AZD3293 (Lanabecestat), BACE-1 inhibitor (ab223888)

Overview

  • Product name

    AZD3293 (Lanabecestat), BACE-1 inhibitor
  • Description

    Potent, highly permeable, orally active, blood-brain barrier (BBB) penetrating, specific BACE-1 inhibitor
  • Alternative names

    • AZD3293
    • Lanabecestat
    • LY3314814
  • Biological description

    Potent, highly permeable, orally active, blood-brain barrier (BBB) penetrating, specific BACE-1 inhibitor with unique slow off-rate kinetics. Displays pM potency (IC50 values are 610 pM (primary neuron cultures from mice), 310 pM (primary neuron cultures from guinea pigs), and 80 pM (SH-SY5Y cells over-expressing AβPP), respectively). Covering a diverse range of receptors, ion channels, transporters, kinases, and enzymes, up to a concentration of 10 μM in in vitro radioligand binding and enzyme activity assays. Reduces levels of Aβ40 and Aβ42 in plasma, cerebrospinal fluid and brain in a range of animal models following oral administration. 

  • Purity

    > 99%
  • CAS Number

    1383982-64-6
  • Chemical structure

    Chemical Structure

Properties

  • Chemical name

    (1α,1'R,4β)-4-Methoxy-5''-methyl-6'-[5-(1-propyn-1-yl)-3-pyridinyl]dispiro[cyclohexane-1,2'-[2H]indene

  • Molecular weight

    412.53
  • Molecular formula

    C26H28N4O
  • PubChem identifier

    67979346
  • Storage instructions

    Shipped at 4°C. Store at -20°C.
  • Solubility overview

    Soluble in DMSO and ethanol < 200 mM

  • Handling

    Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

    Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

  • SMILES

    CC#CC1=CC(=CN=C1)C2=CC3=C(CC4([C@]35N=C(C(=N5)N)C)CCC(CC4)OC)C=C2
  • Source

    Synthetic

References

This product has been referenced in:

  • Eketjäll S  et al. AZD3293: A Novel, Orally Active BACE1 Inhibitor with High Potency and Permeability and Markedly Slow Off-Rate Kinetics. J Alzheimers Dis 50:1109-23 (2016). Read more (PubMed: 26890753) »
  • Yan R Stepping closer to treating Alzheimer's disease patients with BACE1 inhibitor drugs. Transl Neurodegener 5:13 (2016). Read more (PubMed: 27418961) »

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Please note: All products are "FOR RESEARCH USE ONLY. NOT FOR USE IN DIAGNOSTIC PROCEDURES, NOT FOR USE IN HUMANS"
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