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| | N-[1-[[(Cyanomethyl)amino]carbonyl]cyclohexyl]-4-[2-(4-methyl-1-piperazinyl)-4-thiazolyl]benzamide Basic information |
| Product Name: | N-[1-[[(Cyanomethyl)amino]carbonyl]cyclohexyl]-4-[2-(4-methyl-1-piperazinyl)-4-thiazolyl]benzamide | | Synonyms: | I-006,235;L 006235;N-[1-[[(Cyanomethyl)amino]carbonyl]cyclohexyl]-4-[2-(4-methyl-1-piperazinyl)-4-thiazolyl]benzamide;N-[1-(cyanomethylcarbamoyl)cyclohexyl]-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide;L-006235;L 006235;L006235;N-(1-((cyanomethyl)carbamoyl)cyclohexyl)-4-(2-(4-methylpiperazin-1-yl)thiazol-4-yl)benzamide;Benzamide, N-[1-[[(cyanomethyl)amino]carbonyl]cyclohexyl]-4-[2-(4-methyl-1-piperazinyl)-4-thiazolyl]-;L-235,L-006235,collagen,bone,loss,L 235,resorption,L006235,Inhibitor,inhibit,degradation,Cathepsin,L235 | | CAS: | 294623-49-7 | | MF: | C24H30N6O2S | | MW: | 466.6 | | EINECS: | | | Product Categories: | Potent, reversible cathepsin K inhibitor | | Mol File: | 294623-49-7.mol | ![N-[1-[[(Cyanomethyl)amino]carbonyl]cyclohexyl]-4-[2-(4-methyl-1-piperazinyl)-4-thiazolyl]benzamide Structure](CAS/GIF/294623-49-7.gif) |
| | N-[1-[[(Cyanomethyl)amino]carbonyl]cyclohexyl]-4-[2-(4-methyl-1-piperazinyl)-4-thiazolyl]benzamide Chemical Properties |
| 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 |
| | N-[1-[[(Cyanomethyl)amino]carbonyl]cyclohexyl]-4-[2-(4-methyl-1-piperazinyl)-4-thiazolyl]benzamide Usage And Synthesis |
| 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. |
| | N-[1-[[(Cyanomethyl)amino]carbonyl]cyclohexyl]-4-[2-(4-methyl-1-piperazinyl)-4-thiazolyl]benzamide Preparation Products And Raw materials |
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