Powder: -20°C for 3 years
In solvent: -80°C for 2 years
Fezagepras sodium is an orally active GPR40 agonist and is an antagonist or inverse agonist for GPR84, with anti-fibrotic, anti-inflammatory and anti-proliferative actions.
Description | Fezagepras sodium 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 | PBI-4050 sodium salt, Setogepram sodium salt |
Molecular Weight | 228.267 |
Formula | C13H17NaO2 |
CAS No. | 1254472-97-3 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
H2O: 90.0 mg/mL (394.3 mM)
DMSO: 57.6 mg/mL (252.3 mM)
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
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Fezagepras sodium 1254472-97-3 G蛋白偶联受体 内分泌与激素 GPR Setogepram sodium salt PBI-4050 sodium salt Inhibitor inhibitor inhibit