Product Overview
Oxadiazine is a potent modulator of γ-secretase with Aβ 42 IC50 value of 11 nM and Aβ total/ Aβ 42 value of 1170.γ-Secretase is one of intramenbrane-cleaving aspartyl protease which cleaves many type-I membrane proteins and many of them have important biological functions. γ-secretase is responsible for the generation Aβ from the amyloid precusor protein. γ-Secretase has been considered as an important drug target for Alzheimers disease. γ-Secertase also is responsible for Notch processing which is related to cancer such as leukemia. Oxadiazine is one analogues of BMS-869780 which is anotherγ-secretase modulator. It showed a four folds separation between the IC 50 of Aβ 42 and Aβ 40 H4-APPsw cells which overexpress APP protein. It also increase Aβ 37 and Aβ 38 levels whereas decrease Aβ 42 and Aβ 40 level. It also has little effect on APP-CTFα and no effect on APP-CTFβ and notch processing. It can significantly decrease Aβ 42 and Aβ 40 level in rat brain and plasma.
Chemical Name
(4R,7E,9aS)-7-[[3-methoxy-4-(4-methylimidazol-1-yl)phenyl]methylidene]-4-(3,4,5-trifluorophenyl)-1,3,4,8,9,9a-hexahydropyrido[2,1-c][1,4]oxazin-6-one
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