NGP-555

NGP-555 is a modulator of gamma-secretase that inhibits APP intracellular signaling domain (AICD) cleavage to amyloid-beta (Abeta, IC50s = 531 and 131 nM for Abeta40 and Abeta42, respectively, in HeLa cell membranes). It is selective for AICD cleavage to Abeta over E-cadherin and Notch cleavage to their signaling effectors, E-cadherin gamma-C-terminal fragment and NICD, respectively, processes also mediated by gamma-secretase, when used at a concentration of 30 µM. Dietary administration of NGP-555 (~50 mg/kg per day) reduces cortical and hippocampal plaque area in the Tg2576 transgenic mouse model of Alzheimer's disease. NGP-555 (25 mg/kg per day, p.o.) decreases plasma and brain Abeta40 and Abeta42 levels, as well as increases spontaneous alternations in the Y-maze, indicating prevention of memory deficits, in Tg2576 mice.Formal Name: N-(5-ethyl-2,4-dimethylphenyl)-4-[3-fluoro-4-(4-methyl-1H-imidazol-1-yl)phenyl]-2-thiazolamine. CAS Number: 1304630-27-0. Molecular Formula: C23H23FN4S. Formula Weight: 406.5. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMSO: soluble. SMILES: CC1=CC(C)=C(CC)C=C1NC2=NC(C3=CC(F)=C(N4C=NC(C)=C4)C=C3)=CS2. InChi Code: InChI=1S/C23H23FN4S/c1-5-17-10-20(15(3)8-14(17)2)26-23-27-21(12-29-23)18-6-7-22(19(24)9-18)28-11-16(4)25-13-28/h6-13H,5H2,1-4H3,(H,26,27). InChi Key: WDEKUGNKKOGFOA-UHFFFAOYSA-N.