| Identification | Back Directory | [Name]
N-[1-[[(Cyanomethyl)amino]carbonyl]cyclohexyl]-4-[2-(4-methyl-1-piperazinyl)-4-thiazolyl]benzamide | [CAS]
294623-49-7 | [Synonyms]
L 006235
I-006,235
L-006235;L 006235;L006235
N-(1-((cyanomethyl)carbamoyl)cyclohexyl)-4-(2-(4-methylpiperazin-1-yl)thiazol-4-yl)benzamide
N-[1-(cyanomethylcarbamoyl)cyclohexyl]-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
N-[1-[[(Cyanomethyl)amino]carbonyl]cyclohexyl]-4-[2-(4-methyl-1-piperazinyl)-4-thiazolyl]benzamide
Benzamide, N-[1-[[(cyanomethyl)amino]carbonyl]cyclohexyl]-4-[2-(4-methyl-1-piperazinyl)-4-thiazolyl]- | [Molecular Formula]
C24H30N6O2S | [MOL File]
294623-49-7.mol | [Molecular Weight]
466.6 |
| Chemical Properties | Back Directory | [density ]
1.31±0.1 g/cm3(Predicted) | [storage temp. ]
Store at +4°C | [solubility ]
<46.66mg/ml in DMSO | [form ]
solid | [pka]
12.07±0.20(Predicted) | [color ]
White |
| Hazard Information | Back Directory | [Uses]
L 006235 is a cathepsin K inhibitor, which displays greater than 4000-fold selectivity against the lysosomal/endosomal antitargets cathepsin B, L, and S. | [Biological Activity]
l-006235 is a potent and selective inhibitor of cathepsin k. | [in vitro]
after dilution of l-006235 to 0.05 nm, the cathepsin k enzyme activity was initially inhibited, but slowly recovered with a first-order rate constant of 0.023 s-1. the final steady-state enzyme activity was 80-90% that of control, suggesting the complete reversibility of the l-006235-cathepsin k complex. l-006235 was found to be not a substrate for the nitrilase activity of cat k [1]. | [in vivo]
l-006235 was orally bioavailable in rats, with a terminal half-life of over 3 h. l-006235 was orally dosed in ovariectomized rhesus monkeys once per day for 7 days. results showed that collagen breakdown products were dose-dependently reduced by up to 76%. plasma concentrations of l-006235 above the bone resorption ic50 after 24 h indicated a correlation between functional cellular and in vivo assays. these findings suggested that the inhibition of collagen breakdown by cathepsin k inhibitors, such as l-006235, might be useful in osteoporosis and other indications involving bone resorption [1]. | [IC 50]
0.25 nm | [storage]
Store at 4°C | [References]
[1] palmer jt,bryant c,wang dx et al. design and synthesis of tri-ring p3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin k. j med chem.2005 dec 1;48(24):7520-34. |
|
|