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

CAS: 365462-23-3 Cat. No.: D655067 Fórmula: C₂₇H₃₀N₄O₄ Peso molecular: 474.6 PubChem CID: 9912771

GRAU & PUREZA 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Visão geral

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.

Especificações

Especificações e pureza

10mM in DMSO

Mecanismos bioquímicos e fisiológicos

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

Condições de armazenamento de armazenamento

Store at -80°C

Enviado em

Dry ice packs + Cold packs

Este produto requer transporte de cadeia fria. Serviços terrestres e outros serviços econômicos não estão disponíveis.

Tipo de ação

INHIBITOR

Mecanismo de ação

Coagulation factor X inhibitor

Propriedades do produto

ALogP

3.5

Nomes e identificadores

SMILES isoméricas

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

CAS alternativo

365462-23-3

PubChem CID

9912771

Termos de entrada MeSH

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

Peso molecular

474.6

Alvos associados (humanos)

F10 Tclin Coagulation factor X (2 Activities)

Discover Target: F10

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