Name | Fezagepras |
Description | Fezagepras (Setogepram) is an orally active GPR40 agonist and is an antagonist or inverse agonist of GPR84 with anti-inflammatory, anti-fibrotic, and anti-proliferative actions. |
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 [2]. |
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 [1]. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice./Shipping at ambient temperature. |
Solubility Information | DMSO : 60 mg/mL (290.87 mM), Sonication is recommended.
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Keywords | PBI4050 | PBI 4050 | Inhibitor | inhibit | GPR84 | GPR40 | G protein coupled receptor 84 | Free Fatty Acid Receptor | FFAR | Fezagepras | Diabetes,Kidney,Renal,Pancreatic,Liver,Fibrosis,Nephrology |
Inhibitors Related | Vincamine | Monomethyl fumarate | Questiomycin A | 3-Hydroxyoctanoic Acid | Azathioprine | CRTh2 antagonist 2 | Fezagepras sodium | Benzyl nicotinate | TUG-1375 | CAY10595 | Timapiprant | NF-56-EJ40 |
Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | NO PAINS Compound Library | Immunology/Inflammation Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |