GW-501516

SKU: orb1301031

Description

GW 501516 (Endurobol) is a potent and selective PPARβ/δ agonist with an EC50 of 1 nM, exhibiting 1000-fold selectivity over hPPARα/γ. It is widely used in metabolic, muscle physiology, and endurance research, with applications in both in vitro cell-based assays and in vivo animal studies.

Research Area

Stem Cell & Developmental Biology

Key Properties

• CAS Number: 317318-70-0
• MW: 453.50
• Purity: >98%
• Formula: C₂₁H₁₈F₃NO₃S₂
• SMILES: C(SC1=CC(C)=C(OCC(O)=O)C=C1)C=2SC(=NC2C)C3=CC=C(C(F)(F)F)C=C3
• Target: Transcription factor
• Solubility: Soluble in DMSO (up to 40 mg/ml) or in Ethanol (up to 20 mg/ml)

Bioactivity

• Target IC50:
  PPARδ:1 nM(Ki)
• In Vivo:
  GW 501516 adversely affects bone formation, resulting in reduced bone mineral density (BMD) and compromised bone integrity in ovariectomized (OVX) rats. Additionally, it mitigates interstitial inflammation and damage to proximal tubular cells in a mouse model of protein-overload nephropathy. Furthermore, treatment with GW 501516 improves running endurance and increases the number of succinate dehydrogenase (SDH)-positive muscle fibers in both conditioned and unconditioned mice.
• In Vitro:
  GW 501516 is the most potent and selective PPARδ agonist, with an EC50 of 1.1 nM against PPARα and 1000-fold selectivity over other human subtypes, PPARα and -γ. It exhibits anti-inflammatory effects in mouse cultured proximal tubular (mProx) cells, inhibiting palmitate- and TNFα-induced increases in MCP-1 mRNA expression in a dose-dependent manner.
• Cell Research:
  GW 501516 is dissolved in DMSO. Cells are starved by incubation in 0.2% FCS DMEM for 9 h, then pre-incubated with GW 501516, at a final concentration of 2.5 and 5 μM, or 0.05% DMSO as control for 3 hours, followed by stimulation with 150 μM palmitate bound to 8.0% BSA for 12 h.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PPAR, PPARδ, Peroxisome proliferator-activated receptors, Autophagy, Cardarine, GW1516, GW-1516, GW 1516, GW 501516, GW501516, GW-501516, GSK 516, GSK516, GSK-516, Endurobol, inhibit, Inhibitor

Compound Identifiers

PubChem CID

9803963