Fezagepras

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Fezagepras

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1002101-19-0

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品名称

Setogepram
PBI-4050

产品介绍

Fezagepras (Setogepram) 是一种具有口服活性的GPR40激动剂和GPR84拮抗剂或反向激动剂。Fezagepras 减轻肾，肝和胰腺纤维化。Fezagepras 具有抗纤维化，抗炎和抗增殖作用。

生物活性

Fezagepras (Setogepram) acts as an orally active agonist forGPR40and as an antagonist or inverse agonist forGPR84^[1]. Fezagepras decreases renal, liver and pancreatic fibrosis^[1]^[2]. Fezagepras exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions^[2].

IC₅₀& Target

GPR40, GPR84^[1]

体外研究
(In Vitro)

Fezagepras (500 μM; 24 hours) inhibits TGF-β (10 ng/mL)-activated human hepatic stellate cells (HSCs) proliferation^[2].
Fezagepras (250 or 500 μM; 24hours) dose-dependently arrests HSCs at the G0/G1 phase without inducing apoptosis^[2].

Cell Proliferation Assay^[2]

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^[2]

Cell Line:	HSCs
Concentration:	250 μM, 500 μM
Incubation Time:	24 hours
Result:	Inhibited cell cycle progression.

体内研究
(In Vivo)

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/dbmice^[1].

Animal Model:	Type 2 diabetes eNOS^-/-db/dbmice^[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.

Clinical Trial

分子量

206.28

Formula

C₁₃H₁₈O₂

CAS 号

1002101-19-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.