Conantokin R

Con-R
An Antagonist of GluN2A and GluN2B Receptors
  • New
Cat #: STC-777
Alternative Name Con-R
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic peptide
    MW: 3098 Da.
    Endotoxin Level NR
    Purity: >98%
    Form Lyophilized powder.
    Effective concentration 50-500 nM.
    Sequence GEXXVAKMAAXLARXNIAKGCKVNCYP
    Modifications Cys21-Cys25, X = 4-Carboxyglutamate.
    Structure
    • Conantokin R
    Molecular formula C127H201N35O49S3
    CAS No.: 202925-60-8
    Activity Conantokin R is a potent and non-competitive NMDA receptor 2A/B antagonist1.
    References-Activity
    1. White, H.S. et al. (2000) J. Pharmacol. Exp. Ther. 292, 425.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility Soluble in any aqueous buffer. Centrifuge all product preparations before use (10000 x g for 5 min).
    Storage of solutions Store at 4°C for up to 1 week. For longer periods, small aliquots should be stored at -20°C. Avoid multiple freezing and thawing.
    Our bioassay
    • Conantokin R
      Alomone Labs Conantokin R efficiently inhibits NMDA receptors expressed in Xenopus oocytes.
      Representative NR1A/NR2A current elicited in Mg2+-free bath solution by a continuous co-application of 2 µM glutamate and 10 µM glycine (black bar). Current is significantly inhibited by 3 µM Conantokin R (#STC-777) application (green bar). Membrane potential was held at -80 mV and current was recorded by two-electrode voltage-clamp.
    References - Scientific background
    1. Layer, R.T. et al. (2004) Curr. Med. Chem. 11, 3073.
    2. Prorok, M. and Castellino, F.J. (2001) Curr. Drug Targets 2, 313.
    3. Castellino, F.J. and Prorok, M. (2000) Curr. Drug Targets 3, 219.
    4. White, H.S. et al. (2000) J. Pharmacol. Exp. Ther. 292, 425.
    Scientific background

    Conantokin R is a peptide toxin originally isolated from the Conus radiatus (Rayed cone) venom, and preferentially antagonizes GluN2A and GluN2B NMDA receptors1,2,4. Conantokins are a group of short linear peptides (17-27 amino acids) originally isolated from the venom of cone snails. They structurally possess a high degree of alpha-helicity in the presence of divalent cations, and contain gamma-carboxyglutamic acid residues. Four naturally occurring conantokins have been identified and characterized to date, Conantokin G, Conantokin T, Conantokin R, and Conantokin-L1,2.

    Conantokins appear to function by inhibiting the spermine/spermidine stimulation of ion flow through the NMDAR channel and different conantokin species present different NMDA receptor subunit specificity3.

    NMDR inhibition by conantokins is related to various human pathologies including pain, convulsive disorders, stroke, and Parkinson’s disease. The potential pharmacological selectivity of conantokins, coupled to their efficacy in preclinical disease model and favorable safety profiles, indicate that these peptides represent both novel probes for NMDA receptor function as well as an important class of compounds for continued investigation as human therapeutics1.

    Target GluN2B receptor
    Net Peptide Content: 100%

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    Last update: 05/03/2020

    Conantokin R (#STC-777) is a highly pure, synthetic, and biologically active peptide toxin.

    For research purposes only, not for human use
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