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JNJ0966

CAS No. : 315705-75-0

產(chǎn)品活性：JNJ0966 is a highly selective MMP-9 zymogen inhibitor with an IC₅₀ of 440 nM.

研究領(lǐng)域：Metabolic Enzyme/Protease

作用靶點(diǎn)：MMP

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 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.

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 (~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.

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