPK has been found to attenuate inflammatory responses in metabolic disorders in both healthy and diabetic mice. In research in mice, AMPK activation, as is caused by AICAR, was found to improve insulin sensitivity, energy homeostasis, lipid metabolism, and inflammatory markers.

Exercise increases the number of GLUT-4 insulin receptors that are present on the surface of muscle cells. It is one of the most effective means of boosting glucose uptake by muscle cells and effectively reduces both glucose levels and insulin resistance. It turns out that AICAR mimics the effects of exercise very precisely and that repeated administration of AICAR has effects similar to long-term exercise.

AICAR and Cancer Research
AMPK plays a complex role in the growth and metastasis of cancer, both slowing and accelerating the growth of tumors under varying circumstances. Overall, research indicates that prolonged activation of the enzyme eventually leads to cancer cell death 

by slowing cancer cell metabolism and making cancer cells more susceptible to environmental

insults. This has been demonstrated both in cell culture and in rats]. Scientists are investigating the ability of AICAR to work in tandem with other chemotherapeutic agents to boost effectiveness. The thought is that AICAR might

  • reduce side effects,
  • allow for lower dosing of chemotherapeutic drugs, and
  • improve outcomes in chemo-resistant tumors.

AICAR inhibits clonal growth of glioma (C6) and prostate cells.
Source: Journal of Biological Chemistry

Research in thyroid cancer cells indicates that AICAR may also operate by causing apoptosis (programmed cell death). It appears that this activity is mediated through the induction of p21 accumulation and the eventual activation of caspase 3. The overall effect is inhibition of cancer cell proliferation and survival.

AMPK activators, like AICAR, influence a number of pathways that can impact cancer growth.
Source: PubMed

AICAR Anti-inflammatory Properties

AMPK activators have been shown to play an important role in inflammation at the cellular level. Research into metformin, a common and long-used diabetes medication, indicates that at least part of the reason the drug is effective is that it reduces inflammation and boosts the function of the pancreas. AICAR has a similar effects, playing a protective role in inflammatory conditions like acute lung injury, asthma, colitis, atherosclerosis, and hepatitis .

There is ongoing research into the use of AICAR to mediate the effects of auto-immune diseases and other inflammatory conditions. For instance, studies in mice indicate that ACIAR may be effective in reducing inflammation in colitis. It appears that AICAR acts as a central inhibitor of immune responses in this setting by reducing NF-kappaB activation in macrophages as well as TH1- and TH17-type cytokines.

AICAR Research and the Heart

Much of heart disease is related to inflammation. The ability to control inflammation could reduce the progression of vascular disease, including atherosclerosis. Research in rabbit models of atherosclerosis indicated that AICAR suppression vascular smooth muscle proliferation. This is not only an important component of cardiovascular disease, but is also one of the reasons that cardiac stents fail over time. Controlling vascular inflammation could reduce both short-term and long-term complications of stent placement without the need for drugs that increase the risk of bleeding.

Research also suggests that AMPK activation can suppression certain immune responses that lead to atherosclerosis. The buildup of LDL, often referred to as “bad cholesterol,” leads to macrophage proliferation. This process is integral to the formation of plaques that can eventually lead to heart attack. Anything that can mitigate this proliferation has the potential to reduce heart disease and even heart attack prevalence.

AICAR Research and Fertility

A great deal of AICAR research has revolved around the ability of the peptide to improve sperm motility, energy metabolism, and fertilizing ability. Research in both cats, goats, and chickens indicates that AMPK activators like AICAR can improve sperm motility by improving energy metabolism. It appears that AICAR regulates the activity of energetic enzymes in spermatozoa and therefore impacts overall fertilizing ability.

AICAR exhibits minimal side effects, low oral and excellent subcutaneous bioavailability in mice. Per kg dosage in mice does not scale to humans. 

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.

Scientific Journal Author

SRencer Gaskin, M.D., Ph.D. is an American Board of Internal Medicine certified cardiologist and medical practitioner. His expertise of Internal medicine and cardiology sources from UT Southwestern Cardiology, Washington University lnterventional Cardiology, and the Mid America Heart Institute. Dr. Gaskin led a study that examined the prevention of Postischemic Leukocyte Rolling and Adhesion via preconditioning with AICAR.

Spencer Gaskin, M.D., Ph.D. is being referenced as one of the leading scientists involved in the research and development of AICAR. In no way is this doctor/scientist endorsing or advocating the purchase, sale, or use of this product for any reason. There is no affiliation or relationship, implied or otherwise, between Guide to Peptide and this doctor. The purpose of citing the doctor is to acknowledge, recognize, and credit the exhaustive research and development efforts conducted by the scientists studying this peptide. Dr. Gaskin is listed in [14] under the referenced citations.

Referenced Citations

  1. Z. Yang et al., “The full capacity of AICAR to reduce obesity-induced inflammation and insulin resistance requires myeloid SIRTl,” PloS One, vol. 7, no. 11, p. e49935, 2012.
  2. K. Pan et al., “AMPK activation attenuates inflammatory response to reduce ambient PM2.5-induced metabolic disorders in healthy. and diabetic mice,” Ecotoxicol. Environ. Saf., vol. 179, pp. 290-300, Sep. 2019.
  3. N. Jessen, R. Paid, E. S. Buhl, L. S. Jensen, 0. Schmitz, and S. Lund, “Effects of AICAR and exercise on insulin-stimulated glucose uptake, signaling, and GLUT-4 content in rat muscles,” J. Appl. Physiol. Bethesda Md 1985,vol.94, no.4, pp. 1373-1379,Apr. 2003.
  4. J. Zhuge, “Overexpression of CYP2El induces HeRG2 cells death by the AMP kinase activator 5′-aminoimidazole-4- carboxamide-1-beta-D-ribofuranoside.{AICAR).,” Cell Biol. Toxicol., vol. 25, no. 3, pp. 253-263, Jun.2009.
  5. R. Rattan, S. Giri, A. K. Singh, and I. Singh, “5-Aminoimidazole-4-carboxamide-1-beta-D­ribofuranoside inhibits cancer cell proliferation in vitro and in vivo via AMP-activated protein kinase/ J. Biol. Chem., vol. 280, no. 47, pp. 39582-39593, Nov. 2005.
  6. M. M. H. Yung, H. Y. S. Ngan, and D. W. Chan, ‘Targeting AMPK signaling in combating ovarian cancers: opportunities and challenges,” Acta Biochim. Biophys.  Sin, vol. 48, no. 4, pp. 301-317, Apr. 2016.
  7. W. G. Kim, H.-J. Choi, T. Y. Kim, Y. K. Shong, and W. B. Kim, “The effect of 5-aminoimidazole-4-carboxamide­ribonucleoside was mediated by_p38 mitogen activated protein kinase signaling pathway in FRO thyroid cancer cells,” Korean J. Intern. Med., vol. 29, no. 4, pp. 474-481, Jul. 2014.
  8. X.-W. Peng, H.-H. Zhou, J. Dai, and L. Zhang, “[Advances on the anti-inflammatory and protective effect of AMPK activators],” Sheng Li Xue Bao, vol. 71, no. 2, pp. 319-326, Apr. 2019.
  9. A. Bai et al., “Novel anti-inflammatory action of 5-aminoimidazole-4-carboxamide ribonucleoside with protective effect in dextran sulfate sodium-induced acute and chronic colitis,” J. Pharmacol. Exp. Ther., vol. 333, no.3, pp. 717-725,Jun. 2010.
  10. M. lgata et al., “Adenosine monophosphate­ activated protein kinase suppresses vascular smooth muscle cell proliferation through the inhibition of cell cycle progression,” Circ. Res., vol. 97, no. 8, pp. 837-844, Oct. 2005.
  11. M. Sakai, S. Kobori, A. Miyazaki, and S. Horiuchi, “Macrophage proliferation in atherosclerosis,” Curr. Opin. Lipidol., vol. 11, no. 5, pp. 503-509, Oct. 2000.
  12. P. Thuwanut, P. Comizzoli, K. Pruksananonda, K. Chatdarong, and N. Songsasen, “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., May 2019.
  13. Z. Zhu et al., “5′-AMP-Activated Protein Kinase Regulates Goat Sperm Functions via Energy Metabolism In Vitro,” Cell. Physiol. Biochem. Int. J. Exp. Cell. Physiol. Biochem. Pharmacol., vol. 47, no. 6, pp. 2420-2431, 2018.
  14. F. Spencer Gaskin, Kazuhiro Kamada, Mozow Yusof, William Durante, Garrett Gross & Ronald J. Korthuis (2009) AICAR Preconditioning Prevents Postischemic Leukocyte Rolling and Adhesion: Role of KATP Channels and Heme  Oxygenase, Microcirculation, 16:2, 167- 176, DOI: 10.1080/10739680802355897
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ALL ARTICLES AND PRODUCT INFORMATION PROVIDED ON THIS WEBSITE ARE FOR INFORMATIONAL AND EDUCATIONAL PURPOSES ONLY.
The products offered on this website are furnished for in-vitro studies only. In-vitro studies {Latin: in glass) are performed outside of the body. These products are not medicines or drugs and have not been approved by the FDA to prevent, treat or cure any medical condition, ailment or disease. Bodily introduction of any kind into humans or animals is strictly forbidden by law.

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