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

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

目录号: HY-11091

Razaxaban hydrochloride (BMS 561389 hydrochloride) 是一种高效,选择性和口服活性的 factor Xa 抑制剂,Ki 为 0.19 nM。Razaxaban hydrochloride 对 factor Xa 的选择性优于其他相关丝氨酸蛋白酶 (> 5000 倍)。Razaxaban hydrochloride 也是一种有效的凝血酶抑制剂,Ki 为 540 nM。Razaxaban hydrochloride 具有很强的抗血栓形成活性。

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Razaxaban hydrochloride Chemical Structure

Razaxaban hydrochloride Chemical Structure

CAS No. : 405940-76-3

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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.





Room temperature in continental US; may vary elsewhere.


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

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Razaxaban hydrochloride 相关分类

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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Help & FAQs
  • 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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