1. GPCR/G Protein
  2. Free Fatty Acid Receptor GPR84
  3. Fezagepras

Fezagepras  (Synonyms: Setogepram; PBI-4050)

目录号: HY-100775A
产品使用指南

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。

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Fezagepras Chemical Structure

Fezagepras Chemical Structure

CAS No. : 1002101-19-0

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规格 是否有货
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100 mg   询价  
250 mg   询价  

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Fezagepras 的其他形式现货产品:

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Other Forms of Fezagepras:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Fezagepras (Setogepram) acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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/db mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
分子量

206.28

Formula

C13H18O2

CAS 号
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.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Fezagepras
目录号:
HY-100775A
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