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
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Ki: 0.19 nM (Factor Xa); 540 nM (Thrombin)[1]
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Rabbit arterio-venous shunt thrombosis model[1]
-
Dosage:0.21 mg/kg/hour, 0.7 mg/kg/hour, 2.1 mg/kg/hour, 9.4 mg/kg/hour
-
Administration:Intravenous injection
-
Result:Inhibited thrombus formation in a dose-dependent manner with an ID50 of 1.6 µmol/kg/h.
Chemical Information
-
CAS No. 405940-76-3
-
Molecular Weight 564.92
-
Formula C24H21ClF4N8O2
-
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
-
Synonyms
BMS 561389 hydrochloride; DPC 906 hydrochloride
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
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)