丝氨酸蛋白酶抑制剂;Serine Protease Inhibitors;;InformationUK-371804 HCl UK-371804 is a potent and selective urokinase-type plasmogen activator (uPA) inhibitor with excellent enzyme potency (Ki=10 nM) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin).TargetsuPA (Cell-free assay) 10 nM(Ki)In vitroUK-3718046 is able to inhibit exogenous uPA in human chronic wound fluid (IC50=0.89 µM).In vivoin a porcine acute excisional wound model, following topical delivery, UK-3718046 is able to penetrate into pig wounds and inhibit exogenous uPA activity with no adverse effect on wound healing parameters.
参考文献:
1. Paul V Fish, et al. Selective urokinase-type plasminogen activator inhibitors. 4. 1-(7-sulfonamidoisoquinolinyl)guanidines. J Med Chem. 2007, 50, 10.