Protease-Activated Receptor-1 antagonist 2

Cat. No.: HY-143314: Ficha de datos Instrucciones de manejo
FAQs
Technical Support

Protease-Activated Receptor-1 antagonist 2 is an orally active protease-activated receptor-1 (PAR-1) antagonist, with an IC₅₀ value of 7 nM. Protease-Activated Receptor-1 antagonist 2 has favorable pharmacokinetic properties which is useful in the research of cardiovascular disease (CVD), such as atherosclerosis and restenosis.

Para uso exclusivo en investigación. No vendemos a pacientes.

Protease-Activated Receptor-1 antagonist 2 Estructura química

No. CAS : 1454588-34-1

Tamaño		Stock
MOQ		Minimum order quantity
50 mg		Obtener un presupuesto
100 mg		Obtener un presupuesto
250 mg		Obtener un presupuesto
Other size		Obtener un presupuesto

* Seleccione Cantidad antes de agregar artículos.

This product is a controlled substance and not for sale in your territory.

Recomendaciones destacadas

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas Protease Activated Receptor (PAR):

Ver todas las isoformas

PAR1 PAR2 PAR4

Actividad biológica
Pureza y Documentación
Referencias
Revisión del cliente

Descripciòn

IC₅₀ & Target

PAR1

7 nM (IC₅₀)

In Vivo

Protease-Activated Receptor-1 antagonist 2 (Compound 14, 1 mpk i.v. dosing, rat and monkey) inhibits PAR-1 with an IC₅₀ of 7 nM^[1].
Protease-Activated Receptor-1 antagonist 2 (10-50 mpk, p.o., rat) increase s both the AUC_{0?24 h} and C_max in a dose-dependent manner^[1].
Protease-Activated Receptor-1 antagonist 2 doesn’t elicit any prominent liver bioactivation or tissue toxicity signals up to an AUC of 44 μM?h^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Rat, monkey, dog^[1]

Dosage:

i.v. (3 mpk for rat, 0.3 mpk for dog and monkey), p.o (10 mpk for rat, 1 mpk for dogs and monkey)

Administration:

i.v., p.o (Pharmacokinetic Analysis)

Result:

Pharmacokinetic parameters.

compound	FLIPR IC₅₀ (nM)	MRT (R;^c D; ^d M^e)	F% (R;^f D; ^g M^h)	predicted human MRT
Protease-Activated Receptor-1 antagonist 2	7	1.9; 18; 25	54; 100; 37	20−48

Peso molecular

423.46

Fòrmula

C₂₄H₂₃F₂N₃O₂

No. CAS

1454588-34-1

SMILES

[H][C@]12[C@H]([C@@H](C(F)(C[C@]1(C(O[C@@H]2C)=O)N)F)C)/C=C/C3=CC=C(C=N3)C4=CC=CC=C4C#N

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[1]. Mihirbaran Mandal, et al. Lead Optimization to Advance Protease-Activated Receptor-1 Antagonists in Early Discovery. J Med Chem. 2022 Apr 14;65(7):5575-5592. [Content Brief]