Fezagepras sodium

SKU: orb1708932

Description

Fezagepras sodium (Setogepram sodium salt) is an orally bioavailable small molecule that acts as a GPR40 agonist and a GPR84 antagonist/inverse agonist. It exhibits anti-fibrotic, anti-inflammatory, 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

Images & Validation

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Key Properties

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CAS Number	1254472-97-3
MW	228.26
Purity	99.59%
Formula	C₁₃H₁₇NaO₂
SMILES	CCCCCC1=CC(=CC=C1)CC(=O)[O-].[Na+]
Target	GPCR
Solubility	H2O:90 mg/mL (394.29 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (8.76 mM);DMSO:60 mg/mL (262.86 mM)

Bioactivity

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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.

Storage & Handling

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Storage	Powder: -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

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Fezagepras sodium, GPR40, PBI-4050 sodium, PBI-4050 sodium salt, Setogepram sodium, Setogepram sodium salt

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Compound Identifiers

PubChem CID

46944243 ↗

Key Properties

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No computed properties available.

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