LY-411575

Notch S3 cleavage:0.39 nM, γ-secretase (cell-based assay):0.082 nM, γ-secretase (membrane-based):0.078 nM

LY-411575 是一种高效的γ-secretase 抑制剂，能够抑制 Aβ40 蛋白的产生，在膜中的 IC50 为 0.078 nM，在细胞中为 0.082 nM。 它还抑制 Notch 切割，IC50 为 0.39 nM。

LY-411575, a potent γ-secretase inhibitor, is with IC50 of 0.078 nM in the membrane and 0.082 nM in cell-based. It also suppresses Notch clevage with IC50 of 0.39 nM.

479.48

99.38%

LY-411575 inhibits γ-secretase which can be assessed by the substrates like amyloid precursor protein (APP) and Notch S3 cleavage. [1] LY-411575, which blocks Notch activation, results in apoptosis in primary and immortalized KS cells. [2]

10 mg/kg oral dose of LY-411575 decreases brain and plasma Aβ40 and -42 dose-dependently. [1] 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. [3]

LY411575

C26H23F2N3O4

209984-57-6

1.40 g/cm3

H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 88 mg/mL (183.53 mM), Sonication is recommended. Ethanol: 11 mg/mL (22.94 mM), Sonication is recommended.

keep away from moisture,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.