盐酸贝曲西班 T4690

Product Introduction
Bioactivity


英文名: Betrixaban hydrochloride(330942-05-7(free base))

描述: Betrixaban hydrochloride(330942-05-7(free base)) (PRT054021 hydrochloride) 是一种有效的、选择性的、口服有效的 Xa 因子 (fXa) 抑制剂 (IC50: 1.5 nM)。

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)[1].

体内活性: Betrixaban (0.5 mg/kg, i.v. and 2.5 mg/kg, p.o.) 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. Thus, 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 : 20 mg/mL (44.26 mM)


关键字: Betrixaban hydrochloride(330942057(free base)) | PRT054021 Hydrochloride | PRT 054021 Hydrochloride | PRT-054021 Hydrochloride | Betrixaban hydrochloride(330942 05 7(free base)) | Betrixaban hydrochloride(330942-05-7(free base))

相关产品: Rivaroxaban Impurity | Fondaparinux sodium | CH3OCO-D-CHA-Gly-Arg-pNA acetate | Edoxaban | Coumarin | Frunexian | Rivaroxaban | Dechloro Rivaroxaban | 2-Methoxyphenothiazine | Rivaroxaban-d4

相关库: FDA-Approved Drug Library | Drug Repurposing Compound Library | FDA-Approved & Pharmacopeia Drug Library | Inhibitor Library | EMA Approved Drug Library | Metabolism Compound Library | Orally Active Compound Library | Target-Focused Phenotypic Screening Library | NO PAINS Compound Library | Anti-Cardiovascular Disease Compound Library

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