Betrixaban maleate
Based on 5 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 99.78%
- CAS No.: 936539-80-9
- Formula: C27H26ClN5O7
- Molecular Weight:567.98
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Betrixaban maleate
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Biological Activity
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 936539-80-9
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Appearance Solid
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Molecular Weight 567.98
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Formula C27H26ClN5O7
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Color White to off-white
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SMILES
N=C(N(C)C)C(C=C1)=CC=C1C(NC2=CC=C(OC)C=C2C(NC(C=C3)=NC=C3Cl)=O)=O.O=C(O)/C=C\C(O)=O
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Synonyms
PRT054021 maleate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (5)
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Journal Impact Factor
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Most Recent
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Thromb Haemost
Betrixaban: Impact on Routine and Specific Coagulation Assays-A Practical Laboratory Guide. [Abstract]2018 Jul;118(7):1203-1214. PMID: 29890519 -
Molecules
Generic Methods for Simultaneous Analysis of Four Direct Oral Anticoagulants in Human Plasma and Urine by Ultra-High Performance Liquid Chromatography-Tandem Mass Spectrometry. [Abstract]2023 Feb 28;28(5):2254. PMID: 36903499 -
Int J Lab Hematol
Development of new methodologies for the chromogenic estimation of betrixaban concentrations in plasma. [Abstract]2019 Apr;41(2):250-261. PMID: 30604921 -
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Elife
2022 Mar 23:11:e77444. PMID: 35294338
Solvent & Solubility
DMSO : 50 mg/mL (88.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 2 mg/mL (3.52 mM; ultrasonic and warming and heat to 60°C)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (279 KB)
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SDS (557 KB)
- English - EN (557 KB)
- Français - FR (557 KB)
- Deutsch - DE (557 KB)
- Norwegian - NO (557 KB)
- Español - ES (557 KB)
- Swedish - SV (557 KB)
- Italian - IT (557 KB)
- Korean - KR (557 KB)
- Portuguese - PT (557 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.7606 mL | 8.8031 mL | 17.6063 mL | 44.0156 mL |
| DMSO | 5 mM | 0.3521 mL | 1.7606 mL | 3.5213 mL | 8.8031 mL |
| 10 mM | 0.1761 mL | 0.8803 mL | 1.7606 mL | 4.4016 mL | |
| 15 mM | 0.1174 mL | 0.5869 mL | 1.1738 mL | 2.9344 mL | |
| 20 mM | 0.0880 mL | 0.4402 mL | 0.8803 mL | 2.2008 mL | |
| 25 mM | 0.0704 mL | 0.3521 mL | 0.7043 mL | 1.7606 mL | |
| 30 mM | 0.0587 mL | 0.2934 mL | 0.5869 mL | 1.4672 mL | |
| 40 mM | 0.0440 mL | 0.2201 mL | 0.4402 mL | 1.1004 mL | |
| 50 mM | 0.0352 mL | 0.1761 mL | 0.3521 mL | 0.8803 mL | |
| 60 mM | 0.0293 mL | 0.1467 mL | 0.2934 mL | 0.7336 mL | |
| 80 mM | 0.0220 mL | 0.1100 mL | 0.2201 mL | 0.5502 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Betrixaban maleate Related Classifications
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