GW 501516

SKU: orb1225321

Description

A potent and subtype-selective PPARδ agonist with Ki of 1.1 nM in human PPARδ binding assay; displays >1,000-fold selectivity over other PPAR subtypes; increases expression of the reverse cholesterol transporter ATP-binding cassette A1 and induces apolipoprotein A1-specific cholesterol efflux in macrophages, fibroblasts, and intestinal cells.Dyslipidemia Phase 2 Discontinued(In Vitro):GW 501516 is shown to be the most potent and selective PPARδ agonists known with an EC50 of 1.1 nM against PPARδ and 1000-fold selectivity over the other human subtypes, PPARα and-γ. GW 501516 exerts anti-inflammatory effects in mouse cultured proximal tubular (mProx) cells. GW 501516 inhibits palmitate- and TNFα-induced increases in MCP-1 mRNA expression in a dose-dependent manner.\n(In Vivo):GW 501516 causes impaired bone formation, leading to decreased BMD and deterioration of bone properties in OVX rats. GW 501516 attenuates interstitial inflammation and proximal tubular cell damage in a protein-overload mouse nephropathy model. GW 501516 treatment enhances running endurance and the proportion of succinate dehydrogenase (SDH)-positive muscle fibres in both trained and untrained mice.

Key Properties

• CAS Number: 317318-70-0
• MW: 453.4977
• Purity: >98% (HPLC)
• Formula: C₂₁H₁₈F₃NO₃S₂
• SMILES: O=C(O)COC1=CC=C(SCC2=C(C)N=C(C3=CC=C(C(F)(F)F)C=C3)S2)C=C1C
• Target: PPAR
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  GW 501516 causes impaired bone formation, leading to decreased BMD and deterioration of bone properties in OVX rats. GW 501516 attenuates interstitial inflammation and proximal tubular cell damage in a protein-overload mouse nephropathy model. GW 501516 treatment enhances running endurance and the proportion of succinate dehydrogenase (SDH)-positive muscle fibres in both trained and untrained mice.
• In Vitro:
  GW 501516 is shown to be the most potent and selective PPARδ agonists known with an EC50 of 1.1 nM against PPARδ and 1000-fold selectivity over the other human subtypes, PPARα and-γ. GW 501516 exerts anti-inflammatory effects in mouse cultured proximal tubular (mProx) cells. GW 501516 inhibits palmitate- and TNFα-induced increases in MCP-1 mRNA expression in a dose-dependent manner.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GW 1516 | GSK-516 | GW-501516

Quick Database Links

Gene Symbol

PPAR