Cathepsin G Inhibitor I

一种cathepsin G抑制剂（IC50=53 nM）；对cathepsin G具有选择性，抑制作用明显强于对凝血酶、因子Xa、因子IXa、纤溶酶、胰蛋白酶和PR3的抑制（IC50均>100 µM），但也对胰凝乳蛋白酶有弱抑制作用；在10 µM时，抑制cathepsin G诱导的中性粒细胞颗粒释放物中的IL-36激活；在10 µM时，减少TTC处理的B细胞中CD4+ T细胞诱导的IFN-γ和IL-17分泌，并减少TTC在B细胞中的呈递；在小鼠IgG诱导的脑损伤模型中，与西维拉特（sivelestat）联合使用时，减少神经脊髓炎损伤的大小并减少血管周围中性粒细胞的数量，剂量为5 µg/只动物。A cathepsin G inhibitor (IC50 = 53 nM); selective for cathepsin G over thrombin, Factor Xa, Factor IXa, plasmin, trypsin, and PR3 (IC50s = >100 µM for all), but also weakly inhibits chymotrypsin; inhibits cathepsin G-induced activation of IL-36 in neutrophil degranulates at 10 µM; reduces CD4+ T cell-induced secretion of IFN-γ and IL-17 in B cells incubated with TTC and also reduces TTC presentation in B cells at 10 µM; decreases the size of neuromyelitis optica lesions and reduces the number of perivascular neutrophils when used in combination with sivelestat in a mouse model of IgG-induced brain injury at 5 µg/animal.