|N-(2-((2-甲氧基苯基)氨基)-4'-甲基-[4,5'-噻唑]-2'-基)乙酰胺|CsnPharm

CAS No.: 315705-75-0

JNJ0966 Catalog No. CSN25429

Synonyms: Jnj0966

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.

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400-920-2911

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技术信息

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].
参考文献

[1] Scannevin RH, Alexander R, Haarlander TM, Burke SL, Singer M, Huo C, Zhang YM, Maguire D, Spurlino J, Deckman I, Carroll KI, Lewandowski F, Devine E, Dzordzorme K, Tounge B, Milligan C, Bayoumy S, Williams R, Schalk-Hihi C, Leonard K, Jackson P, Todd M, Kuo LC, Rhodes KJ. Discovery of a highly selective chemical inhibitor of matrix metalloproteinase-9 (MMP-9) that allosterically inhibits zymogen activation. J Biol Chem. 2017 Oct 27;292(43):17963-17974. doi: 10.1074/jbc.M117.806075

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.7743 mL
- 13.8714 mL
- 27.7428 mL
- 5 mM
- 0.5549 mL
- 2.7743 mL
- 5.5486 mL
- 10 mM
- 0.2774 mL
- 1.3871 mL
- 2.7743 mL

技术信息

CAS号

315705-75-0

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H16N4O2S2

运输

蓝冰

分子量

360.45

别名

Jnj0966

溶解度

DMSO	72.0 mg/mL (199.7 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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