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Overview
GV-58 (#G-140) is a highly pure, synthetic, and biologically active compound.
Structure
Image & Title 
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.
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.
For research purposes only, not for human use
Applications
Citations (10)
Citations
Powered by BiozProduct citations
- Beske, P.H. et al. (2017) Sci. Rep. 7, 15862.
- Tedeschi, A. et al. (2016) Neuron 92, 419.
Specifications
Properties
Technical Specifications
MW 374.2
Purity >98%
Molecular formula C18H26N6OS.
Form Lyophilized powder.
CAS No. 1402821-41-3
Source Synthetic
Chemical name (2R)-2-[(6-{[(5-Methylthiophen-2-yl)methyl]amino}-9-propyl-9H-purin-2-yl)amino]butan-1-ol.
Biological Activity
Target CaV2.1, CaV2.2 Ca2+ channels
Effective concentration 1-100 µM.
Activity GV-58 is an opener of N- and P/Q-type Ca2+ channels1.
References
- Tarr, T.B. et al. (2013) J. Neurosci. 33, 10559.
Solubility and Storage
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.
Scientific Background
Scientific Background
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.
References
- Tarr, T.B. et al. (2012) Ann. N. Y. Acad. Sci. 1275, 85.
- Liang, M. et al. (2012) ACS Med. Chem. Lett. 3, 985.
Last Update: 08/01/2025
