We are proud to offer GW-50156 in a bottle of 90 capsules with 10mg per capsule.
GW501516, commonly known as GW or Cardarine, is a synthetic peroxisome proliferator-activated receptor delta (PPARδ) agonist that has attracted attention for its potential benefits in enhancing physical performance and improving metabolism. Extensive research has been conducted to understand its mechanism of action, both in vitro and in vivo. This article aims to delve into the intricate workings of GW501516, exploring its therapeutic potential and shedding light on the experimental studies conducted to unravel its biological effects.
Structure and Properties of GW501516:
GW501516 is a synthetic compound with a chemical structure that mimics the structure of naturally occurring fatty acid derivatives. It is highly lipophilic, enabling efficient absorption and distribution throughout the body. GW501516 is classified as a selective PPARδ agonist, as it specifically targets and activates the PPARδ receptor.
Mechanism of Action:
GW501516 exerts its effects by selectively binding to and activating the PPARδ receptor. PPARδ is a transcription factor that plays a crucial role in regulating genes involved in energy metabolism, fatty acid oxidation, and inflammation. By activating PPARδ, GW501516 modulates various cellular pathways and biological processes . Here are the key mechanisms through which GW501516 operates:
a. Enhanced Fat Utilization:
GW501516 increases the expression of genes involved in fatty acid oxidation and energy metabolism. By activating PPARδ, it stimulates the breakdown of stored fats and promotes their utilization as an energy source. This mechanism leads to increased fat burning, improved endurance, and potential benefits in weight management .
b. Improved Insulin Sensitivity:
GW501516 has been shown to enhance insulin sensitivity. It increases the expression of genes involved in glucose uptake and utilization, facilitating better glucose regulation in cells. This improvement in insulin sensitivity can have positive implications for managing diabetes and metabolic disorders .
c. Anti-inflammatory Effects:
GW501516 exerts anti-inflammatory effects by inhibiting the activation of pro-inflammatory signaling pathways. It reduces the production of inflammatory mediators and modulates immune responses. This anti-inflammatory action may have implications for managing inflammatory conditions and promoting overall health .
d. Endurance and Performance Enhancement:
GW501516 has been associated with improved endurance and physical performance. It increases the expression of genes involved in mitochondrial biogenesis and oxygen utilization, leading to enhanced aerobic capacity. These effects make GW501516 of interest to athletes and individuals seeking to improve their exercise performance .
In Vitro Studies:
In vitro studies have provided valuable insights into the cellular mechanisms of GW501516. Researchers have utilized cell cultures to investigate its effects on various cell types, including muscle cells, adipocytes, and immune cells. These studies have highlighted the following findings:
a. Fatty Acid Oxidation and Energy Metabolism:
GW501516 has been shown to increase the expression of genes involved in fatty acid oxidation and energy metabolism in muscle cells and adipocytes. It enhances the activity of enzymes responsible for fat utilization and mitochondrial function, supporting its potential role in promoting fat burning and energy production.
b. Glucose Uptake and Insulin Sensitivity:
In vitro studies have demonstrated that GW501516 increases glucose uptake in muscle cells and improves insulin sensitivity. It enhances the translocation of glucose transporters to the cell membrane, promoting glucose uptake and utilization. These findings suggest its potential application in managing insulin resistance and related metabolic disorders .
In Vivo Studies:
In vivo studies have provided further evidence of GW501516’s potential benefits for endurance, metabolism, and overall health. These studies have been conducted in animal models, including rodents. Here are some key findings from in vivo studies:
a. Enhanced Endurance and Performance:
Animal studies have demonstrated that GW501516 administration leads to improved endurance and physical performance. It increases running capacity, time to exhaustion, and exercise tolerance. These effects are attributed to the enhancement of mitochondrial function, oxygen utilization, and fatty acid oxidation .
b. Metabolic Effects:
GW501516 has shown efficacy in improving lipid metabolism and reducing body fat in animal models. It promotes fat burning, increases energy expenditure, and improves lipid profiles. Animal studies have also indicated that GW501516 administration can improve insulin sensitivity and glucose homeostasis .
c. Cardioprotective Effects:
GW501516 has exhibited cardioprotective properties in animal models. It has been shown to improve cardiac function, reduce inflammation, and protect against ischemic injury. These findings suggest its potential application in cardiovascular health and the prevention of heart diseases .
Clinical Applications and Future Perspectives:
The potential applications of GW501516 in clinical settings and sports performance have garnered interest. While research is ongoing, preliminary clinical studies have shown promising results. GW501516 has demonstrated efficacy in improving endurance, promoting fat loss, and potentially addressing metabolic disorders.
In the future, further investigations are needed to determine the optimal dosage, treatment duration, and potential long-term effects of GW501516. Clinical trials are underway, aiming to evaluate its safety and efficacy in larger patient populations. Moreover, research is focused on exploring potential applications of GW501516 in conditions such as obesity, diabetes, and cardiovascular diseases.
GW501516, as a selective PPARδ agonist, holds promise in the fields of endurance enhancement, metabolism improvement, and overall health. In vitro and in vivo studies have elucidated its ability to activate PPARδ, leading to enhanced fat utilization, improved insulin sensitivity, anti-inflammatory effects, and performance enhancement. These findings provide a foundation for the potential applications of GW501516 in enhancing endurance, managing metabolic disorders, and promoting cardiovascular health. As research continues, GW501516 may emerge as a valuable tool in improving physical performance, metabolic health, and overall well-being. However, it is important to note that further research and regulatory considerations are necessary before its widespread use can be recommended.
WARNING: This product is intended for research purposes only. The research chemical designation allows the use of research chemicals strictly for in vitro testing and laboratory experimentation only. Bodily introduction of any kind into humans or animals is strictly forbidden by law.
- Gu L, Shi Y, Xu W, Ji Y. PPARβ/δ Agonist GW501516 Inhibits Tumorigenesis and Promotes Apoptosis of the Undifferentiated Nasopharyngeal Carcinoma C666-1 Cells by Regulating miR-206. Oncol Res. 2019;27(8):923-933. doi:10.3727/096504019X15518706875814
- Wang D, Fu L, Wei J, Xiong Y, DuBois RN. PPARδ Mediates the Effect of Dietary Fat in Promoting Colorectal Cancer Metastasis. Cancer Res. 2019;79(17):4480-4490. doi:10.1158/0008-5472.CAN-19-0384
- Kim WJ, Lee W, Jung Y, Jang HJ, Kim YK, Kim SN. PPARβ/δ agonist GW501516 inhibits TNFα-induced repression of adiponectin and insulin receptor in 3T3-L1 adipocytes. Biochem Biophys Res Commun. 2019;510(4):621-628. doi:10.1016/j.bbrc.2019.02.013
- Defaux A, Zurich MG, Braissant O, Honegger P, Monnet-Tschudi F. Effects of the PPAR-beta agonist GW501516 in an in vitro model of brain inflammation and antibody-induced demyelination. J Neuroinflammation. 2009;6:15. Published 2009 May 7. doi:10.1186/1742-2094-6-15
- Chen W, Gao R, Xie X, et al. A metabolomic study of the PPARδ agonist GW501516 for enhancing running endurance in Kunming mice. Sci Rep. 2015;5:9884. Published 2015 May 6. doi:10.1038/srep09884
- Shao Q, Xia J, Wu P, Ying J. Dexmedetomidine protects cardiac microvascular endothelial cells from the damage of ogd/r through regulation of the pparδ-mediated autophagy. Microcirculation. 2021;28(4):e12675. doi:10.1111/micc.12675
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