ChemicalBook--->CAS DataBase List--->253174-92-4

253174-92-4

253174-92-4 Structure

253174-92-4 Structure
IdentificationBack Directory
[Name]

BMS-262084
[CAS]

253174-92-4
[Synonyms]

BMS-262084
I0IR71971G
CHEMBL71037
UNII-I0IR71971G
[Molecular Formula]

C18H31N7O5
[MDL Number]

MFCD34567230
[MOL File]

253174-92-4.mol
[Molecular Weight]

425.48
Chemical PropertiesBack Directory
[density ]

1.46±0.1 g/cm3(Predicted)
[form ]

Solid
[pka]

2.96±0.40(Predicted)
[color ]

White to off-white
Hazard InformationBack Directory
[Uses]

BMS-262084 is a potent, selective and irreversible inhibitor of factor XIa, with an IC50 of 2.8 nM against human factor XIa. BMS-262084 also inhibits human tryptase (IC50=5 nM). BMS-262084 exhibits antithrombotic effects[1][2].
[in vivo]

BMS-262084 (2-12 mg/kg + 2-12 mg/kg/h; i.v.) reduces carotid artery thrombus weight and improves both vessel patency and integrated flow in rats[1].

Animal Model:Male Sprague Dawley rats (310-390 g) were induced venous thrombosis by FeCl2[1]
Dosage:2 mg/kg + 2 mg/kg/h, 6 mg/kg + 6 mg/kg/h, 12 mg/kg + 12 mg/kg/h
Administration:I.v. 10 min before FeCl2 application
Result:Reduced carotid artery thrombus weight by 73% at the dose of 12 mg/kg + 12 mg/kg/h.
Improved both vessel patency and integrated flow.
[References]

[1] Schumacher WA, et, al. Antithrombotic and hemostatic effects of a small molecule factor XIa inhibitor in rats. Eur J Pharmacol. 2007 Sep 10;570(1-3):167-74. DOI:10.1016/j.ejphar.2007.05.043
[2] Qian X, et, al. A stereoselective synthesis of BMS-262084, an azetidinone-based tryptase inhibitor. J Org Chem. 2002 May 31;67(11):3595-600. DOI:10.1021/jo010757o
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