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| 5mg |
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| 10mg |
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| 25mg |
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GV-58 is a pupin analog that acts as a novel, potent and selective agonist of N- and P/Q-type Ca2+ channels with EC50 of 7.21/8.81 uM for N-type/P-Q-type Ca2+ channel. It has the potential to be used for treating neuromuscular weakness.
| ln Vitro |
The ability of LEMS to passively transfer neuromuscular junctions is restored by GV-58 (50 μM; 30 minutes) [1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: Upper arm muscle isolated from LEMS mice Tested Concentrations: 50 μM Incubation Duration: 30 minutes Experimental Results: mEPP frequency increased from 3.27 s−1 in vehicle control to 10.45 s−1. A slight boost was shown in the final EPP on the train, which subsequently dropped to 94%. |
| References |
[1]. Tarr TB, et al. Evaluation of a novel calcium channel agonist for therapeutic potential in Lambert-Eaton myasthenic syndrome. J Neurosci. 2013 Jun 19;33(25):10559-67.
[2]. Tarr TB, et al. Complete reversal of Lambert-Eaton myasthenic syndrome synaptic impairment by the combined use of a K+ channel blocker and a Ca2+ channel agonist. J Physiol. 2014 Aug 15;592(16):3687-96. [3]. Meriney SD, et al. Lambert-Eaton myasthenic syndrome: mouse passive-transfer model illuminates disease pathology and facilitates testing therapeutic leads. Ann N Y Acad Sci. 2018 Jan;1412(1):73-81. |
| Molecular Formula |
C₁₈H₂₆N₆OS
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|---|---|
| Molecular Weight |
374.50
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| CAS # |
1402821-41-3
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| SMILES |
CC[C@@H](NC1=NC(NCC2=CC=C(C)S2)=C3N=CN(CCC)C3=N1)CO
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| Synonyms |
GV-58GV 58GV58
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~75 mg/mL (~200.27 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.68 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.68 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6702 mL | 13.3511 mL | 26.7023 mL | |
| 5 mM | 0.5340 mL | 2.6702 mL | 5.3405 mL | |
| 10 mM | 0.2670 mL | 1.3351 mL | 2.6702 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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