货号 | 3066/50 |
别名 | N-[1-[[(Cyanomethyl)amino]carbonyl] |
供应商 | Tocris |
生物活性 | Potent, reversible cathepsin K inhibitor (IC50 = 0.25 nM) that displays > 4000-fold selectivity over cathepsins B, L and S. Displays reduced selectivity in cell-based assays possibly due to lysosomal accumulation. Reduces collagen breakdown and promotes bone deposition in vivo. Orally active and has intrinsic fluorescence. |
运输条件 | Blue Ice |
存放说明 | 4℃ |
纯度 | >98 % |
计算分子量 | 466.6 |
分子式 | C24H30N6O2S |
可溶性/溶解性 | Soluble to 100 mM in DMSO |
CAS号 | 294623-49-7 |
参考文献 | Desmaraiset al (2008) Effects of cathepsin K inhibitors basicity on in vivo off-target activities. Mol.Pharmacol. 73 147. PMID: 17940194. Falgueyretet al (2005) Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. J.Med.Chem. 48 7535. PMID: 16302795. Palmeret al (2005) Design and synthesis of tri-ring P3 benamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K. J.Med.Chem. 48 7520. PMID: 16302794. |