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An Activator of CaV2.2 and CaV2.1 Ca2+ Channels

Cat #: G-140
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 374.2
    Purity: >98%
    Form Lyophilized powder.
    Effective concentration 1-100 µM.
    Chemical name (2R)-2-[(6-{[(5-Methylthiophen-2-yl)methyl]amino}-9-propyl-9H-purin-2-yl)amino]butan-1-ol.
    Molecular formula C18H26N6OS.
    CAS No.: 1402821-41-3
    Activity GV-58 is an opener of N- and P/Q-type Ca2+ channels1.
    1. Tarr, T.B. et al. (2013) J. Neurosci. 33, 10559.
    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 100 mM in DMSO. Centrifuge all product preparations before use (10000 x g for 1 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs GV-58 increases P/Q-type CaV channel tail currents expressed in Xenopus oocytes.
      Alomone Labs GV-58 increases P/Q-type CaV channel tail currents expressed in Xenopus oocytes.
      A. Time course of CaV2.1 (co-expressed with α2δ1 and β1 auxiliary subunits) normalized tail current area (see tails in panel B, at the end of the ramp stimulation, back at -100 mV), elicited by 100 ms voltage ramp from holding potential of -100 mV to +50 mV (see panel B, top), delivered every 10 seconds. Application of 20 and 100 µM GV-58 (#G-140) increases the CaV2.1 tail current (periods of application are indicated by the horizontal bars) up to 18 fold, in a reversible manner. B. Representative current traces before and during application of 20 and 100 µM GV-58 as indicated. Note the lack of effect on CaV currents during the ramp stimulation.
    References - Scientific background
    1. Tarr, T.B. et al. (2012) Ann. N. Y. Acad. Sci1275, 85.
    2. Liang, M. et al. (2012) ACS Med. Chem. Lett. 3, 985.
    Scientific background

    GV-58, a Ca2+ channel agonist, is selective for N- (CaV2.2) and P/Q-type (CaV2.1) channels. GV-58 was developed as a modification of (R)-roscovitine, which was previously shown to be a Ca2+ channel agonist. 100 μM GV-58 was originally tested on N-, P/Q-, or L-type channels expressed in tsA-201 cells. GV-58 was shown to be more potent on N- and P/Q Ca2+ channels with an EC50 = 6.8 and 9.9 μM, respectively over L-type calcium channels (EC50 > 100 μM)1. GV-58 slows the closing of the channel, resulting in a large increase in total Ca2+ entry during motor nerve action potential activity.

    GV-58 is being tested for the treatment of neuromuscular weakness2.

    Target CaV2.1, CaV2.2 Ca2+ channels
    Image & Title GV-58
    Alomone Labs GV-58 activates presynaptic Ca2+ influx in rat neuronal cells.Representative whole cell recordings of evoked neurotransmission in cultures treated with vehicle or GV-58 (#G-140).Adapted from Beske, P.H. et al. (2017) Sci. Rep. 7, 15862. with permission of SPRINGER NATURE.
    Last update: 06/11/2022

    GV-58 (#G-140) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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