GV-58
Based on 2 publication(s) in Google Scholar
GV-58 is a novel N- and P/Q-type calcium (Ca2+) channel agonist with EC50s of 7.21 and 8.81 μM, respectively. GV-58 slows the deactivation of channels, resulting in a large increase in presynaptic Ca2+ entry during activity. GV-58 can be used in lambert-eaton myasthenic syndrome (LEMS) research.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.22%
- No. CAS: 1402821-41-3
- Fòrmula: C18H26N6OS
- Peso molecular:374.50
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) GV-58
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Actividad biológica
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N-type calcium channel 7.21 μM (EC50) |
P/Q-type calcium channel 8.81 μM (EC50) |
GV-58 (50 μM; 30 min) restores function in LEMS passive transfer neuromuscular junction[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Upper arm muscle isolated from LEMS mice
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Concentration:50 μM
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Incubation Time:30 min
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Result:Increased the mEPP frequency from 3.27 s−1 in vehicle controls to 10.45 s−1.
Showed a slight facilitation followed by depression to ∼94% at the final EPP in the train.
Chemical Information
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No. CAS 1402821-41-3
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Appearance Solid
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Peso molecular 374.50
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Fòrmula C18H26N6OS
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Color Off-white to light brown
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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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Cell Discov
Cancer cells sense solid stress to enhance metastasis by CKAP4 phase separation-mediated microtubule branching. [Abstract]2024 Nov 12;10(1):114. PMID: 39528501 -
Br J Pharmacol
Contributions of synaptic energetic dysfunction by microtubule dynamics and microtubule-based mitochondrial transport disorder to morphine tolerance. [Abstract]2025 May 13. PMID: 40361281
Solvente y solubilidad
DMSO : 100 mg/mL (267.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.68 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6702 mL | 13.3511 mL | 26.7023 mL | 66.7557 mL |
| 5 mM | 0.5340 mL | 2.6702 mL | 5.3405 mL | 13.3511 mL | |
| 10 mM | 0.2670 mL | 1.3351 mL | 2.6702 mL | 6.6756 mL | |
| 15 mM | 0.1780 mL | 0.8901 mL | 1.7802 mL | 4.4504 mL | |
| 20 mM | 0.1335 mL | 0.6676 mL | 1.3351 mL | 3.3378 mL | |
| 25 mM | 0.1068 mL | 0.5340 mL | 1.0681 mL | 2.6702 mL | |
| 30 mM | 0.0890 mL | 0.4450 mL | 0.8901 mL | 2.2252 mL | |
| 40 mM | 0.0668 mL | 0.3338 mL | 0.6676 mL | 1.6689 mL | |
| 50 mM | 0.0534 mL | 0.2670 mL | 0.5340 mL | 1.3351 mL | |
| 60 mM | 0.0445 mL | 0.2225 mL | 0.4450 mL | 1.1126 mL | |
| 80 mM | 0.0334 mL | 0.1669 mL | 0.3338 mL | 0.8344 mL | |
| 100 mM | 0.0267 mL | 0.1335 mL | 0.2670 mL | 0.6676 mL |