LY2811376

Accumulation of the beta-amyloid (Abeta) peptide in the brain is implicated as the primary cause of neurodegeneration and progression of Alzheimer's disease. Abeta is derived from sequential proteolytic cleavage of the amyloid precursor protein (APP) by beta-secretase (BACE) and gamma-secretase. LY2811376 is a non-peptide inhibitor of BACE1 (IC50 = 239 nM for the synthetic peptide) that demonstrates ~10-fold selectivity over BACE2 and >50-fold selectivity over the aspartyl proteases cathepsin D, pepsin, and renin. LY2811376 treatment in APP-overexpressing cells and transgenic animal models yields a dose-dependent decrease in Abeta. Furthermore, LY2811376 has been reported to reduce C99 and sAPPbeta, the two primary APP cleavage products generated by BACE1.Formal Name: (4S)-4-[2,4-difluoro-5-(5-pyrimidinyl)phenyl]-5,6-dihydro-4-methyl-4H-1,3-thiazin-2-amine. CAS Number: 1194044-20-6. Molecular Formula: C15H14F2N4S. Formula Weight: 320.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml, Ethanol: 25 mg/ml. SMILES: FC(C=C(F)C([C@]1(C)CCSC(N)=N1)=C2)=C2C3=CN=CN=C3. InChi Code: InChI=1S/C15H14F2N4S/c1-15(2-3-22-14(18)21-15)11-4-10(12(16)5-13(11)17)9-6-19-8-20-7-9/h4-8H,2-3H2,1H3,(H2,18,21)/t15-/m0/s1. InChi Key: MJQMRGWYPNIERM-HNNXBMFYSA-N.