JNJ0966 is a highly selective MMP-9 zymogen inhibitor with an IC₅₀ of 440 nM.

IC50: 440 nM (MMP-9 zymogen)^[1]

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^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

360.45

C₁₆H₁₆N₄O₂S₂

315705-75-0

Room temperature in continental US; may vary elsewhere.

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

In Vitro: 

DMSO : 100 mg/mL (277.43 mM; Need ultrasonic)

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: 2.5 mg/mL (6.94 mM); Suspended solution; Need ultrasonic

  此方案可获得 2.5 mg/mL (6.94 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 2.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.5 mg/mL (6.94 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (6.94 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [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.

HT1080 cells are added (13,000 cells/well) in 10 μL of serum-free medium to the top chamber with JNJ0966. The bottom feeder tray is filled with serum-free medium supplemented with 6% fetal bovine serum and JNJ0966 and incubated at 5% CO₂, 37°C for 24 h. Calcein AM is added to the feeder layer to label cells, and fluorescence intensity from cells that have migrated to the bottom layer is quantified. Mean percentage inhibition of invasion and IC₅₀ values are calculated. Images of migrated cells are acquired on an inverted microscope with a digital camera^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Encephalomyelitis (EAE) studies are conducted in female C57Bl/6 mice age 6 to 8 weeks. Mice are randomly assigned to different groups. Vehicle-treated animals receive 20% hydroxypropyl-β-cyclodextrin via oral gavage. JNJ0966 is dissolved in 20% hydroxypropyl-β-cyclodextrin, such that animals receive 10 or 30 mg of drug per kg of body weight (mg/kg) of JNJ0966 which administered by oral gavage. All groups are dosed twice daily every day until day 17 of the study, at which point animals are sacrificed, and plasma and brain tissue are collected to analyze JNJ0966 levels using mass spectroscopy^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [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.