AICAR is believed to regulate metabolism and lipid profile. This comprehensive AICAR guide will tell you everything you need to know about AICAR and how it helps with metabolism.
In this blog, we’ll discuss what AICAR is and how it works. Next, we’ll explain its general benefits and side effects, before revealing the optimal AICAR dose.
What is AICAR?
AICAR (5-Aminoimidazole-4-carboxamide ribonucleoside) is an analog of AMP that stimulates the activity of AMP-activated protein kinase (APMK). AMPK is an enzyme found in various body cells. Its activation increases the availability of energy throughout the body. [1]
What Does AICAR Do?
AICAR regulates metabolism. When AICAR is introduced to cells expressing AMPK it increases AMP levels and activates AMPK which boosts energy-conserving processes.
This process suppresses the enzymes involved in lipogenesis and leads to the inhibition of fatty acid and cholesterol synthesis. At the same time, the AICAR boots fatty acid oxidation in the liver and skeletal muscle to promote the breakdown of fat for energy.
AICAR has also shown promise as a potential treatment for type 2 diabetes. A human trial involving patients with this condition reported reduced glucose production after AICAR treatment. The patients also experienced an improvement in their glucoregulation.
In preclinical studies, AICAR has shown promise as an anabolic agent. It has been reported that AICAR may stimulate muscle fiber activity, which is a precursor to muscle growth.
AICAR was initially investigated as an agent to preserve blood flow to the heart during surgery. Later, human trials explored whether it could treat cardiac ischemia after a heart attack. In these trials, AICAR proved to be effective at high doses with only mild side effects. [2]
How Does AICAR Work?
AICAR has different working mechanisms for different biological processes. Below we have described how AICAR works.
Increases Nitric Oxide Production
Nitric oxide helps blood vessels expand to promote proper blood flow. It can also provide various health benefits, such as better brain function, lower blood pressure, and improved exercise performance. Aside from that, it helps with penile erection. [3]
Increases ATP levels
In isolated human endothelial cells, AICAR treatment increased fatty acid and glucose oxidation, causing an increase in ATP production. Increased ATP levels help reduce fatigue, and boost strength and endurance.
Activates Glycogen Phosphorylase
AICAR activates glycogen phosphorylase and stimulates myocardial glycogenolysis in skeletal muscle cells. Both these processes help break down glycogen, a carbohydrate, into glucose to provide immediate energy.
Potential benefits of AICAR:
AICAR reportedly has various benefits including:
May Help with Type 2 Diabetes
In a clinical study of patients with type 2 diabetes, AICAR treatment (45 mg/kg/hr) produced a significant decrease in glucose production. The AMPK activator also improves glucoregulation, which is crucial for normal blood glucose levels in your body. [4]
Has anti-inflammatory properties
In various preclinical studies, AICAR has demonstrated a protective role in inflammatory conditions like atherosclerosis, lung injury, colitis, and hepatitis.
A cell-based study reported that AICAR reduced the replication of the hepatitis C virus in the treated cells. Another preclinical study found that this AMPK activator may ameliorate ischemia-reperfusion injury in kidneys.
May Protect Heart Health
As noted above, AICAR has been clinically used to prevent and treat cardiac ischemic injury (injury arising from reduced blood flow) after a heart attack.
In addition to the above effect, AICAR has demonstrated the ability to:
- Ameliorate cardiac dysfunction
- Counteract cardiac hypertrophy
- Ameliorate cardiac atrophy
May have the Potential to Fight Cancer
A cell-based study showed that AICAR induces apoptosis (cell death) and inhibits migration and invasion in prostate cancer cells. In addition to these effects, AICAR-treated prostate cancer cells exhibited increased chemosensitivity to docetaxel, an anti-cancer chemotherapy drug. [5]
Another study revealed three different ways AICAR may exhibit its anti-cancer effects. These include stimulation of the mitochondrial apoptotic pathway, reduction of Akt phosphorylation, and the activation of cell death by different metabolic pathways.
Potential Side Effects of AICAR
One of the major side effects of AICAR is that if AMPK activation exceeds the required level, this could lead to serious consequences. Moreover, it is said that if it gets activated in the wrong tissue cells it may cause:
- Neurodegeneration Problems [6]
- Preventing cells from dividing [6]
- Metabolic Disorders [6]
The accumulation of naturally occurring AICAR in the body has been associated with metabolic disorders in humans. [6]
Recommended AICAR Dosage
An initial 10 – 15 dosage will be good to check how your body responds to it.
There’s a consensus among AICAR users that the optimal dosage range lies between 10 mg and 50 mg, with the maximum dose mostly preferred by users with prior experience with performance enhancers.
Remember AICAR has very low bioavailability when taken orally (less than 5%). It’s suggested that this AMPK activator be administered via subcutaneous injections.
Where to buy AICAR?
If you are looking for a high-quality AICAR product, you can buy it from one of the following vendors:
| Vendors | Rating | Buying Link | Verdict |
| PureRawz | 4.9/5 | Buy AICAR from PureRawz | High-quality, trusted vendor |
| Behemoth Labz | 4.7/5 | Buy AICAR Peptide from Behemoth Labz | Reputable source, with great reviews |
| RCDBio | 4.7/5 | Visit RCDBio.co | Pure form, excellent reputation |
| Iron Mountain Labz | 4.6/5 | Buy AICAR from Iron Mountain Labz | Reliable vendor, consistent quality |
Winding up:
AICAR activates AMPK, which can help bodybuilders by increasing available energy and promoting fat loss while preserving muscle mass. Aside from that, it has demonstrated significant efficacy in type-2 diabetes trials.
References
- Rana, S., Blowers, E. C., & Natarajan, A. (2014). Small Molecule Adenosine 5′-Monophosphate Activated Protein Kinase (AMPK) Modulators and Human Diseases. Journal of Medicinal Chemistry, 58(1), 2–29. https://doi.org/10.1021/jm401994c
- Ewart, M.-A., & Kennedy, S. (2012). Diabetic Cardiovascular Disease – AMP-Activated Protein Kinase (AMPK) as a Therapeutic Target. Cardiovascular & Hematological Agents in Medicinal Chemistry, 10(3), 190–211. https://doi.org/10.2174/187152512802651015
- Daignan-Fornier, B., & Pinson, B. (2012). 5-Aminoimidazole-4-carboxamide-1-beta-D-ribofuranosyl 5’-Monophosphate (AICAR), a Highly Conserved Purine Intermediate with Multiple Effects. Metabolites, 2(2), 292–302. https://doi.org/10.3390/metabo2020292
- Nigro, E., Scudiero, O., Monaco, M. L., Palmieri, A., Mazzarella, G., Costagliola, C., Bianco, A., & Daniele, A. (2014). New Insight into Adiponectin Role in Obesity and Obesity-Related Diseases. BioMed Research International, 2014, 1–14. https://doi.org/10.1155/2014/658913
- Xiang, X., Saha, A. K., Wen, R., Ruderman, N. B., & Luo, Z. (2004). AMP-activated protein kinase activators can inhibit the growth of prostate cancer cells by multiple mechanisms. Biochemical and Biophysical Research Communications, 321(1), 161–167. https://doi.org/10.1016/j.bbrc.2004.06.133
- Perishable. (2019, November 14). What Athletes Should Know About AICAR and Others | USADA. https://www.usada.org/spirit-of-sport/education/aicar-and-other-prohibited-amp-activated-protein-kinase-activators/
