1. Metabolic Enzyme/Protease
  2. MMP
  3. JNJ0966

JNJ0966 

Cat. No.: HY-103482 Purity: 98.01%
Handling Instructions

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

For research use only. We do not sell to patients.

JNJ0966 Chemical Structure

JNJ0966 Chemical Structure

CAS No. : 315705-75-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 95 In-stock
Estimated Time of Arrival: December 31
1 mg USD 70 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
25 mg USD 390 In-stock
Estimated Time of Arrival: December 31
50 mg USD 700 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1250 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target

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

In Vitro

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].

In Vivo

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].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

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

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7743 mL 13.8715 mL 27.7431 mL
5 mM 0.5549 mL 2.7743 mL 5.5486 mL
10 mM 0.2774 mL 1.3872 mL 2.7743 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

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

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

360.45

Formula

C₁₆H₁₆N₄O₂S₂

CAS No.

315705-75-0

SMILES

CC1=C(C2=CSC(NC3=C(OC)C=CC=C3)=N2)SC(NC(C)=O)=N1

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
JNJ0966
Cat. No.:
HY-103482
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JNJ0966

Cat. No.: HY-103482