Thrombin inhibitor 6

Thrombin inhibitor 6 is a potent thrombin inhibitor (IC50: 1 nM). Thrombin inhibitor 6 has the function as an anticoagulant[1].

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Metabolic Enzyme/Protease >> Thrombin

Thrombin inhibitor 6 (compound 73) 在与 CD-1 小鼠和人微粒体孵育时是稳定的 (Clint (小鼠) = 60 μL/min/mg；Clint (人) = 17 μL/min/mg)[1].

Thrombin inhibitor 6 (compound 73) (9 mg/kg，静脉注射) 可延长 CD-1 小鼠的尾部出血时间[1]。 Thrombin inhibitor 6 (compound 73) (5 mg/kg，口服) 在雄性 CD-1 小鼠中的 F(%) 为 22.8%，AUC 为 713.3 h.ng/mL，Cmax 为 127 ng/mL[1]。 Animal Model: CD-1 mice[1] Dosage: 9 mg/kg Administration: Intravenous injection (i.v.) Result: The mice bled for 25 min following transection. Led to 1.5-fold increase of liberated whole blood cells.

[1]. Short KM, et al. Discovery of novel N-acylpyrazoles as potent and selective thrombin inhibitors. Eur J Med Chem. 2022 Oct 27;246:114855.