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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $55 | In Stock | |
2 mg | $75 | In Stock | |
5 mg | $97 | In Stock | |
10 mg | $147 | In Stock | |
25 mg | $322 | In Stock | |
50 mg | $578 | In Stock | |
100 mg | $833 | In Stock | |
500 mg | $1,690 | In Stock | |
1 mL x 10 mM (in DMSO) | $76 | In Stock |
Description | JNJ0966 is a highly selective [MMP-9 zymogen] inhibitor with an IC50 of 440 nM. |
Targets&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. |
Molecular Weight | 360.45 |
Formula | C16H16N4O2S2 |
Cas No. | 315705-75-0 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 150 mg/mL (416.15 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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