BMS-262084

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CAS:253174-92-4
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CAS:253174-92-4
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BMS-262084 Basic information
Product Name:BMS-262084
Synonyms:BMS-262084;CHEMBL71037;I0IR71971G;UNII-I0IR71971G;(2S,3R)-1-[4-(tert-butylcarbamoyl)piperazine-1-carbonyl]-3-[3-(diaminomethylideneamino)propyl]-4-oxoazetidine-2-carboxylicacid;2-Azetidinecarboxylic acid, 3-[3-[(aminoiminomethyl)amino]propyl]-1-[[4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperazinyl]carbonyl]-4-oxo-, (2S,3R)-
CAS:253174-92-4
MF:C18H31N7O5
MW:425.48
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Mol File:253174-92-4.mol
BMS-262084 Structure
BMS-262084 Chemical Properties
density 1.46±0.1 g/cm3(Predicted)
form Solid
pka2.96±0.40(Predicted)
color White to off-white
Safety Information
MSDS Information
BMS-262084 Usage And Synthesis
UsesBMS-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
BMS-262084 Preparation Products And Raw materials
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