LY2811376

SKU: orb1305231

Description

LY2811376 is a potent and orally bioavailable small molecule BACE1 inhibitor with an IC50 of 239-249 nM, reducing Aβ secretion (EC50: 300 nM). It shows high selectivity over BACE2 and other aspartic proteases, making it a valuable tool for in vitro and in vivo Alzheimer's disease research.

Research Area

Neuroscience

Key Properties

• CAS Number: 1194044-20-6
• MW: 320.36
• Purity: 99.01% (May vary between batches)
• Formula: C₁₅H₁₄F₂N₄S
• SMILES: C[C@]1(CCSC(N)=N1)c1cc(c(F)cc1F)-c1cncnc1
• Target: BACE,Beta-Secretase,Beta Amyloid
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:13 mg/mL (40.58 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.24 mM);Ethanol:60 mg/mL (187.29 mM)

Bioactivity

• Target IC50:
  BACE1:239 nM-249 nM|β-Amyloid:300 nM(EC50)
• In Vivo:
  LY2811376 exhibits a concentration-dependent reduction in the secretion of Aβ in HEK293 cells overexpressing APP. It also concentration-dependently inhibits hBACE1, including small synthetic peptide substrates (IC50: 239 nM) and larger chimeric protein substrates (IC50: 249 nM). In primary neuronal cultures from PDAPP transgenic mice, LY2811376 inhibits Aβ secretion (EC50: 100 nM).
• In Vitro:
  In the APPV717F mouse model of Aβ pathology, LY2811376 (10/30/100 mg/kg) induced a dose-dependent significant reduction in Aβ, sAPPβ, and C99, which are the closest breakdown products following the hydrolysis of APP by BACE1 protein. In beagle dogs, LY2811376 (5 mg/kg) resulted in a decrease in plasma Aβ1-x levels, with the maximum reduction of 85% occurring between 4-12 hours post-administration.
• Cell Research:
  The cytotoxicity in the HEK293Swe cell model is assessed using a CellTiter 96 Aqueous Non-Radioactive Cell Proliferation Assay. (Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Beta Amyloid, BetaAmyloid, b Amyloid, Aβ, bAmyloid, BACE, BACE1, b-Secretase, bSecretase, BetaSecretase, Beta-secretase, inhibit, LY 2811376, LY2811376, LY-2811376, Inhibitor, β-Secretase, βSecretase, βAmyloid, β Amyloid

Compound Identifiers

PubChem CID

44251605