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编 号:F429590
分子式:C24H40O5
分子量:408.57
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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.

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.

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.
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