Razaxaban hydrochloride

Modify Date: 2024-01-14 09:40:54

Razaxaban hydrochloride Structure
Razaxaban hydrochloride structure
Common Name Razaxaban hydrochloride
CAS Number 405940-76-3 Molecular Weight 564.92300
Density N/A Boiling Point 654.8ºC at 760 mmHg
Molecular Formula C24H21ClF4N8O2 Melting Point N/A
MSDS N/A Flash Point 349.8ºC

 Use of 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[1].

 Names

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
Synonym More Synonyms

 Razaxaban hydrochloride Biological Activity

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].
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

[1]. Quan ML, et al. Discovery of 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4- [(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor. J Med Chem. 2005 Mar 24;48(6):1729-44.

 Chemical & Physical Properties

Boiling Point 654.8ºC at 760 mmHg
Molecular Formula C24H21ClF4N8O2
Molecular Weight 564.92300
Flash Point 349.8ºC
Exact Mass 564.14100
PSA 124.25000
LogP 5.36930

 Safety Information

Hazard Codes Xi

 Synonyms

DPC 906
Razaxaban Hydrochloride
Razaxaban HCl
UNII-7CLJ1MEZ8V