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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 | |
| CAS | No.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 |
| MDL | MFCD16038040 |
| SMILES | CN(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 |
| InChIKey | XHOLNRLADUSQLD-UHFFFAOYSA-N |
| InChI | InChI=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 CID | 10275777 |
| 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]. |
| IC50 | IC50: 1.5 nM (fXa)[1] |
| In Vitro | Betrixaban (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 | 瓶 |
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文献和实验bSuKm1foWOq5wNpboNQLmlo2Fn6wS/ZjqQvb2Gy88CULhuQ5TVEaoQ2gtdU9TtPRtFgh/BbLYDrlNQtO4GHJJVoXvFg0UhwMJHFBz8InEEZPh1ZysOf82LTuunw2ReE8zcuwcvBs9FhSwx9ygL9MIXF3cE5dCHQW6tUCFBRmfdHz/iB3LBwEAHsR9N0y8571/wU9NGdk3x4RpaZL/f4OLeO2i7bi76ls+Z7gQPsYry5csjR44c9GX7BuIIRl9f
释放,任何由 DW12 品系衍生出的品系可以用作牲畜词料……”。同样,“自 2006 年 6 月 22 日起,普通小麦品系 BW255-2 和 BW238-3 也被批准环境释放和用作牲畜伺料”。尽管上述品系已通过审批,但能否完全商业化还不能确定。 4.2 耐虫性 最近与耐虫性相关的研究报道有:利用豇豆胰蛋白酶抑制剂防治麦蛾(Sitotroga cerealella Olivier) [ 22 ] , 利用马铃暮蛋白酶抑制剂(PIN2 ) 防治线虫 [23]。 4.3 耐病性
Phage‐Based Expression Cloning to Identify Interacting Proteins
(see recipe ), ice cold Sephadex G‐50 equilibrated in recipeZ′‐KCl E. coli Y1090r− or other appropriate host strain
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