Camostat (mesylate)

蛋白酶抑制剂；抑制胰蛋白酶(Ki=1nM)以及各种炎性蛋白酶，包括纤溶酶、激肽释放酶和凝血酶；在50µM时抑制假型SARS-CoV或SARS-CoV-2刺突糖蛋白的VSV颗粒进入Calu-3细胞和原代人肺上皮细胞；减少Calu-3细胞中SARS-CoV-2基因组等价物（感染标志物）的数量；抑制人气道上皮细胞的钠通道功能（IC50=50nM）；增强绵羊的粘液纤毛清除能力；饮食给药以1mg/kg的剂量抑制单核细胞产生TNF-α和趋化因子（CC基序）配体2(CCL2)，以及抑制大鼠胰腺纤维化模型中胰腺星状细胞的增殖。A protease inhibitor; inhibits trypsin (Ki = 1 nM), as well as various inflammatory proteases, including plasmin, kallikrein, and thrombin; inhibits entry of VSV particles pseudotyped with SARS-CoV or SARS-CoV-2 spike glycoprotein in Calu-3 cells and primary human lung epithelial cells at 50 µM; reduces the number of SARS-CoV-2 genomic equivalents, a marker of infection, in Calu-3 cells; inhibits sodium channel function in human airway epithelial cells (IC50 = 50 nM); enhances mucociliary clearance in sheep; dietary administration inhibits the production of TNF-α and chemokine (C-C motif) ligand 2 (CCL2) by monocytes, as well as proliferation of pancreatic stellate cells in a rat model of pancreatic fibrosis at 1 mg/kg.