货号 | 4000/50 |
别名 | N-[cis-4-[(4-Chlorophenyl)sulfonyl] |
供应商 | Tocris |
生物活性 | γ-secretase inhibitor; inhibits proteolytic cleavage of amyloid precursor protein (APP) over the Notch pathway. Reduces levels of Aβ in the brain (inhibits Aβ40 and Aβ42 in SH-SY5Y neuroblastoma cells with an IC50 of 0.65 nM); attenuates plaque deposition. Orally bioavailable. |
运输条件 | Blue Ice |
存放说明 | 4℃ |
纯度 | >99 % |
计算分子量 | 517.92 |
分子式 | C19H17ClF5NO |
可溶性/溶解性 | Soluble to 100 mM in DMSO and to 50 mM in ethanol |
参考文献 | Bestet al (2007) The novel γ-secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) reduces amyloid plaque deposition without evidence of Notch-related pathology in the Tg2576 mouse. J.Pharm.Exp.Ther. 320 552. PMID: 17099072. Bestet al (2006) In vivo characterization of Aβ(40) changes in brain and cerebrospinal fluid using the novel γ-secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) in the rat. J.Pharm.Exp.Ther. 317 786. PMID: 16443723. |