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

CAS: 365462-23-3 Cat. No.: D655067 Summenformel: C₂₇H₃₀N₄O₄ Molekulargewicht: 474.6 PubChem CID: 9912771

QUALITÄT & REINHEIT 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Übersicht

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.

Spezifikationen

Spezifikationen & Reinheit

10mM in DMSO

Biochemische und physiologische Mechanismen

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

Storage

Store at -80°C

Verschickt in

Dry ice packs + Cold packs

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Aktionsart

INHIBITOR

Mechanismus der Wirkung

Coagulation factor X inhibitor

Produkteigenschaften

ALogP

3.5

Namen und Kennungen

Isomere SMILES

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

Alternative CAS-Nummer

365462-23-3

PubChem CID

9912771

MeSH-Eintrag

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

Molekulargewicht

474.6

Zugehörige Ziele (menschlich)

F10 Tclin Coagulation factor X (2 Activities)

Discover Target: F10

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