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- LY-411575 209984-57-6

- LY-411575 209984-57-6
LY-411575 209984-57-6
产品描述 描述 LY411575 is a potent γ-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), also inhibits Notch clevage with withIC50 of 0.39 nM.
纯度 >98%储存/保存方法 Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.基本信息 别名 LY411575;LY 411575外观 white to beige Powder可溶性/溶解性 DMSO : 33.33 mg/mL (69.51 mM; Need ultrasonic)生物活性 靶点 γ secretase (membrane-based);γ secretase (cell-based) ;Notch S3 cleavageIn vitro(体外研究) LY-411575 inhibits γ-secretase which can be assessed by the substrates like amyloid precursor protein (APP) and Notch S3 cleavage. LY-411575, which blocks Notch activation, results in apoptosis in primary and immortalized KS cells.In vivo(体内研究) 10 mg/kg oral dose of LY-411575 decreases brain and plasma Aβ40 and -42 dose-dependently. LY-411575 reduces cortical Aβ40 in young (preplaque) transgenic CRND8 mice (ED50 ≈ 0.6 mg/kg) and produces significant thymus atrophy and intestinal goblet cell hyperplasia at higher doses (>3 mg/kg). The therapeutic window is similar after oral and subcutaneous administration and in young and aged CRND8 mice. Both the thymus and intestinal side effects are reversible after a 2-week washout period. Three-week treatment with 1 mg/kg LY411575 reduces cortical Aβ40 by 69% without inducing intestinal effects, although a previously unreported change in coat color is observed.研究领域 研究领域 NeuroscienceDrug DiscoverySmall Molecule DrugLead Compound DiscoveryLY-411575 209984-57-6温馨提示:本产品仅作科研实验使用,不支持临床等研究
