JNJ0966 |
Catalog No.GC32792
One-Click Copy Product Info
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JNJ0966 est un inhibiteur hautement sélectif du zymogène MMP-9 avec une IC50 de 440 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 315705-75-0
Sample solution is provided at 25 µL, 10mM.
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JNJ0966 is a highly selective MMP-9 zymogen inhibitor with an IC50 of 440 nM.
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].
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].
[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.
Cell experiment: | 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]. |
Animal experiment: | 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]. |
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. | |
| Cas No. | 315705-75-0 | SDF | |
| Canonical SMILES | CC1=C(C2=CSC(NC3=C(OC)C=CC=C3)=N2)SC(NC(C)=O)=N1 | ||
| Formula | C16H16N4O2S2 | M.Wt | 360.45 |
| Solubility | DMSO : 100 mg/mL (277.43 mM);Water : < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7743 mL | 13.8715 mL | 27.7431 mL |
| 5 mM | 554.9 μL | 2.7743 mL | 5.5486 mL |
| 10 mM | 277.4 μL | 1.3872 mL | 2.7743 mL |
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g
μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)