CP 471,474

Description

CP 471,474 is a broad-spectrum inhibitor of matrix metalloproteinases (MMPs) with IC₅₀ values of 0.7, 16, 13, and 0.9 nM for MMP-2, MMP-3, MMP-9, and MMP-13, respectively. It is selective for these MMPs over MMP-1 (IC₅₀ = 1,170 nM). CP 471,474 reduces left ventricular enlargement and decreases the incidence of cardiac rupture in mouse models of myocardial infarction when administered at doses of 120 mg/kg twice per day and 240 mg/kg per day, respectively.

Chemical Properties

White Solid

Uses

A broad spectrum inhibitor of matrix metalloproteinases that attenuates early left ventricular dilation after experimental myocardial infarction in mice. Studies show that it also inhibits cigarette smoke-induced lung inflammation and the progression of emphysema in guinea pig models.

Biochem/physiol Actions

CP-471474 is a broad spectrum inhibitor of matrix metalloproteinases. CP-471474 has a low nM IC50 efficacy for MMP-2, MMP-3, MMP-9, and MMP-13. CP-471474 has low potency against MMP-1 (IC50 > 1 uM). CP-471474 prevents left ventricular remodeling after experimental myocardial infarction in mice. CP-471474 also inhibits cigarette smoke-induced lung inflammation and the progression of emphysema in guinea pig models.