LY411575 - 10mM in DMSO , CAS No.209984-57-6

CAS: 209984-57-6 Cat. No.: L409285 Fórmula: C₂₆H₂₃F₂N₃O₄ Peso molecular: 479.48

GRADE & PURITY 10mM in DMSO

Synonyms

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)-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Visão geral

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%

Specifications

Sinónimos

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)-

Especificações e pureza

10mM in DMSO

Mecanismos bioquímicos e fisiológicos

LY411575 is a potent γ-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), also inhibits Notch cleavage with IC50 of 0.39 nM in APP or NΔE expressing HEK293 cells. LY411575 induces apoptosis.

Condições de armazenamento de armazenamento

Store at -80°C

Enviado em

Dry ice packs + Cold packs

Este produto requer transporte de cadeia fria. Serviços terrestres e outros serviços econômicos não estão disponíveis.

Nomes e identificadores

SMILES isoméricas

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

WGK Alemanha

3

Peso molecular

479.48

Reaxy-Rn

54940486

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=54940486&ln=

Alvos associados (humanos)

SPPL2A Tchem Signal peptide peptidase-like 2A (1 Activities)

Discover Target: SPPL2A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PSEN1 Tchem Presenilin-1 (2 Activities)

Discover Target: PSEN1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propriedades químicas e físicas

• Solubilidade: 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
• Ponto de ebulição (°C): ~836.0 °C at 760 mmHg
• Ponto de fusão (°C): 328.47°C