LY411575

Notch Selective Inhibitors

10mM in DMSO

CAS编号: 209984-57-6(DMSO)
分子式: C₂₆H₂₃F₂N₃O₄
分子量: 479.48

有货

库存信息

关闭

货号 (SKU)	包装规格	是否现货	价格	数量
L409285-1ml	1ml	现货

查看相关系列

Compound libraries (12332)

Skip to the end of the images gallery

Skip to the beginning of the images gallery

基本描述

英文别名	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-α-hydroxy-, (αS)-
规格或纯度	10mM in DMSO
英文名称	LY411575
生化机理	LY411575 是一种强效的 γ 分泌酶抑制剂，其 IC50 为 0.078 nM/0.082 nM（膜基/细胞基），在表达 APP 或 NΔE 的 HEK293 细胞中也能抑制 Notch 的裂解，其 IC50 为 0.39 nM。LY411575 可诱导细胞凋亡。
储存温度	-80℃储存
运输条件	超低温冰袋运输
产品介绍	LY411575是γ-secretase抑制剂，基于膜和细胞的实验IC50分别为0.078 nM/0.082 nM，还能抑制Notch clevage，IC50为0.39 nM。A potent γ-secretase inhibitor Information LY411575 is a potentγ-secretaseinhibitor withIC50of 0.078 nM/0.082 nM (membrane/cell-based), also inhibits Notch cleavage withIC50of 0.39 nM in APP or NΔE expressing HEK293 cells. LY411575 inducesapoptosis. In vitro 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 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. Cell Data cell lines： Concentrations：500 μM Incubation Time：24 hours Powder Purity:≥99%

产品属性

IC50	Notch S3 cleavage, IC50: 0.39 nM
ALogP	2.625
hba_count	3
HBD Count	3
Rotatable Bond	5

关联靶点（人）

SPPL2A Tchem 信号肽肽酶类2A(Signal peptide peptidase-like 2A) (1 活性数据)

点击查看靶蛋白信息： SPPL2A

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

PSEN1 Tchem 早老素-1(Presenilin-1) (2 活性数据)

点击查看靶蛋白信息： PSEN1

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

名称和识别符

分子类型	小分子
Canonical SMILES	CC(NC(=O)C(O)C1=CC(=CC(=C1)F)F)C(=O)NC2C(=O)N(C)C3=C(C=CC=C3)C4=C2C=CC=C4
分子量	479.48
Reaxy-Rn	54940486
Reaxys-RN link address	https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=54940486&ln=

化学和物理性质

溶解性	Solubility (25°C) In vitro DMSO: 10 mg/mL warmed with 50ºC Water: bath (74.0 mM); 5%TFA 6.03 mg/mL (44.62 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility	95
DMSO(mM) Max Solubility	198.13
Water(mg / mL) Max Solubility	<1