1. Neuronal Signaling
    Stem Cell/Wnt
  2. γ-secretase

LY-411575 (Synonyms: LY411575; LY 411575)

Cat. No.: HY-50752 Purity: 99.22%
Data Sheet SDS Handling Instructions

LY-411575 is a potent γ-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), and also inhibits Notch S3 cleavage with IC50 of 0.39 nM.

For research use only. We do not sell to patients.
LY-411575 Chemical Structure

LY-411575 Chemical Structure

CAS No. : 209984-57-6

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10 mM * 1 mL in DMSO $121 In-stock
5 mg $110 In-stock
10 mg $198 In-stock
50 mg $590 In-stock
100 mg $960 In-stock
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500 mg   Get quote  

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Description

LY-411575 is a potent γ-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), and also inhibits Notch S3 cleavage with IC50 of 0.39 nM.

IC50 & Target

IC50: 0.078 nM (γ-secretase in membrane), 0.082 nM (γ-secretase cell-based), 0.39 nM (Notch S3 cleavage cell-based)[1]

In Vitro

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[2]. 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 daclatasvir (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[4]. LY411575 significantly attenuates EMT by inhibiting the Notch signaling activation in vitro[5].

In Vivo

LY-411,575 (10 mg/kg) decreases brain and plasma Aβ40 and -42 robustly when chronically administered to TgCRND8 mice[1]. 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[3]. LY411575 inhibits mouse proliferative vitreoretinopathy (PVR) formation in vivo[5].

References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 2.0856 mL 10.4280 mL 20.8559 mL
5 mM 0.4171 mL 2.0856 mL 4.1712 mL
10 mM 0.2086 mL 1.0428 mL 2.0856 mL
Animal Administration
[3]

LY-411575 is formulated as 10 mg/mL solutions and diluted 1:10 with 0.4% methycellulose for oral administration; LY-411575 is formulated in 10 mg/mL stock solution and diluted 1:10 with 20% hydroxyl-propyl-β-cyclodextrin for subcutaneous dosing.

Mice from the aged cohort (16-26 months old) are either retired breeders or experimentally naive mice. Before dosing begin and for the duration of the study, mice are singly housed with a plastic igloo and nesting material. Mice are sacrificed 2 to 4 h after their final dosing. For oral dosing, LY411,575 and LY-D are formulated as 10 mg/mL solutions and diluted 1:10 with 0.4% methycellulose. In the case of subcutaneous dosing, the 10 mg/mL stock solution is diluted 1:10 with 20% hydroxyl-propyl-β-cyclodextrin. If necessary, serial dilutions are made from the 1 mg/mL solution using the appropriate 1:10 vehicle. The dosing volume is 10 mL/kg. After oral administration of 10 mg/kg LY411,575, inhibition of plasma Aβ is still significant 24, but not 48, h after dosing, so in an effort to maintain continuous γ-secretase inhibition, LY411,575 and LY-D are dosed once per day in all studies.

References
M.Wt

479.48

Formula

C₂₆H₂₃F₂N₃O₄

CAS No.

209984-57-6

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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LY-411575
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HY-50752
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