Butaprost
目录号 : KM3875 CAS No. : 69685-22-9 纯度 : 98%

Butaprost 是一种选择性前列腺素 E 受体 (EP2) 激动剂,对鼠类 EP2 受体的 EC50 值为 33 nM,Ki 值为 2.4 μM。Butaprost 对鼠类 EP1,EP3 和 EP4 受体的活性较低。Butaprost 通过阻碍 TGF-β/Smad2 信号传导来减轻纤维化。

规格 价格 是否有货 数量
5mg
In-stock

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生物活性

Butaprost is a selective prostaglandin E receptor (EP2) agonist with an EC50 of 33 nM and a Ki of 2.4 μM for murine EP2 receptor. Butaprost is less activity against murine EP1, EP3 and EP4 receptors. Butaprost attenuates fibrosis by hampering TGF-β/Smad2 signalling.

IC50&Target

m-EP2 receptor

2400 nM (Ki)

m-EP2 receptor

33 nM (EC50)

体外研究

Butaprost (1-100 nM; 0.5-24 hours) induces about a five-fold upregulation of Nur77 mRNA expression in hEP2-HEK293/EBNA cells in a dose- and time-dependent. Butaprost upregulated Nur77 gene expression through the PKC pathway.
Butaprost (50 μM; 24 hours) reduces TGF-β-induced fibronectin (FN) expression, Smad2 phosphorylation and epithelial-mesenchymal transition in Madin-Darby Canine Kidney (MDCK) cells.

Western Blot Analysis

Cell Line: HEK 293/EBNA cells stably expressing the human EP2 receptor (hEP2-HEK 293/EBNA cells)
Concentration: 1 nM, 10 nM, 100 nM
Incubation Time: 0.5 hours, 1 hours, 6 hours, 24 hours
Result: Induced about a five-fold upregulation of Nur77 mRNA expression in hEP2-HEK293/EBNA cells.
体内研究

Butaprost (1-4 mg/kg; intraperitoneal injection; twice daily; for 7 days) treatment attenuates the development of fibrosis in mice that underwent unilateral ureteral obstruction surgery, as illustrated by a reduction in the gene and protein expression of α-smooth muscle actin, fibronectin and collagen 1A1.

Animal Model: Male C57BL/6 mice (8 weeks of age; 21 g) bearing unilateral ureteral obstruction surgery
Dosage: 1 mg/kg, 2 mg/kg, 4 mg/kg
Administration: Intraperitoneal injection; twice daily; for 7 days
Result: Attenuated the development of fibrosis in mice that underwent unilateral ureteral obstruction surgery.
分子式
C24H40O5
分子量
408.57
CAS号
69685-22-9
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Solution, -20°C, 2 years

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