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Fezagepras

Catalog No. T12883   CAS 1002101-19-0
Synonyms: PBI-4050, Setogepram

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.

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Fezagepras Chemical Structure
Fezagepras, CAS 1002101-19-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 48.00
2 mg In stock $ 68.00
5 mg In stock $ 97.00
10 mg In stock $ 143.00
25 mg In stock $ 258.00
50 mg In stock $ 369.00
100 mg In stock Inquiry
1 mL * 10 mM (in DMSO) In stock $ 94.00
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Purity: 99.38%
Purity: 96.73%
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Biological Description
Chemical Properties
Storage & Solubility Information
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].
Synonyms PBI-4050, Setogepram
Molecular Weight 206.28
Formula C13H18O2
CAS No. 1002101-19-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 60 mg/ml (290.87 mM)

TargetMolReferences and Literature

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):71-81.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library GPCR Compound Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Inhibitor Library Orally Active Compound Library Clinical Compound Library Endocrinology-Hormone Compound Library Bioactive Compounds Library Max Preclinical Compound Library

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Keywords

Fezagepras 1002101-19-0 Endocrinology/Hormones GPCR/G Protein GPR PBI 4050 Free Fatty Acid Receptor PBI-4050 GPR84 inhibit PBI4050 FFAR G protein coupled receptor 84 Diabetes,Kidney,Renal,Pancreatic,Liver,Fibrosis,Nephrology Inhibitor Setogepram inhibitor

 

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