GW501516 – Cardarine

GW501516 Historical Development:

The journey of GW501516 commenced in the late 1990s when it was jointly developed by Ligand Pharmaceuticals and GlaxoSmithKline. The impetus behind the development was to address metabolic disorders such as obesity and type 2 diabetes. As a PPARδ agonist, GW501516 garnered attention for its ability to modulate fatty acid metabolism and energy homeostasis.

GW501516 Chemical Structure:

The structure of Cardarine is comprised of a thiazole ring bonded to a methylsulfanyl group, which is attached to a 2-methylphenoxy moiety. Additionally, there is a trifluoromethyl-substituted phenyl group attached to the thiazole. This combination of functional groups is orchestrated to confer specific interactions with the PPARδ receptor.

Properties and Mechanism of Action:

As an agonist of PPARδ, GW501516 binds to the receptor, inducing a conformational change that enables interaction with specific coactivators. This interaction leads to the transcription of genes involved in energy expenditure, fatty acid oxidation, and insulin sensitivity.

In some studies, GW501516 has been found to increase the oxidation of fatty acids and facilitate a shift in the substrate utilization from glucose to fatty acids. This property has led to the notion that GW501516 can be used to enhance endurance.

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