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CAS No.: 209984-57-6

LY-411575 Catalog No. CSN17132

Synonyms: LSN-411575

LY411575 is an inhibitor of γ-secretase with IC50 of 0.078 nM and it can also inhibit Notch clevage (IC50 = 0.39 nM).

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Notch clevage

IC50:0.39nM γ secretase

IC50:0.078nM/0.082nM
描述LY411575 is a potent γ-secretase inhibitor with IC50 values of 0.078nM, 0.082nM and 0.39nM for membrane- and cell-based γ-secretase, and Notch S3 cleavage, respectively. Oral administration of 1 or 10mg/kg LY411575 daily significantly reduced brain and plasma Aβ42 and Aβ40 in TgCRND8 mice (overexpressing human APP with both the Swedish and Indiana familial AD mutations), with maximal effect on decreased plasma Aβ40 being observed by 1 h after administration at dose of 10mg/kg. However, atrophy of the thymus could be observed at 15 days post treatment, with overall decrease in thymocyte number, impaired intrathymic differentia tion at the CD4^-CD8^-CD44⁺CD25⁺ precursor stage and altered maturation of peripheral B cells. Also increased goblet cell number and drastically altered tissue morphology could be observed in intestine. Through indirect inhibition of Notch signaling, one of the most important target cleaved by γ-secretase, LY411575 at concentration of 10μM induced hair cell differentiation from inner ear stem cells.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
CHO cells	-	Function assay	24 h	Reduction of human PS1 delta exon9 mutant-induced amyloid beta-42 level in CHO cells overexpressing human APP751after 24 hrs by liquid phase electrochemiluminescence assay relative to control, EC50=0.000352 μM	17573346
CHO cells	-	Function assay	24 h	Reduction of human PS1 delta exon9 mutant-induced amyloid beta-40 level in CHO cells overexpressing human APP751after 24 hrs by liquid phase electrochemiluminescence assay relative to control	17573346
CHO cells	-	Function assay	24 h	Reduction of human wild type PS1-induced amyloid beta-40 level in CHO cells overexpressing human APP751 after 24 hrs by liquid phase electrochemiluminescence assay relative to control, EC50=0.000114 μM	17573346

更多
动物研究
剂量
Mice: 1 mg/kg - 10 mg/kg^[1] (p.o.), 50 mg/kg^[2] (p.o.)

给药途径
p.o.
参考文献

动物研究
剂量	Mice: 1 mg/kg - 10 mg/kg^[1] (p.o.), 50 mg/kg^[2] (p.o.)
给药途径	p.o.

[1] Wong GT, Manfra D, et al. Chronic treatment with the gamma-secretase inhibitor LY-411,575 inhibits beta-amyloid peptide production and alters lymphopoiesis and intestinal cell differentiation. J Biol Chem. 2004 Mar 26;279(13):12876-82. Epub 2004 Jan 6.
[2] Mizutari K, Fujioka M, et al. Notch inhibition induces cochlear hair cell regeneration and recovery of hearing after acoustic trauma. Neuron. 2013 Jan 9;77(1):58-69.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0856 mL
- 10.4281 mL
- 20.8561 mL
- 5 mM
- 0.4171 mL
- 2.0856 mL
- 4.1712 mL
- 10 mM
- 0.2086 mL
- 1.0428 mL
- 2.0856 mL

技术信息

CAS号

209984-57-6

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H23F2N3O4

运输

蓝冰

分子量

479.48

别名

LSN-411575

溶解度

DMSO	95.0 mg/mL (198.1 mM)
Water	Insoluble
Ethanol	12.0 mg/mL (25.0 mM)

动物实验配方

30% PEG400+0.5% Tween80+5% propylene glycol+water

30 mg/mL

suspension

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

CHO cells	-	Function assay	24 h	Reduction of human PS1 delta exon9 mutant-induced amyloid beta-42 level in CHO cells overexpressing human APP751after 24 hrs by liquid phase electrochemiluminescence assay relative to control, EC50=0.000352 μM	17573346
CHO cells	-	Function assay	24 h	Reduction of human PS1 delta exon9 mutant-induced amyloid beta-40 level in CHO cells overexpressing human APP751after 24 hrs by liquid phase electrochemiluminescence assay relative to control	17573346
CHO cells	-	Function assay	24 h	Reduction of human wild type PS1-induced amyloid beta-40 level in CHO cells overexpressing human APP751 after 24 hrs by liquid phase electrochemiluminescence assay relative to control, EC50=0.000114 μM	17573346
CHO cells	-	Function assay	24 h	Reduction of human wild type PS1-induced amyloid beta-42 level in CHO cells overexpressing human APP751 after 24 hrs by liquid phase electrochemiluminescence assay relative to control, EC50=0.000135 μM	17573346
H4 cells	100 nM	Function assay	16 h	Inhibition of gamma secretase expressed in human H4 cells expressing BRI-C99 fusion protein assessed as C99 fragment accumulation fragment at 100 nM incubated for 16 hrs in by immunoblot	23181502
H4 cells	100 nM	Function assay	16 h	Inhibition of gamma secretase expressed in human H4 cells assessed as reduction in C83 levels at 10 uM incubated for 16 hrs by immunoblot	23181502
H4 cells	10 uM	Function assay	16 h	Inhibition of gamma secretase expressed in human H4 cells assessed as reduction in CTF levels at 10 uM incubated for 16 hrs by immunoblot	23181502
HEK293 cells	-	Function assay	-	Inhibition of gamma secretase in human HEK293 cells assessed as amyloid beta 40 production, EC50=0.000119 μM	17573346
HEK293 cells	-	Function assay	3 days	Modulation of gamma-secretase in HEK293 cells expressing guinea pig Swedish mutant SFV-APP695sw coexpressing DLL4 assessed as inhibition of notch processing in human TE671 cells after 3 days by dual-cell luciferase reporter gene assay, IC50=1.2 μM	24139583
SH-SY5Y cells	-	Function assay	-	Inhibition of gamma secretase-mediated amyloid beta (1 to 40) production in human SH-SY5Y cells, IC50=0.001 μM	19694467

LY-411575 Catalog No. CSN17132

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