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，同时，Butaprost 对鼠类 EP1，EP3 和 EP4 受体的活性较低。Butaprost 通过阻碍TGF-β/Smad2信号传导的作用机制，减轻肾纤维化。

Butaprost is a selective prostaglandin E receptor (EP2) agonist with an EC 50 of 33 nM and a K i of 2.4 μM for murine EP2 receptor. However, Butaprost is less activity against murine EP1, EP3 and EP4 receptors. Butaprost attenuates fibrosis by hampering TGF-β/Smad2 signalling pathway [1] [2] [3].

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 manner. Butaprost upregulated Nur77 gene expression through the PKC pathway [1]. 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 [2]. Western Blot Analysis [1] 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.

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 demonstrated by a reduction in the gene and protein expression of α-smooth muscle actin, fibronectin and collagen 1A1 [2]. Animal Model: Male C57BL/6 mice (8 weeks of age; 21 g) bearing unilateral ureteral obstruction surgery [2] 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.

69685-22-9

C24H40O5

408.57

TR-4979;(R)-Butaprost;Butaprostum;Butaprost

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years