| 名称 | Apixaban |
| 描述 | Apixaban (BMS-562247-01) 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. |
| 激酶实验 | 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. |
| 体外活性 | 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. |
| 体内活性 | 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。 |
| 存储条件 | Keep away from direct sunlight,
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 10.00 mg/mL (21.76 mM), Sonication is recommended.
10% DMSO+90% Saline : < 1 mg/mL (2.18 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (2.18 mM), Solution.
H2O : < 1 mg/mL (insoluble or slightly soluble)
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| 关键字 | rabbit | plasma | Inhibitor | inhibit | human | Fxa | FactorXa | Factor Xa (rabbit) | Factor Xa (human) | Factor Xa | Factor | EC2x | clotting | Apixaban |
| 相关产品 | Heparin sodium salt | 2-Methoxyphenothiazine | Gabexate mesylate | Coumarin | Edoxaban Tosylate Monohydrate | Edoxaban | 4-Chlorophenylurea | Zifaxaban | Fondaparinux sodium | Rivaroxaban | Letaxaban | FXIIa-IN-1 HCl |
| 相关库 | 抑制剂库 | 经典已知活性库 | 已知活性化合物库 | ReFRAME 相关化合物库 | EMA 上市药物库 | 抗心血管疾病化合物库 | 高选择性抑制剂库 | 上市药物库 | 抗病毒库 | FDA 上市药物库 | 药物功能重定位化合物库 | 儿童药物库 |