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IB1090 贝曲西班 代谢酶/蛋白酶 索莱宝

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  • ¥790 - 5790
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  • 北京
  • IB1090
  • 2025年07月23日
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    • 详细信息
    • 文献和实验
    • 技术资料
    • 保存条件

      Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year

    • 保质期

      Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year

    • 英文名

      Betrixaban

    • 库存

      现询

    • 供应商

      北京索莱宝科技有限公司

    • CAS号

      330942-05-7

    • 规格

      100mg/50mg/10mg/5mg

    规格:100mg产品价格:¥5790.0
    规格:50mg产品价格:¥3590.0
    规格:10mg产品价格:¥1190.0
    规格:5mg产品价格:¥790.0

    基本信息
    CASNo.330942-05-7
    中文名称贝曲西班
    英文名称Betrixaban
    别名PRT054021
    分子式C23H22ClN5O3
    分子量451.91
    溶解性Soluble in DMSO(Need ultrasonic)
    纯度≥98%
    外观(性状)Solid
    储存条件Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
    MDLMFCD16038040
    SMILESCN(C)C(=N)C1=CC=C(C=C1)C(=O)NC2=C(C=C(C=C2)OC)C(=O)NC3=NC=C(C=C3)Cl
    InChIKeyXHOLNRLADUSQLD-UHFFFAOYSA-N
    InChIInChI=1S/C23H22ClN5O3/c1-29(2)21(25)14-4-6-15(7-5-14)22(30)27-19-10-9-17(32-3)12-18(19)23(31)28-20-11-8-16(24)13-26-20/h4-13,25H,1-3H3,(H,27,30)(H,26,28,31)
    PubChem CID10275777
    靶点Factor Xa
    通路Metabolic Enzyme&Protease
    背景说明Betrixaban是一种有效的,选择性 factor Xa 抑制剂。
    生物活性Betrixaban (PRT054021) is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor with an IC50 of 1.5 nM. Betrixaban shows antithrombotic effect[1][3].
    IC50IC50: 1.5 nM (fXa)[1]
    In VitroBetrixaban (PRT054021) shows IC50 of 8.9 μM in patch clamp hERG assays[1].Betrixaban shows an IC50 and a Ki of 6.3 μM and 3.5 μM for the plasma kallikrein, respectively[1].Betrixaban (hERG Ki 1.8 μM) exhibits significantly lower hERG activity than all the others (hERG Ki?0.5 μM)[1].Betrixaban (5-25 ng/mL) inhibits thrombin generation[3].
    细胞实验Betrixaban (0.5 mg/kg, i.v.; 2.5 mg/kg, p.o.) has oral bioavailability of 51.6% in dog[1].Betrixaban (0.75 mg/kg, i.v.; 7.5 mg/kg, p.o.) has oral bioavailability of 58.7% in monkey[1].Betrixaban mediated whole-blood INR increase is reversed by r-Antidote. After i.v. infusion for 30 min, the total plasma concentrations of Betrixaban is 0.2±0.01 μM, and the percentages of unbound inhibitor is 40%±7.2%. After administration of r-Antidote, the total plasma concentration increased to 2.0±0.4 μM, and the percentage of unbound inhibitor declined to 0.3%±0.1%[2].Betrixaban (3 mg/kg) shows nearly comparable inhibition of thrombus mass to enoxaparin 1.6 mg/kg (76% vs 96% inhibition) in the rabbit abdominal vena cava model of clot accretion on cotton threads[3].Betrixaban (19.1 mg/kg) is at least as effective at maintaining patency as enoxaparin 7.6 mg/kg and clopidogrel 3 mg/kg/d (90% vs 70% vs 80% patency, respectively) in the ferric chloride injury model of rodent carotid artery[3].
    动物实验Rats[2]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.
    数据来源文献[1]. Zhang P, et al. Discovery of Betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor. Bioorg Med Chem Lett. 2009 Apr 15;19(8):21
    [2]. Lu G, et al. A specific antidote for reversal of anticoagulation by direct and indirect inhibitors of coagulation factor Xa. Nat Med. 2013 Apr;19(4):446-51.
    [3]. Chan NC, et al. Profile of betrixaban and its potential in the prevention and treatment of venous thromboembolism. Vasc Health Risk Manag. 2015 Jun 26;11:343-51.
    单位

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