產(chǎn)品描述: | JNJ0966 is a highly selective MMP-9 zymogen inhibitor with an IC50 of 440 nM |
靶點(diǎn): |
IC50: 440 nM (MMP-9 zymogen);MMP |
體外研究: |
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 |
體內(nèi)研究: |
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 |
參考文獻(xiàn): |
1. Scannevin RH, et al. Discovery of a highly selective chemical inhibitor of matrix metalloproteinase-9 (MMP-9) thatallosterically inhibits zymogen activation. J Biol Chem. 2017 Oct 27;292(43):17963-17974. |
溶解性: |
Soluble in DMSO |
保存條件: |
-20°C |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
2.774 ml |
13.872 ml |
27.743 ml |
5 mM |
0.555 ml |
2.774 ml |
5.549 ml |
10 mM |
0.277 ml |
1.387 ml |
2.774 ml |
50 mM |
0.055 ml |
0.277 ml |
0.555 ml |
|
注意: |
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