LY-411575 (Cat.No:I002614) is a potent and selective inhibitor of gamma-secretase, an enzyme involved in the processing of amyloid precursor protein (APP) and the generation of beta-amyloid peptides implicated in Alzheimer’s disease. It has shown promise in preclinical studies for reducing beta-amyloid plaque formation and cognitive decline. Clinical trials are ongoing to evaluate its therapeutic potential in Alzheimer’s disease treatment.
| Catalog Number | I002614 |
| CAS Number | 209984-57-6 |
| Synonyms | (2S)-2-[[(2S)-2-(3,5-difluorophenyl)-2-hydroxyacetyl]amino]-N-[(7S)-5-methyl-6-oxo-7H-benzo[d][1]benzazepin-7-yl]propanamide |
| Molecular Formula | C₂₆H₂₃F₂N₃O₄ |
| Purity | ≥95% |
| Target | Gamma Secretase |
| Solubility | DMSO: 95 mg/mL, H2O: <1 mg/mL |
| Storage | 3 years -20℃ powder |
| IC50 | 0.078 nM/0.082 nM (membrane/cell-based) [1] |
| IUPAC Name | (2S)-2-[[(2S)-2-(3,5-difluorophenyl)-2-hydroxyacetyl]amino]-N-[(7S)-5-methyl-6-oxo-7H-benzo[d][1]benzazepin-7-yl]propanamide |
| InChI | InChI=1S/C26H23F2N3O4/c1-14(29-25(34)23(32)15-11-16(27)13-17(28)12-15)24(33)30-22-20-9-4-3-7-18(20)19-8-5-6-10-21(19)31(2)26(22)35/h3-14,22-23,32H,1-2H3,(H,29,34)(H,30,33)/t14-,22-,23-/m0/s1 |
| InChIKey | ULSSJYNJIZWPSB-CVRXJBIPSA-N |
| SMILES | CC(C(=O)NC1C2=CC=CC=C2C3=CC=CC=C3N(C1=O)C)NC(=O)C(C4=CC(=CC(=C4)F)F)O |
| Reference | </br>1:Existing plaques and neuritic abnormalities in APP:PS1 mice are not affected by administration of the gamma-secretase inhibitor LY-411575. Garcia-Alloza M, Subramanian M, Thyssen D, Borrelli LA, Fauq A, Das P, Golde TE, Hyman BT, Bacskai BJ.Mol Neurodegener. 2009 May 6;4:19. doi: 10.1186/1750-1326-4-19. PMID: 19419556 Free PMC Article</br>2:Quantitative measurement of changes in amyloid-beta(40) in the rat brain and cerebrospinal fluid following treatment with the gamma-secretase inhibitor LY-411575 [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]. Best JD, Jay MT, Otu F, Ma J, Nadin A, Ellis S, Lewis HD, Pattison C, Reilly M, Harrison T, Shearman MS, Williamson TL, Atack JR.J Pharmacol Exp Ther. 2005 May;313(2):902-8. Epub 2005 Mar 2. PMID: 15743924 Free Article</br>3:Studies of Abeta pharmacodynamics in the brain, cerebrospinal fluid, and plasma in young (plaque-free) Tg2576 mice using 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 (LY-411575). Lanz TA, Hosley JD, Adams WJ, Merchant KM.J Pharmacol Exp Ther. 2004 Apr;309(1):49-55. Epub 2004 Jan 12. PMID: 14718585 Free Article |
