贝曲西班 T4341
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
500 mg | 330942-05-7 | ¥9,420.00 | 询底价 |
50 mg | 330942-05-7 | ¥2,960.00 | 询底价 |
100 mg | 330942-05-7 | ¥4,370.00 | 询底价 |
1 mL | 330942-05-7 | ¥728.00 | 询底价 |
2 mg | 330942-05-7 | ¥395.00 | 询底价 |
25 mg | 330942-05-7 | ¥1,780.00 | 询底价 |
5 mg | 330942-05-7 | ¥663.00 | 询底价 |
1 mg | 330942-05-7 | ¥283.00 | 询底价 |
10 mg | 330942-05-7 | ¥980.00 | 询底价 |
Product Introduction
Bioactivity
英文名: Betrixaban
描述: Betrixaban (PRT054021) 是一种口服具有活力的选择性factor Xa(fXa) 抑制剂,IC50=1.5 nM。
激酶实验: To measure the inhibition of fXa activity by direct fXa inhibitors and the reversal of its inhibitory effect by r-Antidote, purified human plasma fXa (3 nM) (Haematologic Technologies), varying concentrations of inhibitor (0, 2.5, 5.0 and 7.5 nM) and r-Antidote are added to the assay buffer (20 mM Tris, 150 mM NaCl, 5 mM Ca2+ and 0.1% BSA, pH 7.4). After incubation at room temperature for 30 min, 100 μM Spectrozyme-fXa is added to the mixture, and the initial rate of sub?strate cleavage is monitored continuously for 5 min at 405 nm in a 96-well plate reader. The initial velocity of product formation as a function of inhibitor and r-Antidote concentrations is analyzed by Dynafit to estimate the binding affinity of r-Antidote to each inhibitor[2]. .
动物实验: Whole-blood INR values (mean±s.d.) in rats infused with Betrixaban (1 mg/kg per hour) or vehicle and then treated with either vehicle or r-Antidote by i.v. bolus (6 mg) over 5 min plus infusion (9 mg/h) for up to 90 min. Circles, vehicle+vehicle; squares, Betrixaban + vehicle; triangles, Betrixaban + r-Antidote. *P≤0.02 compared to the r-Antidote treatment group determined by unpaired two-tailed t test. Whole-blood INR values (mean±s.d.) in rats infused with Apixaban (0.5 mg per kg body weight h?1) or vehicle and then treated with either vehicle or r-Antidote by i.v. bolus (6 mg) over 5 min plus infusion (6 mg/h) for up to 90 min. Circles, vehicle + vehicle; squares, apixaban + vehicle; triangles, apixaban+r-Antidote. *P≤0.01 compared to the r-Antidote treatment group determined by unpaired two-tailed t test.
体外活性: In patch clamp hERG assays, Betrixaban has IC50 of 8.9 μM. The plasma kallikrein IC50 and Ki values for Betrixaban are 6.3 μM and 3.5 μM respectively. Betrixaban (hERG Ki 1.8 μM) exhibits significantly lower hERG activity than all the others (hERG Ki?0.5 μM)
体内活性: Dosed at 0.5 mg/kg IV and 2.5 mg/kg PO, Betrixaban has bioavailability of 51.6% in dog; dosed at 0.75 mg/kg IV and 7.5 mg/kg PO, Betrixaban has bioavailability of 58.7% in monkey[1]. Both Betrixaban and Apixa-ban-mediated whole-blood INR increases are similarly reversed by r-Antidote. After i.v. infusion of the three fXa inhibitors (each admin¬istered individually) for 30 min, the total plasma concentrations of rivaroxaban, Betrixaban and apixaban are 1.4±0.4 μM (mean±s.d.), 0.2±0.01 μM and 1.4±0.3 μM, respectively, and the percentages of unbound inhibitor are 2.2%±0.8% (mean±s.d.), 40%±7.2% and 1.5%±0.3%, respectively. After administration of r-Antidote, the total plasma concentrations of the inhibitors increased to 1.9±0.09 μM, 2.0±0.4 μM and 4.2±0.7 μM, respectively, and the percentage of unbound inhibitor declined to 0%, 0.3%±0.1% and 0.05%±0.02%, respectively. Therefore, for each of the three inhibitors, correction of prothrombin time by r-Antidote to near-normal values is associated with a reduction in the free fraction of the inhibitor[2].
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 16.67 mg/mL (36.88 mM)
关键字: PRT-054021 | Betrixaban | Factor Xa | inhibit | Fxa | PRT 054021 | Inhibitor
相关产品: Zifaxaban | Fondaparinux sodium | RWJ-445167 | Edoxaban Tosylate Monohydrate | Betrixaban maleate | Heparin sodium salt | Letaxaban | D-Pro-Phe-Arg-Chloromethylketone | 2-Methoxyphenothiazine | Rivaroxaban-d4
相关库: FDA-Approved Drug Library | Drug Repurposing Compound Library | Approved Drug Library | ReFRAME Related Library | Bioactive Compounds Library Max | Inhibitor Library | Pediatric Drug Library | EMA Approved Drug Library | Orally Active Compound Library | Bioactive Compound Library
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途