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Fezagepras sodium

Catalog No. T12375 CAS 1254472-97-3

Synonyms: Setogepram sodium salt, PBI-4050 sodium salt

Fezagepras sodium (Setogepram sodium salt) is an orally active GPR40 agonist and is an antagonist or inverse agonist for GPR84, with anti-fibrotic, anti-inflammatory and anti-proliferative actions.

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Fezagepras sodium, CAS 1254472-97-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 60.00
5 mg	In stock	$ 147.00
10 mg	In stock	$ 239.00
25 mg	In stock	$ 448.00
50 mg	In stock	$ 669.00
100 mg	In stock	$ 953.00
500 mg	In stock	$ 1,920.00
1 mL * 10 mM (in DMSO)	In stock	$ 162.00

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Purity: 99.59%

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Description	Fezagepras sodium (Setogepram sodium salt) is an orally active GPR40 agonist and is an antagonist or inverse agonist for GPR84, with anti-fibrotic, anti-inflammatory and anti-proliferative actions.
In vitro	PBI-4050 inhibited kidney macrophage infiltration, oxidative stress, and TGF-β-mediated fibrotic signaling pathways, and it also protected against the development of tubulointerstitial fibrosis. To confirm a direct antiinflammatory/antifibrotic effect in the kidney, further studies with a nondiabetic model of EGFR-mediated proximal tubule activation confirmed that PBI-4050 dramatically decreased the development of the associated tubulointerstitial injury and macrophage infiltration[1].
In vivo	eNOS-/- db/db mice were treated with PBI-4050 from 8-20 weeks of age (early treatment) or from 16-24 weeks of age (late treatment). PBI-4050 treatment ameliorated the fasting hyperglycemia and abnormal glucose tolerance tests seen in vehicle-treated mice. In addition, PBI-4050 preserved (early treatment) or restored (late treatment) blood insulin levels and increased autophagy in islets. PBI-4050 treatment led to significant improvements in lifespan in the diabetic mice. Both early and late PBI-4050 treatment protected against progression of DN, as indicated by reduced histological glomerular injury and albuminuria, slow decline of glomerular filtration rate, and loss of podocytes[1].

Synonyms	Setogepram sodium salt, PBI-4050 sodium salt
Molecular Weight	228.26
Formula	C13H17NaO2
CAS No.	1254472-97-3

Storage

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

Solubility Information

H2O: 90.0 mg/mL (394.3 mM)

DMSO: 57.6 mg/mL (252.3 mM)

References 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：

Drug Repurposing Compound Library Bioactive Compound Library Bioactive Compounds Library Max Clinical Compound Library

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Keywords

Fezagepras sodium 1254472-97-3 Endocrinology/Hormones GPCR/G Protein GPR Setogepram sodium Setogepram sodium salt PBI-4050 sodium PBI-4050 sodium salt inhibitor inhibit

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