ENMD-1068hydrochloride是一种具有抗血管生成和抗炎活性的选择性蛋白酶激活受体2(PAR2)拮抗剂。ENMD-1068hydrochloride可通过抑制TGF-β1/Smad信号转导而减少星状细胞活化和胶原蛋白表达。
ENMD-1068 hydrochloride is a selective protease-activated receptor 2 (PAR2) antagonist with antiangiogenic and anti-inflammatory activities. ENMD-1068 hydrochloride reduces epatic stellate cells (HSCs) activation and collagen expression through the inhibiton of TGF-β1/Smad signal transduction[1][2].
[1]. Yifeng Wang, et al. ENMD-1068, a protease-activated receptor 2 antagonist, inhibits the development of endometriosis in a mouse model. Am J Obstet Gynecol. 2014 Jun;210(6):531.e1-8. [2]. Quan Sun, et al. ENMD-1068 inhibits liver fibrosis through attenuation of TGF-β1/Smad2/3 signaling in mice. Sci Rep. 2017 Jul 14;7(1):5498.
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