LY-411575

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的 γ-分泌酶抑制剂，可降低 APP 转染细胞系中的 Aβ 水平，其 IC50 值为 119 pM。

A potent γ-secretase inhibitor that has an IC50 value of 119 pM for reduction of Aβ levels in APP-transfected cell lines; dose dependently reduces Aβ(1-40) and Aβ(1-42) in the brain, CSF, and plasma of Tg2576 mice; reduces cortical Abeta(40) in young transgenic CRND8 mice with ED50 of 0.6 mg/kg, and produces significant thymus atrophy and intestinal goblet cell hyperplasia at higher doses (>3 mg/kg).Alzheimer's Disease Preclinical.

LY-411,575 blocks Notch activation, and results in apoptosis in primary and immortalized KS cells. LY-411,575 (500 μM) induces G2/M growth arrest SLK cells. LY411575 treatment significantly decreases the amounts of intracellular HCV RNA with IC50 of 0.56?±?0.20?μM and extracellular HCV particles. LY411575 (0-40?nM) alone or in combination with BMS-790052 (0-40?pM) decreases supernatant infectious titers in a dose-dependent manner, and is synergistic regarding production of infectious virus. LY411575 (10?μM) treatment impairs ROS production in HCVcc-infected cells. LY411575 significantly attenuates EMT by inhibiting the Notch signaling activation in vitro.

LY-411,575 (10 mg/kg) decreases brain and plasma Aβ40 and -42 robustly when chronically administered to TgCRND8 mice. LY411,575 reduces cortical Aβ40 in young transgenic CRND8 mice (ED50 appr 0.6 mg/kg) and produces significant thymus atrophy and intestinal goblet cell hyperplasia at higher doses (>3 mg/kg). The extent of intestinal goblet cell hyperplasia induced by LY411,575 (10 mg/kg) is similar in young and aged mice. LY411575 inhibits mouse proliferative vitreoretinopathy (PVR) formation in vivo.

LY411575 | LY 411575

Wnt/Notch/Hedgehog

γ-secretase

NotchS3cleavage|γsecretase(cell-based)|γsecretase(membrane-based)

Neurological Disease

Alzheimer Disease

209984-57-6

479.4753

C26H23F2N3O4

>98% (HPLC)

10 mM in DMSO

C[C@@H](C(N[C@H]1C2=CC=CC=C2C3=CC=CC=C3N(C)C1=O)=O)NC([C@H](C4=CC(F)=CC(F)=C4)O)=O

Benzeneacetamide, N-[(1S)-2-[[(7S)-6,7-dihydro-5-methyl-6-oxo-5H-dibenz[b,d]azepin-7-yl]amino]-1-methyl-2-oxoethyl]-3,5-difluoro-.alpha.-hydroxy-, (.alpha.S)-

(-20℃)

With Ice Pack

≥ 2 years