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Apixaban (BMS-562247-01) 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 (BMS-562247-01) 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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 278 | 现货 | |
2 mg | ¥ 396 | 现货 | |
5 mg | ¥ 571 | 现货 | |
10 mg | ¥ 851 | 现货 | |
50 mg | ¥ 1,280 | 现货 | |
100 mg | ¥ 1,950 | 现货 | |
200 mg | ¥ 2,930 | 现货 | |
500 mg | ¥ 4,130 | 现货 | |
1 g | ¥ 6,150 | 现货 |
产品描述 | 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. |
靶点活性 | FXa (rabbit):0.17 nM(Ki), FXa (human):0.08 nM(Ki) |
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。 |
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. |
别名 | 阿哌沙班, BMS-562247-01 |
分子量 | 459.5 |
分子式 | C25H25N5O4 |
CAS No. | 503612-47-3 |
Smiles | O=C1C=2N(N=C(C(N)=O)C2CCN1C3=CC=C(C=C3)N4C(=O)CCCC4)C5=CC=C(OC)C=C5 |
密度 | 1.42g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
溶解度信息 | Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 4.59 mg/mL (10 mM), Sonication is recommended. H2O: < 1 mg/mL (insoluble or slightly soluble) | ||||||||||||||||||||
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