化合物 T26925 T26925

Product Introduction
Bioactivity


英文名: Butaprost

描述: Butaprost is a chemical compound that functions as a selective agonist for the prostaglandin E receptor (EP2). It exhibits an EC50 of 33 nM and a Ki of 2.4 μM when interacting with the murine EP2 receptor. However, Butaprost demonstrates lower activity against murine EP1, EP3, and EP4 receptors. Furthermore, it effectively attenuates fibrosis by inhibiting the TGF-β/Smad2 signaling pathway [1] [2] [3].

体外活性: 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.

体内活性: 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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: Butaprost | TR 4979 | TR4979

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途