Edoxaban (DU-176b) hydrochloride 是一种具有口服活性、高效、选择性和直接的Factor Xa (FXa)抑制剂,对人游离FXa和凝血酶原酶的Ki值分别为 0.561 nM 和 2.98 nM。Edoxaban hydrochloride 的选择性是其他凝血蛋白酶的 10000 倍以上。Edoxaban hydrochloride 可用于预防血栓栓塞性疾病的研究。
产品描述
Edoxaban (DU-176b) hydrochloride is an orally active, highly potent, selective, and direct Factor Xa (FXa) inhibitor with K i values of 0.561 and 2.98 nM for free human FXa and prothrombinase. Edoxaban hydrochloride exhibits more than 10,000-fold selectivity over other coagulation proteases. Edoxaban hydrochloride can be used for preventing thromboembolic disease research [1].
体外活性
Edoxaban hydrochloride (1, 1 and 5 minutes respectively) prolongs PT,TT and APTT of human plasma in a concentration-dependent manner [1]. Edoxaban hydrochloride inhibits thrombin-induced platelet aggregation, with an IC 50 of 2.90 μM [1]. Cell Viability Assay [1] Cell Line: Human, rat, cynomolgus monkey and rabbit plasma; Human platelet Concentration: Incubation Time: 1 and 5 minutes Result: Antithrombin.
体内活性
Edoxaban hydrochloride (0.5, 2.5 and 12.5 mg/kg; p.o.; once) significantly and dose-dependently reduces the thrombus formation and prolongs PT [1]. Animal Model: Male Slc: Wistar rats (210-240 g); Male New Zealand White rabbits(2.5-3.5 kg) (Both are venous stasis thrombosis model) [1]. Dosage: 0.5, 2.5 and 12.5 mg/kg Administration: Oral administration; once Result: Inhibited exogenous FXa activity. Antithrombotic.
Cas No.
480448-29-1
分子式
C24H31Cl2N7O4S
分子量
584.52
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years