Protease-Activated Receptor-1 antagonist 2_product_DataBase

Bioactivity	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[1].
Target	IC50: 7 nM (PAR-1).
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 AUC0−24 h and Cmax 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]. Animal Model:
Name	Protease-Activated Receptor-1 antagonist 2
CAS	1454588-34-1
Formula	C24H23F2N3O2
Molar Mass	423.46
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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.

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