Razaxaban hydrochloride

Modify Date: 2025-09-21 08:58:51

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
InChIKey CASCTHHMARGRLB-UHFFFAOYSA-N
SMILES CN(C)Cc1nccn1-c1ccc(NC(=O)c2cc(C(F)(F)F)nn2-c2ccc3onc(N)c3c2)c(F)c1.Cl

 Safety Information

Hazard Codes Xi

 Synonyms

DPC 906
Razaxaban Hydrochloride
Razaxaban HCl
UNII-7CLJ1MEZ8V
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