| Name | Fezagepras sodium |
| 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]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (8.76 mM), Sonication is recommended.
H2O : 90 mg/mL (394.29 mM), Sonication is recommended.
DMSO : 60 mg/mL (262.86 mM), Sonication is recommended.
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| Keywords | Setogepram sodium | PBI-4050 sodium | GPR40 | Fezagepras sodium |
| Inhibitors Related | Monomethyl fumarate | Questiomycin A | Pamoic acid disodium | Azathioprine | CRTh2 antagonist 2 | Benzyl nicotinate | 1-methoxycyclopropanecarboxylic acid | TUG-1375 | CAY10595 | TUG-424 | Timapiprant | Tricosanoic acid |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Fibrosis Compound Library | Orally Active Compound Library | Anti-Aging Compound Library | Immunology/Inflammation Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | GPCR Compound Library |
United States
