Fezagepras sodium|1254472-97-3|(Setogepram sodium; PBI-4050 sodium)-陌孚医药/Medlife

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Fezagepras sodium (Synonyms: Setogepram sodium; PBI-4050 sodium)

目录号: PL01129 纯度: ≥99%

CAS No. :1254472-97-3

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中文名称	Fezagepras sodium
英文名称	Fezagepras sodium
英文别名	Setogepram sodium salt;Setogepram sodium;Setogepram (sodium salt);sodium 2-(3-pentylphenyl)acetate;R05571KE07;sodium;2-(3-pentylphenyl)acetate;3-Pentylbenzenacetic acid sodium salt;3-pentylbenzeneacetic acid sodium salt;SB17465;Benzeneacetic acid, 3-pentyl-, sodium salt (1:1);PBI-4050 sodium salt
Cas No.	1254472-97-3
分子式	C₁₃H₁₇NaO₂
分子量	228.26
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

Fezagepras (Setogepram) sodium 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 sodium 减轻肾，肝和胰腺纤维化。Fezagepras sodium 具有抗纤维化，抗炎和抗增殖作用。

生物活性

Fezagepras (Setogepram) sodium acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84. Fezagepras sodium decreases renal, liver and pancreatic fibrosis. Fezagepras sodium exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions.

性状

Solid

IC50 & Target[1][2]

GPR40, GPR84

体外研究(In Vitro)

Fezagepras sodium (500 μM; 24 hours) inhibits TGF-β (10 ng/mL)-activated human hepatic stellate cells (HSCs) proliferation.
Fezagepras sodium (250 or 500 μM; 24 hours) dose-dependently arrests HSCs at the G0/G1 phase without inducing apoptosis. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Proliferation Assay-tbl">

体内研究(In Vivo)

Fezagepras sodium (100 mg/kg/day; gavage from 8-20 weeks of age) markedly decreases hyperglycemia and markedly improvea glucose tolerance in type 2 diabetes eNOSdb/db mice. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Li Y, et al. Fatty acid receptor modulator PBI-4050 inhibits kidney fibrosis and improves glycemic control. JCI Insight. 2018 May 17;3(10). pii: 120365.
[2]. Grouix B, et al. PBI-4050 Reduces Stellate Cell Activation and Liver Fibrosis through Modulation of Intracellular ATP Levels and the Liver Kinase B1/AMP-Activated Protein Kinase/Mammalian Target of Rapamycin Pathway. J Pharmacol Exp Ther. 2018 Oct;367(1):

溶解度数据	In Vitro: H₂O : ≥ 100 mg/mL (438.10 mM)DMSO : ≥ 64 mg/mL (280.38 mM)

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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