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LY2811376

Catalog No. T2639 CAS 1194044-20-6

LY2811376, an orally available non-peptidic β-secretase(BACE1) inhibitor (IC50: 239-249 nM), can decrease Aβ secretion (EC50: 300 nM). It has 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including pepsin, cathepsin D, or renin.

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LY2811376, CAS 1194044-20-6

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	LY2811376, an orally available non-peptidic β-secretase(BACE1) inhibitor (IC50: 239-249 nM), can decrease Aβ secretion (EC50: 300 nM). It has 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including pepsin, cathepsin D, or renin.
Targets&IC50	Aβ:300 nM(EC50), BACE1:239 nM-249 nM
Kinase Assay	Determination of enzymatic ef?ciency: The stock solution for each FRET peptide substrate is prepared at 30 mM in dimethylsulfoxide (DMSO). The huBACE1:Fc muBACE1:Fc preparation is concentrated through YM10 Centricon. to a ?nal concentration of at least 7 mg/mL. The optimal enzyme concentration for each FRET peptide substrate is determined individually at 30 μM FRET peptide substrate in 50 mM ammonium acetate, pH 4.6, 1 mg/mL BSA and 1 mM Triton X-100. The enzymatic ef?ciency (kcat /Km) of either of the BACE1 orthologs toward individual FRET peptide substrates at 15, 30 and 100 μM is determined under the optimal conditions for each substrate. The progress of the reaction is monitored by measuring an increase of the emission signal at 420 nm with excitation wavelength set at 320 nm, using a GEMINI ?uorescence plate reader. Amino acid conjugated aminobenzoate is used to convert the emission signal in the relative ?uorescence units into the molar concentration of product generated in the reaction mixture. The initial phase of the timedependence curve is ?tted with a linear function whose slope is used to calculate the initial rate for huBACE1:Fc toward each peptide substrate. The kcat /Km values are calculated from the linear dependence of the initial rate on the concentration of each peptide.
Cell Research	The cytotoxicity in the HEK293Swe cell model is assessed using a CellTiter 96 Aqueous Non-Radioactive Cell Proliferation Assay. (Only for Reference)

Molecular Weight	320.36
Formula	C15H14F2N4S
CAS No.	1194044-20-6

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

H2O: <1 mg/mL

DMSO: 13 mg/mL (40.6 mM)

Ethanol: 60 mg/mL (187.3 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. May P, et al. J Neurosci, 2011, 31(46), 16507-16516. 2. Yang HC, et al. J Neurochem, 2004, 91(6), 1249-1259.

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

LY2811376 1194044-20-6 Neuroscience Beta Amyloid BACE Beta-Secretase LY-2811376 Inhibitor LY 2811376 β-Secretase inhibit Beta-secretase inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.