Fenoverine
Based on 1 Customer Validation
Fenoverine (Spasmopriv) is an orally active and powerful anti-spasmodic drug. Fenoverine reduces calcium ion influx by suppressing voltage dependent calcium channels. Fenoverine has antiemetic, analgesic, and antidiarrheal effects. Fenoverine induces rhabdomyolysis. Fenoverine can be used to study smooth muscle overexcitation related conditions such as gastrointestinal spasms.
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- Pureza: 99.69%
- No. CAS: 37561-27-6
- Fòrmula: C26H25N3O3S
- Peso molecular:459.56
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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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Ver todos los productos específicos de isoformas Calcium Channel
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Actividad biológica
Fenoverine (0.5-50 mΜ, 1.5-3 min) inhibits two types of calcium channel currents and is more sensitive to slow channels in smooth muscle cells of rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Tmax | Cmax | T1/2 (Distribution) | T1/2 (Elimination) | Vd/F | CL/F |
|---|---|---|---|---|---|---|---|---|
| Human[3] | 300000 μg | p.o. | 0.758 h | 308 ng/mL | 0.87 h | 49.5 h | 4789 L | 67 L/h |
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 37561-27-6
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Appearance Solid
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Peso molecular 459.56
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Fòrmula C26H25N3O3S
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Color White to off-white
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SMILES
O=C(CN1CCN(CC1)CC2=CC=C3OCOC3=C2)N4C5=C(SC6=C4C=CC=C6)C=CC=C5
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Synonyms
Spasmopriv
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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 (217.60 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 (5.44 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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 (5.44 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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 (276 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. J Mironneau, et al. Fenoverine inhibition of calcium channel currents in single smooth muscle cells from rat portal vein and myometrium. Br J Pharmacol. 1991 Sep;104(1):65-70. [Content Brief]
[2]. Chung-Wen Chen, et al. Rhabdomyolysis induced by fenoverine: a case report and literature review. Acta Neurol Taiwan. 2005 Sep;14(3):143-6. [Content Brief]
[3]. Hu OY, et al. Determination of fenoverine, a modulator of smooth muscle motility, in capsules and in human plasma: application to dosage form stability and a pilot study in humans. J Pharm Sci. 1992 Jan;81(1):91-3. [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 | 2.1760 mL | 10.8800 mL | 21.7599 mL | 54.3999 mL |
| 5 mM | 0.4352 mL | 2.1760 mL | 4.3520 mL | 10.8800 mL | |
| 10 mM | 0.2176 mL | 1.0880 mL | 2.1760 mL | 5.4400 mL | |
| 15 mM | 0.1451 mL | 0.7253 mL | 1.4507 mL | 3.6267 mL | |
| 20 mM | 0.1088 mL | 0.5440 mL | 1.0880 mL | 2.7200 mL | |
| 25 mM | 0.0870 mL | 0.4352 mL | 0.8704 mL | 2.1760 mL | |
| 30 mM | 0.0725 mL | 0.3627 mL | 0.7253 mL | 1.8133 mL | |
| 40 mM | 0.0544 mL | 0.2720 mL | 0.5440 mL | 1.3600 mL | |
| 50 mM | 0.0435 mL | 0.2176 mL | 0.4352 mL | 1.0880 mL | |
| 60 mM | 0.0363 mL | 0.1813 mL | 0.3627 mL | 0.9067 mL | |
| 80 mM | 0.0272 mL | 0.1360 mL | 0.2720 mL | 0.6800 mL | |
| 100 mM | 0.0218 mL | 0.1088 mL | 0.2176 mL | 0.5440 mL |
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