JNJ0966 是高选择性MMP-9酶原抑制剂，其IC50=440 nM。

JNJ0966 is a highly selective MMP-9 zymogen inhibitor (IC50: 440 nM).

The activations of proMMP-1, proMMP-2, and proMMP-3 are not significantly different in the presence or absence of 10 μM 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].

JNJ0966 was efficacious in reducing disease severity in a mouse experimental autoimmune encephalomyelitis model. 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 (~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 (~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].

315705-75-0

C16H16N4O2S2

360.45

DMSO:150 mg/mL(416.15 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years