Darexaban - 10mM in DMSO , Coagulation factor X inhibitor, CAS No.365462-23-3, Coagulation factor X inhibitor

CAS: 365462-23-3 Cat. No.: D655067 분자식: C₂₇H₃₀N₄O₄ 분자량: 474.6 PubChem CID: 9912771

등급 & 순도 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

개요

Darexaban (YM150) is a potent, selective and orally active factor Xa (FXa) inhibitor with an IC 50 of 54.6 nM. Darexaban shows high selectivity against other related serine proteases, such as trypsin, thrombin , and kallikrein. Darexaban has anticoagulant and antithrombotic effects .

In Vitro

Darexaban is an oral direct factor Xa (FXa) inhibitor that is rapidly and extensively metabolized into its glucuronide conjugate (YM-222714) post-administration. Darexaban competitively and selectively inhibits human FXa, and also inhibits the prothrombin activation induced by prothrombinase complex or whole blood clot with similar potency to free FXa. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In mice, Darexaban inhibits FXa activity in plasma with an ED 50 value of 24.8 mg/kg. Darexaban prolonges prothrombin time (PT) at 3 mg/kg. In a pulmonary thromboembolism (PE) mouse model, Darexaban dose-dependently reduces the mortality rate, significantly so at 10 mg/kg. In a FeCl3-induced venous thrombosis (VT) mouse model, Darexaban (0.3-10 mg/kg) dose-dependently decreases the thrombus protein content, significantly so at doses of 3 mg/kg or higher. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

사양

사양 및 순도

10mM in DMSO

생화학 및 생리적 메커니즘

Darexaban (YM150) is a potent, selective and orally active factor Xa (FXa) inhibitor with an IC 50 of 54.6 nM. Darexaban shows high selectivity against other related serine proteases, such as trypsin, thrombin , and kallikrein. Darexaban has anticoagulant

보관 조건

Store at -80°C

배송

Dry ice packs + Cold packs

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작업 유형

INHIBITOR

작동 메커니즘

Coagulation factor X inhibitor

제품 특성

ALogP

3.5

이름과 식별자

이성체 SMILES

CN1CCCN(CC1)C2=CC=C(C=C2)C(=O)NC3=C(C=CC=C3O)NC(=O)C4=CC=C(C=C4)OC

대체 CAS

365462-23-3

PubChem CID

9912771

MeSH 용어

darexaban;N-(2-hydroxy-6-(4-methoxybenzamido)phenyl)-4-(4-methyl-1,4-diazepan-1-yl)benzamide;YM 150;YM-150;YM150 cpd

분자량

474.6

관련 대상(인간)

F10 Tclin Coagulation factor X (2 Activities)

Discover Target: F10

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)