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.
Chemical name(S)-2-Amino-3-(3,4-dihydro-2,4-dioxopyrimidin-1(2H)-yl)propanoic acid
Storage instructionsStore at +4°C. Store under Desiccating conditions. The product can be stored for up to 12 months.
Solubility overviewSoluble in 1.1 eq. NaOH to 50 mM
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.
The application notes include recommended starting dilutions; optimal dilutions/concentrations should be determined by the end user.
Use at an assay dependent concentration.
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. Biochemistry47:398-404 (2008).
Read more (PubMed: 18081322) »
Jane DE et al. Synthesis of willardiine and 6-azawillardiine analogs: pharmacological characterization on cloned homomeric human AMPA and kainate receptor subtypes. J Med Chem40:3645-50 (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. Neuropharmacology34:405-10 (1995).
Read more (PubMed: 7566471) »
Patneau DK et al. Activation and desensitization of AMPA/kainate receptors by novel derivatives of willardiine. J Neurosci12:595-606 (1992).
Read more (PubMed: 1371315) »