计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
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概述
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%
规格
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。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
Isomeric SMILES
C[C@@H](C(=O)N[C@H]1C2=CC=CC=C2C3=CC=CC=C3N(C1=O)C)NC(=O)[C@H](C4=CC(=CC(=C4)F)F)O
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=
高级数据
关联靶点（人）
SPPL2A
Tchem
信号肽肽酶类2A(Signal peptide peptidase-like 2A)
(1 活性数据)
PSEN1
Tchem
早老素-1(Presenilin-1)
(2 活性数据)
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;
沸点
~836.0 °C at 760 mmHg
熔点
328.47°C
安全和危险性（GHS）
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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危险品化学品经营许可证（带存储）