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

LY-411575 (Synonyms: LY411575; LY 411575)

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

LY411575 is a potent γ-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), also inhibits Notch clevage with withIC50 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

Size Price Stock Quantity
Free sample   Apply now  
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
200 mg   Get quote  
500 mg   Get quote  

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Description

LY411575 is a potent γ-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), also inhibits Notch clevage with IC50 of 0.39 nM. IC50 value: 0.078 nM/0.082 nM (membrane/cell-based) [1] Target: γ-secretase in vitro: LY-411575 inhibits γ-secretase which can be assessed by the substrates like amyloid precursor protein (APP) and Notch S3 cleavage [1]. LY-411575, which blocks Notch activation, results in apoptosis in primary and immortalized KS cells [2]. in vivo: 10 mg/kg oral dose of LY-411575 decreases brain and plasma Aβ40 and -42 dose-dependently. [1] 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 [3].

Clinical Trial
Sponsor Condition Start Date Phase
Eli Lilly & Co Alzheimers disease 2009-12-31 Phase 3
Eli Lilly & Co Alzheimers disease 2008-09-30 Phase 3
Eli Lilly & Co Alzheimers disease 2008-03-31 Phase 3
Eli Lilly & Co Alzheimers disease 2005-10-31 Phase 2
Eli Lilly & Co Alzheimers disease 2006-07-31 Phase 1
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
M.Wt

479.48

Formula

C₂₆H₂₃F₂N₃O₄

CAS No.

209984-57-6

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

Purity: 99.22%

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Product Name:
LY-411575
Cat. No.:
HY-50752
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