JNJ0966

315705-75-0

C16H16N4O2S2

DMSO : 100 mg/mL (277.43 mM; Need ultrasonic); H2O : < 0.1 mg/mL (insoluble)

Metabolic Enzyme/Protease

JNJ0966 is a highly selective MMP-9 zymogen inhibitor with an IC₅₀ of 440 nM. IC50 & Target: IC50: 440 nM (MMP-9 zymogen)^[1] In Vitro: JNJ0966 is a highly selective MMP-9 zymogen inhibitor with an IC₅₀ of 440 nM. The activations of proMMP-1, proMMP-2, and proMMP-3 are not significantly different in the presence or absence of 10 uM JNJ0966, whereas proMMP-9 activation by trypsin is significantly attenuated by JNJ0966. The addition of JNJ0966 to the reaction results in a significant reduction in fully processed MMP-9 and an apparent accumulation of the intermediate species^[1]. In Vivo: The exposures of JNJ0966 are dose-dependent, with plasma and brain concentrations for the 10-mg/kg dose of 77.5+/-31.1 ng/mL (215 nM) and 481.6+/-162.5 ng/g (ca.1336 nM), respectively, whereas the 30-mg/kg dose achieves 293.6+/-118.4 ng/mL (815 nM) in plasma and 1394.0+/-649.1 ng/g (ca.3867 nM) in brain. JNJ0966 is preferentially partitioned in brain, with brain/plasma ratios of 6.2 for the 10-mg/kg dose and 4.7 for the 30-mg/kg dose^[1].