LY2811376

LY2811376 is the first orally available non-peptidic β-secretase (BACE1) inhibitor with IC50 of 239 nM-249 nM, that acts to decrease Aβ secretion with EC50 of 300 nM, and demonstrates to have 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including cathepsin D, pepsin, or renin.

Product Specifications

CAS Number

[1194044-20-6]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Beta-secretase

Type

Reference compound

Related Pathways

Neuronal Signaling

Applications

Neuroscience-Neurodegeneration

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/LY2811376.html

Purity

99.64

Solubility

DMSO : ≥ 31 mg/mL

Smiles

FC1=C(C2=CN=CN=C2)C=C([C@]3(C)CCSC(N3)=N)C(F)=C1

Molecular Formula

C15H14F2N4S

Molecular Weight

320.36

Precautions

H302, H315, H319, H335

References & Citations

[1]May PC, et al. Robust central reduction of amyloid-β in humans with an orally available, non-peptidic β-secretase inhibitor. J Neurosci. 2011 Nov 16;31 (46) :16507-16516.|[2]Zhang X, et al. Near-infrared fluorescence molecular imaging of amyloid beta species and monitoring therapy in animal models of Alzheimer's disease. Proc Natl Acad Sci U S A. 2015 Aug 4;112 (31) :9734-9.|[3]Ghosh AK, et al. Prospects of β-Secretase Inhibitors for the Treatment of Alzheimer's Disease. ChemMedChem. 2015 Sep;10 (9) :1463-6|[4]Filser S, et al. Pharmacological inhibition of BACE1 impairs synaptic plasticity and cognitive functions. Biol Psychiatry. 2015 Apr 15;77 (8) :729-39.