Fezagepras

SKU: orb1309110

Description

Fezagepras (Setogepram) is an orally bioavailable small molecule that acts as a GPR40 agonist and a GPR84 antagonist/inverse agonist. It exhibits anti-inflammatory, anti-fibrotic, and anti-proliferative properties, making it a useful research tool for studying metabolic and inflammatory diseases in both in vitro and in vivo models.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1002101-19-0
• MW: 206.28
• Purity: 99.38% (May vary between batches)
• Formula: C₁₃H₁₈O₂
• SMILES: CCCCCc1cccc(CC(O)=O)c1
• Target: GPCR
• Solubility: DMSO:60 mg/mL (290.87 mM);10% DMSO+90% Saline:5 mg/mL (24.24 mM)

Bioactivity

• In Vivo:
  In type 2 diabetes eNOS-/-db/db mice, Setogepram (PBI-4050; 100 mg/kg/day; gavage from 8-20 weeks of age) markedly decreases hyperglycemia and markedly improve glucose tolerance .
• In Vitro:
  TGF-β (10 ng/mL)-activated human hepatic stellate cells (HSCs) proliferation inhibited by Setogepram (PBI-4050; 500 μM; 24 hours). Setogepram (PBI-4050; 250 or 500 μM; 24hours) dose-dependently arrests HSCs at the G0/G1 phase without inducing apoptosis .

Storage & Handling

• Storage: Pure form: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Diabetes,Kidney,Renal,Pancreatic,Liver,Fibrosis,Nephrology, inhibit, PBI4050, PBI-4050, PBI 4050, Inhibitor, G protein coupled receptor 84, Free Fatty Acid Receptor, Fezagepras, FFAR, GPR40, GPR84, Setogepram

Compound Identifiers

PubChem CID

24749700