Powder: -20°C for 3 years | In solvent: -80°C for 1 year
JNJ0966 is a highly selective MMP-9 zymogen inhibitor (IC50: 440 nM).
説明 | JNJ0966 is a highly selective MMP-9 zymogen inhibitor (IC50: 440 nM). |
ターゲット&IC50 | MMP9 zymogen:440 nM |
In vitro | 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]. |
In vivo | JNJ0966 demonstrated effectiveness in alleviating the severity of disease in a mouse model of experimental autoimmune encephalomyelitis. Its effectiveness is dose-dependent, showing plasma and brain concentrations of 77.5±31.1 ng/mL (215 nM) and 481.6±162.5 ng/g (~1336 nM) at a 10-mg/kg dose, and 293.6±118.4 ng/mL (815 nM) in plasma and 1394.0±649.1 ng/g (~3867 nM) in the brain at a 30-mg/kg dose, respectively. Moreover, JNJ0966 exhibits a preference for accumulation in the brain, evidenced by brain/plasma ratios of 6.2 at the 10 mg/kg dose and 4.7 at the 30 mg/kg dose. |
分子量 | 360.45 |
分子式 | C16H16N4O2S2 |
CAS No. | 315705-75-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 150 mg/mL(416.15 mM)
You can also refer to dose conversion for different animals. 詳細
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JNJ0966 315705-75-0 Proteases/Proteasome MMP Inhibitor Matrix metalloproteinases JNJ 0966 JNJ-0966 inhibit inhibitor