Overview

  • Product name

    LY2886721, BACE-1 inhibitor
  • Description

    Potent and selective BACE-1 inhibitor
  • Alternative names

    • LY2886721
  • Biological description

    Potent and selective BACE-1 inhibitor (IC50 = 20.3 nM for recombinant hBACE-1). Human BACE2 is inhibited with an IC50 of 10.2 nM. Does not inhibit other aspartyl proteases such as cathepsin D, pepsin, and renin. A potential agent to treat Alzheimer’s Disease. Inhibits production of Aβ in HEK-293 Swe cells (IC50 values are 18.5 nM and 19.7 nM for Aβ1-40 and Aβ1-42 respectively) and in PDAPP neuronal cells (IC50 ~10 nM). Reduces dose-dependently brain levels of Aβ, C99 and sAPPβ in orally administered mouse model and plasma Aβ in dog model. Ppenetrates the blood-brain barrier.

  • Purity

    > 98%
  • CAS Number

    1262036-50-9
  • Chemical structure

    Chemical Structure

Properties

  • Chemical name

    N-(3-((4aS,7aS)-2-Amino-4a,5,7,7a-tetrahydro-4H-furo[3,4-d][1,3]thiazin-7a-yl)-4-fluorophenyl)-5-fluoropicolinamide

  • Molecular weight

    390.41
  • Molecular formula

    C18H16F2N4O2S
  • PubChem identifier

    49837968
  • Storage instructions

    Shipped at 4°C. Store at -20°C. Store In the Dark. Store under desiccating conditions.
  • Solubility overview

    Soluble in DMSO to 20 mM, in Ethanol < 2 mM

  • SMILES

    C1[C@H]2CSC(=N[C@]2(CO1)C3=C(C=CC(=C3)NC(=O)C4=NC=C(C=C4)F)F)N
  • Source

    Synthetic

References

This product has been referenced in:

  • May PC  et al. The potent BACE1 inhibitor LY2886721 elicits robust central Aß pharmacodynamic responses in mice, dogs, and humans. J Neurosci 35:1199-210 (2015). Read more (PubMed: 25609634) »
  • Qi Y  et al. Longitudinal testing of hippocampal plasticity reveals the onset and maintenance of endogenous human Aß-induced synaptic dysfunction in individual freely behaving pre-plaque transgenic rats: rapid reversal by anti-Aß agents. Acta Neuropathol Commun 2:175 (2014). Read more (PubMed: 25540024) »
  • Lahiri DK  et al. Lessons from a BACE1 inhibitor trial: off-site but not off base. Alzheimers Dement 10:S411-9 (2014). Read more (PubMed: 24530026) »

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