Gallopamil
Gallopamil (Methoxyverapamil), a methoxy derivative of Verapamil, is a phenylalkylamine calcium antagonist. Gallopamil inhibits acid secretion in a concentration-dependent manner with an IC50 of 10.9 μM. Gallopamil is a potent antiarrhythmic and vasodilator agent.
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- No. CAS: 16662-47-8
- Fòrmula: C28H40N2O5
- Peso molecular:484.63
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.017 μM
Compound: Gallopamil
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Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit
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[PMID: 22761000] |
| NIH-3T3-G185 | IC50 |
3.2 μM
Compound: Gallopamil
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TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells
TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells
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[PMID: 11743742] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats weighing 290-370 g[3]
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Dosage:0.2 mg/kg
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Administration:i.v.; 5 min
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Result:Markedly reduced VT and totally prevented VF.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 16662-47-8
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Appearance Solid
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Peso molecular 484.63
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Fòrmula C28H40N2O5
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Color White to off-white
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SMILES
COC1=C(OC)C(OC)=CC(C(CCCN(C)CCC2=CC(OC)=C(OC)C=C2)(C#N)C(C)C)=C1
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Synonyms
Methoxyverapamil
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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 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (206.34 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (5.16 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.16 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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 (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Brogden RN, et al. Gallopamil. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in ischaemic heart disease. Drugs. 1994 Jan;47(1):93-115. [Content Brief]
[2]. Sewing KF, et al. Calcium channel antagonists verapamil and gallopamil are powerful inhibitors of acid secretion in isolated and enriched guinea pig parietal cells. Pharmacology. 1983;27(1):9-14. [Content Brief]
[3]. Kirchengast M, et al. Reperfusion arrhythmias in closed-chest rats: the effect of myocardial noradrenaline depletion and Ca2(+)-antagonism. Clin Exp Pharmacol Physiol. 1991 Apr;18(4):217-21. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0634 mL | 10.3171 mL | 20.6343 mL | 51.5857 mL |
| 5 mM | 0.4127 mL | 2.0634 mL | 4.1269 mL | 10.3171 mL | |
| 10 mM | 0.2063 mL | 1.0317 mL | 2.0634 mL | 5.1586 mL | |
| 15 mM | 0.1376 mL | 0.6878 mL | 1.3756 mL | 3.4390 mL | |
| 20 mM | 0.1032 mL | 0.5159 mL | 1.0317 mL | 2.5793 mL | |
| 25 mM | 0.0825 mL | 0.4127 mL | 0.8254 mL | 2.0634 mL | |
| 30 mM | 0.0688 mL | 0.3439 mL | 0.6878 mL | 1.7195 mL | |
| 40 mM | 0.0516 mL | 0.2579 mL | 0.5159 mL | 1.2896 mL | |
| 50 mM | 0.0413 mL | 0.2063 mL | 0.4127 mL | 1.0317 mL | |
| 60 mM | 0.0344 mL | 0.1720 mL | 0.3439 mL | 0.8598 mL | |
| 80 mM | 0.0258 mL | 0.1290 mL | 0.2579 mL | 0.6448 mL | |
| 100 mM | 0.0206 mL | 0.1032 mL | 0.2063 mL | 0.5159 mL |
Gallopamil Related Classifications
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