JNJ0966
JNJ0966 Basic information
- Product Name:
- JNJ0966
- Synonyms:
-
- JNJ0966
- N-[2-[(2-Methoxyphenyl)amino]-4'-methyl[4,5'-bithiazol]-2'-yl]acetamide
- JNJ0966;JNJ 0966;JNJ-0966;315705-75-0
- Acetamide, N-[2-[(2-methoxyphenyl)amino]-4'-methyl[4,5'-bithiazol]-2'-yl]-
- Inhibitor,Matrix metalloproteinases,JNJ0966,JNJ 0966,MMP,JNJ-0966,inhibit
- N-(2-((2-Methoxyphenyl)amino)-4'-methyl-[4,5'-bithiazol]-2'-yl)acetamide
- JNJ0966, 10 mM in DMSO
- CAS:
- 315705-75-0
- MF:
- C16H16N4O2S2
- MW:
- 360.45
- Product Categories:
-
- API
- Mol File:
- 315705-75-0.mol
JNJ0966 Chemical Properties
- 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
JNJ0966 Usage And Synthesis
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 zymogen, and has no effect on MMP-1, MMP-2, MMP-3, MMP-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
JNJ0966Supplier
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