PBI-4050

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PBI-4050（Setogepram，PBI4050）是一种中链脂肪酸的合成类似物，分别对 GPR40 和 GPR84 显示出激动剂和拮抗剂配体亲和力。

PBI-4050 (Setogepram, PBI4050) is a synthetic analog of a medium-chain fatty acid that displays agonist and antagonist ligand affinity toward GPR40 and GPR84, respectively; PBI-4050 significantly attenuated fibrosis in many injury contexts, as evidenced by the antifibrotic activity observed in kidney, liver, heart, lung, pancreas, and skin fibrosis models; PBI-4050 is a first-in-class compound that may be effective for managing inflammatory and fibrosis-related diseases.Fibrosis Phase 2 Clinical.

Fezagepras (500 μM; 24 hours) inhibits TGF-β (10 ng/mL)-activated human hepatic stellate cells (HSCs) proliferation.Fezagepras (250 or 500 μM; 24hours) dose-dependently arrests HSCs at the G0/G1 phase without inducing apoptosis. Cell Proliferation Assay Cell Line:HSCs Concentration:250 or 500 μM Incubation Time:24 hours Result:Inhibited TGF-β-activated HSC proliferation. TGF-β (10 ng/mL) increased HSC proliferation by 10%. Cell Cycle Analysis Cell Line:HSCs Concentration:250 μM, 500 μM Incubation Time:24 hoursResult:Inhibited cell cycle progression.

Fezagepras (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. Animal Model:Type 2 diabetes eNOS-/-db/db miceDosage: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.

Setogepram | PBI4050

GPCR/G Protein

FFAR

FFAR

Other Indications

Fibrosis

1002101-19-0

206.285

C13H18O2

>98% (HPLC)

——

O=C(O)CC1=CC=CC(CCCCC)=C1

(3-pentylphenyl)acetic acid

(-20℃)

With Ice Pack

≥ 2 years