Apixaban 是一种高度选择性，可逆的、口服具有活力的凝血因子 Xa (Factor Xa) 抑制剂，抑制人和兔凝血因子 Xa 的Ki分别为 0.08 nM 和 0.17 nM。它可以用于研究各种血栓栓塞疾病。

Apixaban is an orally active inhibitor of coagulation factor Xa with anticoagulant activity. Apixaban directly inhibits factor Xa, thereby interfering with the conversion of prothrombin to thrombin and preventing the formation of cross-linked fibrin clots.

Apixaban在犬体内具有优良的药代动力学特性：极低间隙(Cl: 0.02 L/kg/h),低体积分布 (Vdss: 0.2 L/kg),半衰期(T1/2: 5.8 h)和口服生物有效性(F: 58%).作用于静脉血栓形成、动静脉分流血栓形成和电介导颈动脉血栓兔子模型,Apixaban能够抗血栓形成,EC50分别为110 nM,270 nM和70 nM.

作用于体外正常人血浆时,Apixaban延长人凝血时间,使凝血酶原时间（3.6 μM）、改良凝血酶原时间（0.37 μM）、活化部分凝血活酶时间（7.4 μM）和HepTest（0.4 μM）延长一倍。Apixaban对人Factor Xa 和兔Factor Xa的抑制具有高选择,Ki分别为0.08和0.17 nM。此外,在PT和APTT实验中,Apixaban对人和兔血浆的效用最高,对大鼠和犬血浆的效果则较低。

Purified FXa is obtained after activation with Russell's viper venom followed by affinity chromatography. The resulting FXa is >95% pure as judged by sodium dodecylsulfate polyacrylamide gel electrophoresis. The substrate affinity values for FXa, expressed as the Michaelis-Menten-Henri constant (Km), for human, rabbit, rat and dog FXa are determined using the chromogenic substrate S-2765, and are 36, 60, 240 and 70 μM, respectively. The substrate hydrolysis is monitored by measuring absorbance at 405 nm at 25°C for up to 30 min using a SpectraMax 384 Plus plate reader and SoftMax. FXa activity for each substrate and inhibitor concentration pair is determined in duplicate. The Ki values are calculated by non-linear least-squares fitting of the steady-state substrate hydrolysis rates to the equation for competitive inhibition (Equation 1) using GRAFIT, where v equals reactions velocity in OD min?1, Vmax equals maxiumum reaction velocity, S equals substrate concentration, and I equals inhibitor concentration.

503612-47-3

C25H25N5O4

459.506

BMS-562247-01;阿哌沙班

Ethanol:<1 mgml
H2O:<1 mgml
DMSO:15 mg/mL (32.6 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years