| Identification | Back Directory | [Name]
PBI-4050 Sodium salt | [CAS]
1254472-97-3 | [Synonyms]
Fezagepras (sodium)
PBI-4050 Sodium salt
Setogepram sodium salt | [Molecular Formula]
C13H19NaO2 | [MDL Number]
MFCD31657323 | [MOL File]
1254472-97-3.mol | [Molecular Weight]
230.28 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
Water : ≥ 100 mg/mL (438.10 mM);DMSO : ≥ 64 mg/mL (280.38 mM) | [form ]
Solid | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Fezagepras (Setogepram) sodium acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84[1]. Fezagepras sodium decreases renal, liver and pancreatic fibrosis[1][2]. Fezagepras sodium exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions[2]. | [in vivo]
Fezagepras sodium (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: | Type 2 diabetes eNOS-/-db/db mice[1] | | Dosage: | 100 mg/kg/day | | Administration: | Given via daily gavage from 8-20 weeks | | Result: | Compared with vehicle-treated mice, hyperglycemia was markedly decreased, and glucose tolerance was markedly improved. |
| [References]
[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. DOI:10.1172/jci.insight.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. DOI:10.1124/jpet.118.250068 |
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