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

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

Cat. No.: HY-11091
Instrucciones de manejo Technical Support

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.

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Razaxaban hydrochloride

Razaxaban hydrochloride Estructura química

No. CAS : 405940-76-3

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Descripciòn

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].

MedChemExpress (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].

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.
Peso molecular

564.92

Fòrmula

C24H21ClF4N8O2

No. CAS
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

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

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Referencias
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

Nombre del producto:
Razaxaban hydrochloride
Cat. No.:
HY-11091
Cantidad:
MCE Japan Authorized Agent: