GW7647

SKU: orb1219734

Description

GW7647 is a potent agonist of PPARα (EC50s: 6 nM, 1.1 μM, and 6.2 μM for human PPARα, PPARγ, and PPARδ, respectively).GW7647 (50 nM) stimulates the PI3K phosphorylation followed by the Akt (Ser473) phosphorylation, which causes NOS1 phosphorylation increased the amounts of NO released in the stripped antral mucosa. GW7647 (50 nM) enhances the initial phase of Ca2+-regulated exocytotic events stimulated by ACh in antral mucous cells, but GW7647 alone does not evoke any exocytotic event. GW7647 (1 μM) induces a significant increase of PDZK1 protein expression to 129.7 ± 6.5% of vehicle treated control in Caco2BBE cells in the absence and presence of IL-1β. GW7647 also decreases the IL-1β-mediated decrease in PDZK1 expression. GW7647 plus ACh stimulates the effects of wortmannin (50 nM) and AKT-inh (100 nM) on the exocytotic events in antral mucous cells. GW 7647 (100 nM) decreases the AQP9 protein abundance by 43%, but it displays not significant effect at 10 and 1,000 nM in WIF-B9 hepatocytes. GW 7647 (100 nM) reduces a 24% reduction in AQP9 protein abundance in HepG2 cells, however, it does not significantly enhance the protein abundance of L-FABP in HepG2 hepatocytes[3].GW7647 (3 mg/kg per day) does not avoid the development of cardiac hypertrophy. It prevents the decline in left ventricular ejection fraction in vivo.

Key Properties

• CAS Number: 265129-71-3
• MW: 502.75
• Purity: >98% (HPLC)
• Formula: C₂₉H₄₆N₂O₃S
• SMILES: CC(C)(Sc1ccc(CCN(CCCCC2CCCCC2)C(=O)NC2CCCCC2)cc1)C(O)=O
• Target: PPAR
• Solubility: DMSO:60 mg/mL (119.34 mM)

Bioactivity

• In Vivo:
  GW7647 (3 mg/kg per day) does not prevent the development of cardiac hypertrophy, but it prevents the decline in left ventricular ejection fraction In vivo.
• In Vitro:
  GW7647 (1 μM) causes a significant increase of PDZK1 protein expression to 129.7 ± 6.5% of vehicle treated control in Caco2BBE cells in the absence and presence of IL-1β. GW7647 also attenuates the IL-1β-mediated decrease in PDZK1 expression. GW7647 (50 nM) stimulates the PI3K phosphorylation followed by the Akt (Ser473) phosphorylation, which induces NOS1 phosphorylation increased the amounts of NO released in the stripped antral mucosa. GW7647 (50 nM) enhances the initial phase of Ca2+-regulated exocytotic events stimulated by ACh in antral mucous cells, but GW7647 alone does not evoke any exocytotic event. GW7647 plus ACh stimulates the effects of wortmannin (50 nM) and AKT-inh (100 nM) on the exocytotic events in antral mucous cells. GW 7647 (100 nM) reduces the AQP9 protein abundance by 43%, but it shows not significant effect at 10 and 1, 000 nM in WIF-B9 hepatocytes. GW 7647 (100 nM) causes a 24% reduction in AQP9 protein abundance in HepG2 cells, however, it does not significantly increase the protein abundance of L-FABP in HepG2 hepatocytes.

Storage & Handling

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

Quick Database Links

Gene Symbol

PPAR