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Products are for research use only. Not for human use. We do not sell to patients.
(LY411575; LY 411575)
LY-411575 Chemical Structure
|Product name: LY-411575|
|Cat. No.: HY-50752|
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) 
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 .
|M.Wt||479.48||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO(Freely soluble) >200 mg/ml
|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|
|Product Name||Sponsor Only||Condition||Start Date||End Date||Phase||Last Change Date|
|LY-411575||Eli Lilly & Co||Alzheimers disease||31-DEC-09||30-APR-11||Phase 3||16-AUG-11|
|Eli Lilly & Co||Alzheimers disease||31-MAR-08||31-MAY-11||Phase 3||04-OCT-13|
|Eli Lilly & Co||Alzheimers disease||31-OCT-05||31-DEC-06||Phase 2||24-APR-12|
|Eli Lilly & Co||Alzheimers disease||31-JUL-06||30-SEP-07||Phase 1||18-JUN-09|
|Eli Lilly & Co||Alzheimers disease||30-SEP-08||30-APR-11||Phase 3||24-AUG-11|
. Wong GT, et al. Chronic treatment with the gamma-secretase inhibitor LY-411,575 inhibits beta-amyloid peptide production and alters lymphopoiesis and intestinal cell differentiation. J Biol Chem. 2004 Mar 26;279(13):12876-82.
. Hyde LA, et al. Studies to investigate the in vivo therapeutic window of the gamma-secretase inhibitor N2-[(2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl]-L-alaninamide (LY411,575) in the CRND8 mouse. J Pharmacol Exp Ther. 2006 Dec;319(3):1133-43.
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