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].

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.