Fezagepras_product_DataBase

Bioactivity	Fezagepras (Setogepram) acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84[1]. Fezagepras decreases renal, liver and pancreatic fibrosis[1][2]. Fezagepras exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions[2].
Target	GPR40, GPR84
Invitro	Fezagepras (500 µM; 24 hours) inhibits TGF-β (10 ng/mL)-activated human hepatic stellate cells (HSCs) proliferation[2].Fezagepras (250 or 500 µM; 24hours) dose-dependently arrests HSCs at the G0/G1 phase without inducing apoptosis[2]. Cell Proliferation Assay[2] Cell Line:
In Vivo	Fezagepras (100 mg/kg/day; gavage from 8-20 weeks of age) markedly decreases hyperglycemia and markedly improvea glucose tolerance in type 2 diabetes eNOS-/-db/db mice[1]. Animal Model:
Name	Fezagepras
CAS	1002101-19-0
Formula	C13H18O2
Molar Mass	206.28
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Li Y, et al. Fatty acid receptor modulator PBI-4050 inhibits kidney fibrosis and improves glycemic control. JCI Insight. 2018 May 17;3(10). pii: 120365. [2]. Grouix B, et al. PBI-4050 Reduces Stellate Cell Activation and Liver Fibrosis through Modulation of Intracellular ATP Levels and the Liver Kinase B1/AMP-Activated Protein Kinase/Mammalian Target of Rapamycin Pathway. J Pharmacol Exp Ther. 2018 Oct;367(1):

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