贝曲西班|T4341|TargetMol

Betrixaban
330942-05-7

￥283 1mg 起订

￥395 2mg 起订

￥663 5mg 起订

上海更新日期：2024-12-02

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产品详情:

中文名称：: 贝曲西班

英文名称：: Betrixaban

CAS号：: 330942-05-7

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.35%

产品类别：: 抑制剂

货号：: T4341

Product Introduction

Bioactivity

名称	Betrixaban
描述	Betrixaban (PRT054021) is a non-vitamin K oral anticoagulant whose action is driven by the competitive and reversible inhibition of the factor Xa [1]. It was selected among all lead compounds due to its low hERG channel affinity while sustaining its factor Xa inhibition capacity [3]. Betrixaban, now developed by Portola Pharmaceuticals Inc., is prescribed as a venous thromboembolism (VTE) prophylactic for adult patients with moderate to severe restricted motility or with other risks for VTE [2]. VTE can be manifested as deep vein thrombosis or pulmonary embolism and it is a leading cause of preventable death in hospitalized patients [4].
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	在贴片钳制hERG实验中，Betrixaban的IC50为8.9 μM。Betrixaban对于血浆激肽释放酶的IC50和Ki值分别为6.3 μM和3.5 μM。相较于其他所有化合物(hERG Ki≤0.5 μM)，Betrixaban（hERG Ki为1.8 μM）展示了明显较低的hERG活性。
体内活性	以0.5 mg/kg静脉注射（IV）和2.5 mg/kg口服（PO）给予Betrixaban时，其在狗的生物利用度为51.6%；以0.75 mg/kg IV和7.5 mg/kg PO给予时，其在猴子的生物利用度为58.7%[1]。Betrixaban和Apixaban引起的全血国际标准化比率（INR）增加可被r-Antidote类似地逆转。在单独给予三种fXa抑制剂（每种分别给予）静脉（i.v.）输注30分钟后，rivaroxaban、Betrixaban和apixaban的总血浆浓度分别为1.4±0.4 μM（平均值±标准差）、0.2±0.01 μM和1.4±0.3 μM，未结合抑制剂的百分比分别为2.2%±0.8%（平均值±标准差）、40%±7.2%和1.5%±0.3%。r-Antidote给药后，这些抑制剂的总血浆浓度分别上升至1.9±0.09 μM、2.0±0.4 μM和4.2±0.7 μM，未结合抑制剂的百分比分别下降到0%、0.3%±0.1%和0.05%±0.02%。因此，对于这三种抑制剂，r-Antidote纠正凝血酶原时间至接近正常值与抑制剂的自由部分减少相关联[2]。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 16.67 mg/mL (36.88 mM), Sonication is recommended.
关键字	PRT-054021 \| Betrixaban \| Factor Xa \| inhibit \| Fxa \| PRT 054021 \| Inhibitor
相关产品	Heparin sodium salt \| 2-Methoxyphenothiazine \| Gabexate mesylate \| Coumarin \| Apixaban \| Edoxaban Tosylate Monohydrate \| Eribaxaban \| Edoxaban \| 4-Chlorophenylurea \| Zifaxaban \| Fidexaban \| Letaxaban
相关库	抑制剂库 \| 经典已知活性库 \| 已知活性化合物库 \| EMA 上市药物库 \| FDA上市及药典收录分子库 \| FDA 上市药物库 \| 药物功能重定位化合物库

贝曲西班|||PRT054021|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子