S88647 |
JNJ0966 |
源葉(MedMol) | 98% |
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 |
- 產(chǎn)品描述: JNJ0966 is a highly selective MMP-9 zymogen inhibitor with an IC50 of 440 nM
- 靶點: 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:
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:部分產(chǎn)品我司僅能提供部分信息,我司不保證所提供信息的權威性,僅供客戶參考交流研究之用。
輸入產(chǎn)品批號:
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質量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)