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Merck
모든 사진(1)

Key Documents

SML2845

Sigma-Aldrich

Betrixaban

≥98% (HPLC)

동의어(들):

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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About This Item

실험식(Hill 표기법):
C23H22ClN5O3
CAS Number:
Molecular Weight:
451.91
MDL number:
UNSPSC 코드:
12352200
NACRES:
NA.77

Quality Level

분석

≥98% (HPLC)

형태

powder

색상

white to beige

solubility

DMSO: 2 mg/mL, clear

저장 온도

2-8°C

SMILES string

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

생화학적/생리학적 작용

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.

픽토그램

Health hazardExclamation mark

신호어

Warning

유해 및 위험 성명서

예방조치 성명서

Hazard Classifications

Acute Tox. 4 Oral - STOT RE 2

표적 기관

Blood

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


시험 성적서(COA)

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문서 라이브러리 방문

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
Deborah M Siegal et al.
Drug discovery today, 19(9), 1465-1470 (2014-06-01)
Target-specific oral anticoagulants (TSOACs) provide safe and effective anticoagulation for the prevention and treatment of thrombosis in a variety of clinical settings by interfering with the activity of thrombin (dabigatran) or factor Xa (rivaroxaban, apixaban, edoxaban, betrixaban). Although TSOACs have
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
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

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