| Description | JNJ0966 is a highly selective MMP-9 zymogen inhibitor (IC50: 440 nM). |
| In vitro | 在10μM JNJ0966的存在或缺席下，proMMP-1、proMMP-2和proMMP-3的激活没有显著差异，而由胰蛋白酶引发的proMMP-9激活则被JNJ0966显著抑制。添加JNJ0966后，完全处理的MMP-9显著减少，并且中间体种类明显积累[1]。 |
| In vivo | JNJ0966在减轻小鼠实验性自身免疫性脑炎模型的疾病严重性中表现出有效性。JNJ0966的暴露量是剂量依赖的，10-mg/kg剂量的血浆和大脑浓度分别为77.5±31.1 ng/mL (215 nM)和481.6±162.5 ng/g（约1336 nM），而30-mg/kg剂量在血浆中达到293.6±118.4 ng/mL (815 nM)，在大脑中达到1394.0±649.1 ng/g（约3867 nM）。JNJ0966在大脑中的分布比血浆更优，10 mg/kg剂量和30 mg/kg剂量的大脑/血浆比率分别为6.2和4.7。[1] |
| Target activity | MMP9 zymogen:440 nM |
| molecular weight | 360.45 |
| Molecular formula | C16H16N4O2S2 |
| CAS | 315705-75-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 150 mg/mL (416.15 mM) |
| References | 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. |