产品说明书
JNJ0966
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同义名 : | - |
| CAS号 : | 315705-75-0 | |
| 货号 : | A984976 | |
| 分子式 : | C16H16N4O2S2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 360.454 | |
| MDL号 : | MFCD02045222 | |
| 存储条件： |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(291.3 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Matrix metalloproteinases (MMP) are a family of proteolytic enzymes that participate in tissue remodeling and molecular signaling. MMP-9, a member of the MMP family, is excessively expressed in many human diseases. JNJ0966 is a selective inhibitor of MMP-9 zymogen (IC50 = 440nM) that inhibits subsequent generation of the catalytically active enzyme. It showed no effect on the catalytic activity of MMP-1, MMP-2, MMP-3, MMP-9, or MMP-14, and did not inhibit the activation of MMP-2 zymogen. The addition of JNJ0966 (10μM) resulted in a significant reduction in fully processed MMP-9. The administration of JNJ0966 at 10 and 30mg/kg via oral gavage reduced motor deficits in a mouse model of experimental autoimmune encephalomyelitis (EAE). JNJ0966 also partitioned into the brain of EAE mice with brain/plasma ratios of 6.2 for the 10mg/kg dose and 4.7 for the 30mg/kg dose[1]. | ||
| 作用机制 | JNJ0966 interacts with a structural pocket in proximity to the MMP-9 zymogen cleavage site near Arg-106[1]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.77mL 0.55mL 0.28mL |
13.87mL 2.77mL 1.39mL |
27.74mL 5.55mL 2.77mL |
| 参考文献 |
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