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Ro 25-6981 maleate

A Potent and Selective Antagonist of GluN2B-Containing NMDA Receptors

Cat #: R-180
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 455.55
    Purity: >99% (HPLC)
    Effective concentration 0.01-100 µM.
    Structure
    Chemical name 4-[(1R,2S)-3-(4-benzylpiperidin-1-yl)-1-hydroxy-2-methylpropyl]phenol;(Z)-but-2-enedioic acid.
    Molecular formula C26H33NO6 ( C22H29NO2 · C4H4O).
    CAS No.: 169274-78-6
    PubChem CID 53250677
    Activity Ro 25-6981 maleate is a potent, NR2B-subunit selective, activity dependent antagonist of NMDA receptors, exhibiting a >5000-fold selectivity for NR2B-containing receptors (IC50 = 0.009 µM) over NR2A-containing receptors (IC50 = 52 µM) 1. Shows neuroprotective effects in vivo in injury2 and disease3 models, as well as anti-depressant, anti-inflammatory and other effects.
    References-Activity
    1. Fischer, G. et al. (1997) J. Pharmacol. Exp. Ther. 283, 1285.
    2. Dong, F. et al. (2017) Cell Mol. Neurobiol. 37, 743.
    3. Loschmann, P.A. et al. (2004) Exp. Neurol. 187, 86.
    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 desiccated at 4°C.
    Solubility Soluble up to 100 mM in DMSO. Soluble up to 10 mM in water with gentle warming. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Store at -20°C. It is recommended to prepare solutions afresh on the day of use, or aliquot stock solutions stored at -20°C to prevent repeated thawing.
    Our bioassay
    • Alomone Labs Ro 25-6981 maleate inhibits NMDA receptor channels expressed in Xenopus oocytes. 
      Alomone Labs Ro 25-6981 maleate inhibits NMDA receptor channels expressed in Xenopus oocytes. 
      A. Representative time course of NR1/NR2A currents, elicited by transient stimulations with 100 µM glutamate + 100 µM glycine every 50 sec, while membrane potential was held at -80 mV. 3 min application (indicated by bar) of 100 µM Ro 25-6981 maleate (#R-180) significantly inhibits current amplitude. B. Superimposed current traces from the recording shown in A, upon application of control and of 100 µM Ro 25-6981 maleate (as indicated).
    References - Scientific background
    1. Fischer, G. et al. (1997) J. Pharmacol. Exp. Ther. 283, 1285.
    2. Dong, F. et al. (2017) Cell Mol. Neurobiol. 37, 743.
    Scientific background

    Ro 25-6981 maleate is a highly potent and selective antagonist of GluN2B-containing NMDA receptors. The compound is an activity dependent antagonist of the receptor and demonstrates 5000 times fold selectivity for NR2B-containing receptors over NR2A-containing receptors1. Ro 25-6981 demonstrates an IC50 value of 0.009 µM towards NR2B-containing receptors and an IC50 of 52 µM towards NR2A-containing receptors1.

    Ro 25-6981 protects cultured cortical neurons against glutamate toxicity and has anti-depressant and anti-inflammatory effects. It can suppress ischemic brain injury by regulating autophagy-related proteins during ischemia1,2.

    NMDA receptors are composed of NR1 including eight different splice variants and NR2A-D. They are activated by the co-agonists glutamate and glycine1,2.

    Target GluN2B
    Last update: 08/06/2021

    Ro 25-6981 maleate (#R-180) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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