| Identification | Back Directory | [Name]
JNJ0966 | [CAS]
315705-75-0 | [Synonyms]
JNJ0966
JNJ0966;JNJ 0966;JNJ-0966;315705-75-0
N-[2-[(2-Methoxyphenyl)amino]-4'-methyl[4,5'-bithiazol]-2'-yl]acetamide
Acetamide, N-[2-[(2-methoxyphenyl)amino]-4'-methyl[4,5'-bithiazol]-2'-yl]- | [Molecular Formula]
C16H16N4O2S2 | [MDL Number]
MFCD02045222 | [MOL File]
315705-75-0.mol | [Molecular Weight]
360.45 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:63.34(Max Conc. mg/mL);175.72(Max Conc. mM) | [form ]
A crystalline solid | [color ]
Light brown to brown | [InChI]
1S/C16H16N4O2S2/c1-9-14(24-16(17-9)18-10(2)21)12-8-23-15(20-12)19-11-6-4-5-7-13(11)22-3/h4-8H,1-3H3,(H,19,20)(H,17,18,21) | [InChIKey]
ZADCDCMLLGDCRM-UHFFFAOYSA-N | [SMILES]
[s]1c(nc(c1c2nc([s]c2)Nc3c(cccc3)OC)C)NC(=O)C |
| Hazard Information | Back Directory | [Uses]
JNJ0966, is a highly selective MMP-9 zymogen inhibitor. | [Biological Activity]
JNJ0966 is a potent and highly selective inhibitor of matrix metalloproteinase-9 (MMP-9) zymogen activation. It appears th at JNJ0966 binds to a structural pocket in proximity to the MMP-9 zymogen cleavage site near Arg-106. JNJ0966 reduces disease severity in in a mouse experimental autoimmune encephalomyelitis (EAE) model. JNJ0966 does not inhibit activation of MMP-2 zymogenand has no effect on MMP-1MMP-2MMP-3MMP-9 or MMP-14 catalytic activity. | [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]
Store at -20°C |
|
|