Retigabine dihydrochloride

D-23129, Ezogabine, Trobalt®, Potiga®
A Potent and Selective Modulator of KCNQ Channels
    Cat #: R-101
    Alternative Name D-23129, Ezogabine, Trobalt®, Potiga®
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 376.2
    Purity: >98%
    Effective concentration 0.1-100 µM
      • Retigabine dihydrochloride
    Chemical name Ethyl N-[2-amino-4-[(4-fluorophenyl)methylamino]phenyl]carbamate dihydrochloride.
    Molecular formula C16H20Cl2FN3O2.
    CAS No.: 150812-13-8.
    Activity Retigabine is a potent and selective KCNQ (KV7, M-) channel modulator (enhancer)1.
      • Main, M.J. et al. (2000) Mol. Pharmacol. 58, 253.
    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 Water. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
      • Retigabine dihydrochloride
        Alomone Labs Retigabine dihydrochloride modulates KCNQ2/KCNQ3 voltage-gated K+ currents expressed in Xenopus oocytes.
        A. Time course of KCNQ2/KCNQ3 current enhancement by 10 and 100 µM Retigabine dihydrochloride (#R-101) as measured at -50 mV. Currents were elicited by application of voltage ramp from a holding potential of -100 mV to 0 mV (800 msec). B. Superimposed example traces of current responses before and during perfusion of 10 and 100 µM Retigabine dihydrochloride, as indicated.
    References - Scientific background
      • The KCNQ family of voltage-gated K+ channels includes 5 known members: KCNQ1 to KCNQ5. Structurally, the KCNQ family belongs to the six transmembrane domain category of K+ channels. KCNQ family members can form either homomultimeric or heteromultimeric channels with different functional consequences. For example, KCNQ2 and KCNQ3 heteromultimers give rise to a much larger channel current than when either protein is expressed alone. Indeed, KCNQ2/KCNQ3 heteromultimers are believed to be the molecular correlates of the so-called M current. This current is a K+ neuronal current that is strongly inhibited by the activation of the M1 subtype of the muscarinic acetylcholine receptor. Mutations in either KCNQ2 or KCNQ3 are associated with a form of epilepsy known as benign familial neonatal convulsions (BNFC)1-3.

        Retigabine is a potent and selective KCNQ (KV7, M-) channel modulator (enhancer)4-7, which is used in the clinic to treat epilepsy8. Retigabine (0.1 to 10 µM) induced a K+ current and hyperpolarized CHO cells expressing KV7.2/3 cells5 as well as other channels in the following order: KV7.3 > KV7.2/3 > KV7.2 > KV7.46. Similar effects were seen with 10 µM retigabine in oocytes expressing the KV7.2/3 heteromeric channel7.

    Target KCNQ2, KCNQ3, KCNQ4 K+ channels
    Last update: 24/01/2020

    Retigabine dihydrochloride (#R-101) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use