- Betrixaban maleate
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- $33.00 / 5mg
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2026-01-04
- CAS:936539-80-9
- Min. Order:
- Purity: 98.81%
- Supply Ability: 10g
- Betrixaban Maleate
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- $1.00 / 1KG
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2021-04-16
- CAS:936539-80-9
- Min. Order: 1KG
- Purity: 99%
- Supply Ability: 5000KG
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| | N-(5-Chloro-2-pyridinyl)-2-[[4-[(dimethylamino)iminomethyl]benzoyl]amino]-5-methoxybenzamide (2Z)-2-butenedioate (1:1) Basic information |
| Product Name: | N-(5-Chloro-2-pyridinyl)-2-[[4-[(dimethylamino)iminomethyl]benzoyl]amino]-5-methoxybenzamide (2Z)-2-butenedioate (1:1) | | Synonyms: | Betrixaban maleate;N-(5-Chloro-2-pyridinyl)-2-[[4-[(dimethylamino)iminomethyl]benzoyl]amino]-5-methoxybenzamide (2Z)-2-butenedioate (1:1);N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide maleate;N-(5-chloropyridin-2-yl)-2-[4-(N,N-dimethylcarbamimidoyl)benzamido]-5-methoxybenzamide maleic acid salt;Betrixaban maleate salt;Bctriaban;N-(5-chloropyridin-2-yl)-2[4-(N,N-dimethylcarbamimidoyl)-benzoylamino]-5-methoxybenzamide maleate;13C6]-Betrixaban maleate salt | | CAS: | 936539-80-9 | | MF: | C27H26ClN5O7 | | MW: | 567.98 | | EINECS: | | | Product Categories: | | | Mol File: | 936539-80-9.mol | ![N-(5-Chloro-2-pyridinyl)-2-[[4-[(dimethylamino)iminomethyl]benzoyl]amino]-5-methoxybenzamide (2Z)-2-butenedioate (1:1) Structure](CAS/20180808/GIF/936539-80-9.gif) |
| | N-(5-Chloro-2-pyridinyl)-2-[[4-[(dimethylamino)iminomethyl]benzoyl]amino]-5-methoxybenzamide (2Z)-2-butenedioate (1:1) Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMSO: 100 mg/mL (176.06 mM);Ethanol: Insoluble | | form | Solid | | color | White to off-white | | Water Solubility | Water: 1 mg/mL (1.76 mM) |
| | N-(5-Chloro-2-pyridinyl)-2-[[4-[(dimethylamino)iminomethyl]benzoyl]amino]-5-methoxybenzamide (2Z)-2-butenedioate (1:1) Usage And Synthesis |
| Uses | Betrixaban (PRT054021) maleate is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor with an IC50 of 1.5 nM. Betrixaban maleate shows antithrombotic effect[1][3]. | | in vivo | 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]. | | References | [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. DOI:10.1016/j.bmcl.2009.02.111
[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. DOI:10.1038/nm.3102
[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. DOI:10.2147/VHRM.S63060 |
| | N-(5-Chloro-2-pyridinyl)-2-[[4-[(dimethylamino)iminomethyl]benzoyl]amino]-5-methoxybenzamide (2Z)-2-butenedioate (1:1) Preparation Products And Raw materials |
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