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GV-58

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.
    Structure
    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.
    References-Activity
    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: 12/08/2021

    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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