Vorapaxar (MK-5348) - Moligand™, 10mM in DMSO , Antagonist of PAR1, CAS No.618385-01-6, Antagonist of PAR1

CAS: 618385-01-6 Cat. No.: V408351 Peso molecular: 492.58 Número EC: 612-523-7 PubChem CID: 10077130

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

SCH 530348 | Carbamic acid, N-[(1R,3aR,4aR,6R,8aR,9S,9aS)-9-[(1E)-2-[5-(3-fluorophenyl)-2-pyridinyl]ethenyl]dodecahydro-1-methyl-3-oxonaphtho[2,3-c]furan-6-yl]-, ethyl ester

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Vorapaxar (MK-5348) Vorapaxar (SCH 530348, MK-5348) is a potent and orally active thrombin receptor (PAR-1) antagonist with K i of 8.1 nM.
In vitro

SCH 530348 is a synthetic tricyclic 3-phenylpyridine and an orally active himbacine-based thrombin-receptor antagonist. SCH 530348 shows potent inhibition of thrombin-induced platelet aggregation with an IC50 of 47 nM and haTRAP-induced platelet aggregation with an IC50 of 25 nM, whereas it shows no inhibition of platelet aggregation induced by other agonists such as ADP, collagen and a PAR-4 agonist peptide. SCH 530348 also has no affect on the prothrombin time (PT), partial thromboplastin time (PTT), or activated partial thromboplastin time (aPTT). Moreover, SCH 530348 causes no increase in the bleeding time or in surgical bleeding compared with inactive control. SCH530348 is found to be selective for PAR-1 when tested over a number of ion channels and receptors, including PAR-4 receptor.

In vivo

SCH 530348 is well absorbed in rat (68%; 10 mg/kg) and in monkey (82%; 1 mg/kg) models. T_max is observed at about 3 h in rats and 1 h in monkeys. The elimination half-life is 5.1 h in rats and 13 h in monkeys. The oral bioavailability is 33% in rats and 86% in monkeys. In preclinical studies in cynomolgus monkey platelets, oral administration of SCH 530348 at a dose greater than 0.1 mg/kg resulted in 100% inhibition of thrombin-receptor agonist peptide (TRAP)-induced platelet aggregation for 24 h with partial recovery occurring at 48 h.
Cell Data

cell lines：JVM13

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Sinónimos

SCH 530348 | Carbamic acid, N-[(1R, 3aR, 4aR, 6R, 8aR, 9S, 9aS)-9-[(1E)-2-[5-(3-fluorophenyl)-2-pyridinyl]ethenyl]dodecahydro-1-methyl-3-oxonaphtho[2, 3-c]furan-6-yl]-, ethyl ester

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Vorapaxar (SCH 530348, MK-5348) is a potent and orally active thrombin receptor (PAR-1) antagonist with K_i of 8.1 nM.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

ANTAGONIST

Mecanismo de acción

Antagonist of PAR1

Propiedades del producto

• ALogP: 5.261
• Recuento HBD: 1
• Enlace rotable: 6

Nombres e identificadores

• Isómeros SMILES: CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]3[C@H]([C@H]2/C=C/C4=NC=C(C=C4)C5=CC(=CC=C5)F)[C@H](OC3=O)C
• PubChem CID: 10077130
• Peso molecular: 492.58

Objetivos asociados (humanos)

F2R Tclin Proteinase-activated receptor 1 (13 Activities)

Discover Target: F2R

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

Propiedades químicas y físicas

• DMSO (mg/ml) Solubilidad máxima: 99
• DMSO (mM) Solubilidad máxima: 200.9825815
• Agua (mg/ml) Solubilidad máxima: ＜1