Ro 25-6981 maleate

A Potent and Selective Antagonist of GluN2B-Containing NMDA Receptors
  • New
Cat #: R-180
Sizes: 5 mg, 10 mg, 25 mg, 50 mg
  • Promotion
  • Lyophilized Powder
  • Bioassay Tested
  • Shipped at Room Temp.
  • Source: Synthetic
    MW: 455.55 Da.
    Purity >98%.
    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 number 169274-78-6; 1312991-76-6.
    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.
    Storage before reconstitution The product should be stored desiccated at 4°C.
    Reconstitution 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 after reconstitution 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. 
    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
    1. Fischer, G. et al. (1997) J. Pharmacol. Exp. Ther. 283, 1285.
    2. Dong, F. et al. (2017) Cell Mol. Neurobiol. 37, 743.
    Target: GluN2B

    Promotion

    Use code: new-yl30-18
    Valid until January 31st, 2018.

    New website special

    Last update: 25/12/2017

    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.

    Alomone Labs is pleased to offer Ro 25-6981 maleate (#R-180).

    For research purposes only, not for human use