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GW-501516 (Cardarine), (10mg/capsule) 60 Capsules
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GW-501516 (Cardarine) is a synthetic agonist of peroxisome proliferator-activated receptor delta (PPARδ), a ligand-activated nuclear receptor that regulates transcriptional activity through interaction with specific DNA response elements. High-affinity binding to PPARδ induces receptor conformational changes that promote co-regulator recruitment, transcriptional complex formation, and downstream gene expression modulation. Research applications include PPARδ pharmacology, nuclear receptor signaling, transcriptional regulation, ligand-receptor interaction studies, structure-activity relationship investigations, and comparative analyses of PPAR family agonists.
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- For Laboratory Research Use Only
3D Molecular Structure
Drag to rotate · scroll to zoom| Chemical Formula | C21H18F3NO3S2 |
|---|---|
| Synonyms | Endurobol, GW501516, GW 501516, GW-501516, 2-[2-methyl-4-[[4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl]methylsulfanyl]phenoxy]acetic acid |
| Molar Mass | 453.50 g/mol |
| CAS Number | 317318-70-0 |
| PubChem CID | 9803963 |
| Total Compound Content | 600 mg (10 mg per capsule) |
How does GW-501516's PPARδ selectivity differ from PPARα and PPARγ agonists?
GW-501516 exhibits high selectivity for PPARδ relative to other members of the peroxisome proliferator-activated receptor family. This selectivity enables investigation of PPARδ-dependent transcriptional activity without the confounding receptor interactions associated with PPARα or PPARγ agonists. As a result, GW-501516 is frequently utilized in studies examining receptor subtype specificity, co-regulator recruitment, and ligand-dependent nuclear receptor signaling.
What is the mechanism of action of GW-501516 at the PPARδ receptor?
GW-501516 binds PPARδ with high affinity, promoting receptor activation, heterodimerization with retinoid X receptor (RXR), and recruitment of transcriptional co-regulators. This process facilitates transcriptional complex assembly and modulation of downstream gene expression. These characteristics make GW-501516 a valuable tool for investigating PPARδ signaling mechanisms, transcriptional regulation, and ligand-receptor interactions.
Why is GW-501516 commonly used as a reference compound in PPARδ research?
A: GW-501516 possesses a well-characterized pharmacological profile, high receptor selectivity, and extensive documentation within the scientific literature. These properties have established it as a widely used reference compound for studies involving PPARδ pharmacology, nuclear receptor signaling, transcriptional pathway characterization, structure-activity relationships, and comparative investigations of PPAR family agonists.
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