405940-76-3
405940-76-3 structure
- Name: Razaxaban hydrochloride
- Chemical Name: 2-(3-amino-1,2-benzoxazol-5-yl)-N-[4-[2-[(dimethylamino)methyl]imidazol-1-yl]-2-fluorophenyl]-5-(trifluoromethyl)pyrazole-3-carboxamide,hydrochloride
- CAS Number: 405940-76-3
- Molecular Formula: C24H21ClF4N8O2
- Molecular Weight: 564.92300
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Factor Xa
- Create Date: 2016-01-08 10:52:53
- Modify Date: 2024-01-14 09:40:54
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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].
| Name | 2-(3-amino-1,2-benzoxazol-5-yl)-N-[4-[2-[(dimethylamino)methyl]imidazol-1-yl]-2-fluorophenyl]-5-(trifluoromethyl)pyrazole-3-carboxamide,hydrochloride |
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| Synonyms |
DPC 906
Razaxaban Hydrochloride Razaxaban HCl UNII-7CLJ1MEZ8V |
| 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]. |
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| Related Catalog | |
| 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]. |
| 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]. 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. |
| References |
| Boiling Point | 654.8ºC at 760 mmHg |
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| Molecular Formula | C24H21ClF4N8O2 |
| Molecular Weight | 564.92300 |
| Flash Point | 349.8ºC |
| Exact Mass | 564.14100 |
| PSA | 124.25000 |
| LogP | 5.36930 |
| Hazard Codes | Xi |
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