Overview

  • Product name(S)-Willardiine
  • Description
    AMPA / kainate receptor agonist
  • Biological descriptionSelective AMPA receptor agonist at hGluR1 (Ki = 0.39 μM). Selective over hGluR2 (Ki = 0.90 μM), hGluR4 (Ki = 8.85 μM) and kainate receptor hGluR5 (Ki = 28.9 μM). Produces strong desensitisation.
  • Purity> 98%

Properties

    Applications

    Our Abpromise guarantee covers the use of ab120040 in the following tested applications.

    The application notes include recommended starting dilutions; optimal dilutions/concentrations should be determined by the end user.

    Application Abreviews Notes
    Functional Studies Use at an assay dependent concentration.

    (S)-Willardiine images

    • ab96379 staining MEK1 (phospho S298) in SK-N-SH cells treated with (S)-Williardine (ab120040), by ICC/IF. Increase in MEK1 (phospho S298) expression correlates with increased concentration of (S)-Williardine, as described in literature.
      The cells were incubated at 37°C for 6h in media containing different concentrations of ab120040 ((S)-Williardine) in DMSO, fixed with 4% formaldehyde for 10 minutes at room temperature and blocked with PBS containing 10% goat serum, 0.3 M glycine, 1% BSA and 0.1% tween for 2h at room temperature. Staining of the treated cells with ab96379 (1/100 dilution) was performed overnight at 4°C in PBS containing 1% BSA and 0.1% tween. A DyLight 488 goat anti-rabbit polyclonal antibody (ab96899) at 1/250 dilution was used as the secondary antibody.

    References for (S)-Willardiine (ab120040)

    This product has been referenced in:
    • Mankiewicz KA  et al. Chemical interplay in the mechanism of partial agonist activation in alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors. Biochemistry 47:398-404 (2008). Read more (PubMed: 18081322) »
    • Stensbøl TB  et al. The AMPA receptor binding site: focus on agonists and competitive antagonists. Curr Pharm Des 8:857-72 (2002). Read more (PubMed: 11945136) »
    • Jane DE  et al. Synthesis of willardiine and 6-azawillardiine analogs: pharmacological characterization on cloned homomeric human AMPA and kainate receptor subtypes. J Med Chem 40:3645-50 (1997). Read more (PubMed: 9357531) »
    • Hawkins LM  et al. Binding of the new radioligand (S)-[3H]AMPA to rat brain synaptic membranes: effects of a series of structural analogues of the non-NMDA receptor agonist willardiine. Neuropharmacology 34:405-10 (1995). Read more (PubMed: 7566471) »
    • Patneau DK  et al. Activation and desensitization of AMPA/kainate receptors by novel derivatives of willardiine. J Neurosci 12:595-606 (1992). Read more (PubMed: 1371315) »

    See 1 Publication for this product

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    Please note: All products are "FOR RESEARCH USE ONLY AND ARE NOT INTENDED FOR DIAGNOSTIC OR THERAPEUTIC USE, NOT FOR USE IN HUMANS"