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MRK 560
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MRK 560图片
CAS NO:677772-84-8
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
MRK 560 是一种具有口服活性、可穿透脑屏障的 γ-分泌酶抑制剂,可有效减少大鼠脑和脑脊液中的 Aβ 肽。
Cas No.677772-84-8
化学名N-((1s,4s)-4-((4-chlorophenyl)sulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)-1,1,1-trifluoromethanesulfonamide
Canonical SMILESO=S(C(F)(F)F)(N[C@@H]1CC[C@](C2=CC(F)=CC=C2F)(S(=O)(C3=CC=C(Cl)C=C3)=O)CC1)=O
分子式C19H17ClF5NO4S2
分子量517.92
溶解度<51.79mg/ml in DMSO;<25.9mg/ml in ethanol
储存条件Store at 4℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IC50: 0.65 nM for both Aβ(40) and Aβ(42)

MRK-560 is a novel γ-secretase inhibitor.

γ-Secretase is a member of the I-CLiP protease family and is reported to cleave a number of additional intramembrane substrates, including Erb4, CD-44, Notch, E-cadherin, and the Notch ligands. γ-Secretase is responsible for the intramembraneous proteolytic cleavage of the C-terminal fragment of APP, resulting in mainly Aβ(40) or Aβ(42) production.

In vitro: In SH-SY5Y neuroblastoma cells, MRK-560 inhibited the production of Aβ(40) and Aβ(42) with similar in vitro IC50 values in the range of 0.65 nM [1].

In vivo: MRK-560 was found to be able to reduce Aβ in the brain and cerebrospinal fluid (CSF) in the rat markedly, with ED50s of 6 and 10 mg/kg, respectively. Time-course experiments demonstrated the reductions in Aβ could be maintained for 24 h. Comparable temporal reductions in rat brain and CSF further suggested that these two pools of Aβ were related. Such relationship between the brain and CSF Aβ was maintained when MRK-560 was dosed once a day for 2 weeks. These results indicated that MRK-560 was a γ-secretase inhibitor with the ability to reduce Aβ peptide in the rat brain and CSF [1].

Clinical trial: N/A

Reference:
[1] Best JD,Jay MT,Otu F,Churcher I,Reilly M,Morentin-Gutierrez P,Pattison C,Harrison T,Shearman MS,Atack JR.  In vivo characterization of Abeta(40) changes in brain and cerebrospinal fluid using the novel gamma-secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) in the rat. J Pharmacol Exp Ther.2006 May;317(2):786-90.