1. Metabolic Enzyme/Protease
  2. Factor Xa
    Thrombin
  3. Razaxaban hydrochloride

Razaxaban hydrochloride (Synonyms: BMS 561389 hydrochloride; DPC 906 hydrochloride)

Cat. No.: HY-11091
Handling Instructions

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.

Razaxaban hydrochloride Chemical Structure

Razaxaban hydrochloride Chemical Structure

CAS No. : 405940-76-3

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Description

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[1].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Razaxaban (Compound 11d; 0.21-9.4 mg/kg/hour; intravenous injection) inhibits thrombus formation in a dose-dependent manner with an ID50 of 1.6 µmol/kg/h in the rabbit arterio-venous shunt thrombosis model[1].

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.
Molecular Weight

564.92

Formula

C₂₄H₂₁ClF₄N₈O₂

CAS No.
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

RazaxabanBMS 561389DPC 906BMS561389BMS-561389DPC906DPC-906Factor XaThrombinFxaAntithromboticanticoagulationoralbioavailabilityplasmaInhibitorinhibitorinhibit

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Razaxaban hydrochloride
Cat. No.:
HY-11091
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