Butaprost 

Butaprost is a selective prostaglandin E receptor (EP2) agonist with an EC₅₀ of 33 nM and a K_i 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^[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. 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

408.57

C₂₄H₄₀O₅

69685-22-9

液体

Colorless to light yellow

Room temperature in continental US; may vary elsewhere.

Solution, -20°C, 2 years

• [1]. Yanbin Liang, et al. Upregulation of orphan nuclear receptor Nur77 following PGF(2alpha), Bimatoprost, and Butaprost treatments. Essential role of a protein kinase C pathway involved in EP(2) receptor activated Nur77 gene transcription. Br J Pharmacol. 20  [Content Brief]

  [2]. Michael Schou Jensen, et al. Activation of the prostaglandin E 2 EP 2 receptor attenuates renal fibrosis in unilateral ureteral obstructed mice and human kidney slices. Acta Physiol (Oxf). 2019 Sep;227(1):e13291.  [Content Brief]

  [3]. K Tani, et al. Design and synthesis of a highly selective EP2-receptor agonist. Bioorg Med Chem Lett. 2001 Aug 6;11(15):2025-8.  [Content Brief]