Letaxaban, formerly known as TAK-442, is a potent, selective, and orally bioavailable factor Xa inhibitor, which is a tetrahydropyrimidin-2(1H)-one analogue. TAK-442 inhibited endogenous FXa activity in platelet-poor human [half-maximal inhibitory concentration (IC(50)): 53 nM, TAK-442 ] and rat (IC(50): 32 nM, TAK-442 ) plasma. TAK-442 inhibited in vitro reconstituted human prothrombinase (system included FXa, calcium, and washed platelets) with an IC(50) value of 51 nM. In a rat model of balloon injury, thrombin activity on the surface of injured vessels increased to 3.2-, 22-, and 5.8-fold the activity on the surface of the intact aorta at 5 minutes, 1 hour, and 24 hours after the injury, respectively. At approximately 1 hour after the injury, TAK-442 blocked platelet-associated thrombin generation on the surface of injured aortas with an IC(50) value of 19 nM. ( J Cardiovasc Pharmacol. 2011 Feb;57(2):201-6.) References: Deftereos S, Bouras G, Giannopoulos G, Kossyvakis C, Panagopoulou V, Pyrgakis V, Stefanadis C. Novel oral anticoagulants in the treatment of acute coronary syndromes: is there any room for new anticoagulants? Curr Clin Pharmacol. 2012 Aug;7(3):195-208. PubMed PMID: 22564121.

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CAS：870262-90-1