Razaxaban hydrochloride
Razaxaban hydrochloride (BMS 561389 hydrochloride) is a highly potent, selective and orally active factor Xa inhibitor with a Ki of 0.19 nM. Razaxaban hydrochloride exhibits excellent selectivity (>5000-fold) for factor Xa over other related serine proteases. Razaxaban hydrochloride is also a potent thrombin inhibitor with a Ki of 540 nM. Razaxaban hydrochloride has strongly antithrombotic activity.
For research use only. We do not sell to patients.
- CAS No.: 405940-76-3
- Formula: C24H21ClF4N8O2
- Molecular Weight:564.92
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
Ki: 0.19 nM (Factor Xa); 540 nM (Thrombin)[1]
In Vitro
Razaxaban (compound 11d) shows good Caco-2 permeability[1].
The anticoagulant activity of Razaxaban (compound 11d) is evaluated in the in vitro human plasma activated partial thromboplastin time (aPTT) and human prothrombin time (PT) assays. Razaxaban shows a doubling of aPTT and PT at 6.1 µM and 2.1 µM, respectively. The human and rabbit plasma protein binding are found to be 90.5% and 93.4%, respectively, using equilibrium dialysis. Razaxaban is found to have similar affinity in the rabbit factor Xa assay with a Ki of 0.16 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rabbit arterio-venous shunt thrombosis model[1]
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Dosage:0.21 mg/kg/hour, 0.7 mg/kg/hour, 2.1 mg/kg/hour, 9.4 mg/kg/hour
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Administration:Intravenous injection
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Result:Inhibited thrombus formation in a dose-dependent manner with an ID50 of 1.6 µmol/kg/h.
Chemical Information
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CAS No. 405940-76-3
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Molecular Weight 564.92
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Formula C24H21ClF4N8O2
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SMILES
O=C(C1=CC(C(F)(F)F)=NN1C2=CC3=C(ON=C3N)C=C2)NC4=CC=C(N5C=CN=C5CN(C)C)C=C4F.[H]Cl
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Synonyms
BMS 561389 hydrochloride; DPC 906 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Razaxaban hydrochloride Related Classifications
HY-11091 Related Classifications
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