SML2845
Betrixaban
≥98% (HPLC)
别名:
MK-4448, MLN1021, N-(5-Chloro-2-pyridinyl)-2-[[4-[(dimethylamino)iminomethyl]benzoyl]amino]-5-methoxybenzamide, N-(5-Chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, PRT-054021, PRT054021
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5 MG
$136.00
25 MG
$548.00
About This Item
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质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
ClC1=CN=C(C=C1)NC(C2=C(NC(C3=CC=C(C(N(C)C)=N)C=C3)=O)C=CC(OC)=C2)=O
InChI
1S/C23H22ClN5O3/c1-29(2)21(25)14-4-6-15(7-5-14)22(30)27-19-10-9-17(32-3)12-18(19)23(31)28-20-11-8-16(24)13-26-20/h4-13,25H,1-3H3,(H,27,30)(H,26,28,31)
InChI key
XHOLNRLADUSQLD-UHFFFAOYSA-N
生化/生理作用
Betrixaban is an orally active, active site-targeting, highly potent and selective factor Xa (fXa) inhibitor (IC50 = 1.5 nM; Ki = 117 pM) with much reduced plasma kallikrein inhibitory activity (IC50 = 6.3 μM) and little potency against thrombin, trypsin, t-PA, aPC or plasmin inhibition (IC50 >10 μM). Betrixaban exhibits good pharmacokinetic properties and anticoagulant efficacy against various thromboembolism (VTE) events in vivo.
Orally active, active site-targeting, highly potent and selective factor Xa (fXa) inhibitor with anticoagulant efficacy against thromboembolism (VTE) events in vivo.
警示用语：
Warning
危险声明
危险分类
Acute Tox. 4 Oral - STOT RE 2
靶器官
Blood
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
Romain Siriez et al.
Thrombosis and haemostasis, 118(7), 1203-1214 (2018-06-12)
Betrixaban is a novel direct oral factor Xa inhibitor approved by the Food and Drug Administration for prophylaxis of venous thromboembolism in adult patients hospitalized for an acute illness at risk for thromboembolic complications. Assessment of the anti-coagulant effect of
Menno V Huisman et al.
European heart journal supplements : journal of the European Society of Cardiology, 20(Suppl E), E12-E15 (2018-07-07)
Venous thromboembolism (VTE) in acute medically ill patients is a leading cause of in-hospital morbidity and mortality. A majority of these VTE events occur post-discharge, and patients remain at increased VTE risk for up to 3 months post-discharge. Recent clinical trials
Penglie Zhang et al.
Bioorganic & medicinal chemistry letters, 19(8), 2179-2185 (2009-03-20)
Systematic SAR studies of in vitro factor Xa inhibitory activity around compound 1 were performed by modifying each of the three phenyl rings. A class of highly potent, selective, efficacious and orally bioavailable direct factor Xa inhibitors was discovered. These
Emmanuel J Favaloro et al.
Seminars in thrombosis and hemostasis, 41(2), 208-227 (2015-02-24)
A new generation of antithrombotic agents has recently emerged. These provide direct inhibition of either thrombin (factor IIa [FIIa]) or FXa, and are increasingly replacing the classical anticoagulants (heparin and coumarins such as warfarin) in clinical practice for a variety
Meyer Michel Samama et al.
Clinics in laboratory medicine, 34(3), 503-517 (2014-08-30)
New oral factor Xa inhibitors are intended to progressively substitute the oral vitamin K antagonists and parenteral indirect inhibitors of factor Xa in the prevention and treatment of venous and arterial thromboembolic episodes. This article focuses on the main clinical
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