PD 166793

Использование

PD 166793 is a matrix metalloproteinase inhibitor in the treatment of inflammatory pathological occurrences involving blood pressure and the cardiac system.

Общее описание

A cell-permeable biphenylsulfonylvaline compound that acts as a potent inhibitor against MMP-2, -3, and -13 (IC₅₀ = 47, 12, and 8 nM, respectively) and a weaker inhibitor against AMP deaminase (20% inhibition at 0.1 μM), MMP-1, -7, -9, and -14 (IC₅₀ = 6.1, 7.2, 7.9, and 0.24 μM, respectively). Shown to offer therapeutic benefits in vivo in various animal models of heart failure and diabetes.

Биологическая активность

Broad spectrum matrix metalloprotease (MMP) inhibitor. Displays high affinity for MMP-2, -3 and -13 (IC 50 values are 4, 7 and 8 nM respectively) and exhibits > 750-fold selectivity over MMP-1, -7 and -9. Attenuates left ventricular remodelling and dysfunction in rat model of heart failure.