Ambenonium chloride
Based on 1 Customer Validation
Ambenonium (WIN 8077) chloride is an orally active and reversible inhibitor of Acetyicholinesterase (AChE) with high affinity. Ambenonium chloride inhibits human AChE with an IC50 value of 0.7 nM (hAChE).
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- Pureté : 96.18%
- CAS No.: 115-79-7
- Formule: C28H42Cl4N4O2
- Masse moléculaire:608.47
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
IC50: 0.7 nM (hAChE), 7 μM (hBChE)[1]
In Vitro
Ambenonium chloride inhibits Acetyicholinesterase (AChE) in a rapidly reversible method, and shows strong inhibition with inhibition constant Ki of 0.12 nM against hAChE[1].
Ambenonium chloride shows inhibitory effect towards BChE with an IC50 value of 7 μM (hBChE)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Ambenonium chloride (6 mg/kg; p.o.; daily; 14 d) decreases the number of AChR in motorend-plates[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Sprague Dawley rats (weight 250 g) with myasthenia gravis[3]
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Dosage:6 mg/kg
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Administration:Oral gavage; daily; 14, 30, 60, 90, 360 days (Stop administration 24 h in advance)
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Result:Resulted general activity decreasing and hypersensity to stimulation in rats during day 30-60, but these behaviors disappeared on day 90.
Induced degeneration and simplification of the postsynaptic folds, widening of the synaptic clefts, increased number of the postsynaptic vesicles, and reduction in the number of the AChR in the postsynaptic membrane on days 360.
Chemical Information
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CAS No. 115-79-7
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Appearance Solid
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Masse moléculaire 608.47
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Formule C28H42Cl4N4O2
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Color White to off-white
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SMILES
O=C(NCC[N+](CC)(CC)CC1=CC=CC=C1Cl)C(NCC[N+](CC)(CC)CC2=CC=CC=C2Cl)=O.[Cl-].[Cl-]
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Synonyms
WIN 8077 chloride
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
In Vitro:
H2O : ≥ 100 mg/mL (164.35 mM)
* "≥" means soluble, but saturation unknown.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo Dissolution Calculator
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Pureté et documentation
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Fiche technique (272 KB)
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SDS (761 KB)
- English - EN (761 KB)
- Français - FR (761 KB)
- Deutsch - DE (761 KB)
- Norwegian - NO (761 KB)
- Español - ES (761 KB)
- Swedish - SV (761 KB)
- Italian - IT (761 KB)
- Korean - KR (761 KB)
- Portuguese - PT (761 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Hodge AS, et al. Ambenonium is a rapidly reversible noncovalent inhibitor of acetylcholinesterase, with one of the highest known affinities. Mol Pharmacol. 1992 May. 41(5):937-42. [Content Brief]
[2]. Komloova M, et al. Preparation, in vitro screening and molecular modelling of symmetrical bis-quinolinium cholinesterase inhibitors--implications for early myasthenia gravis treatment. Bioorg Med Chem Lett. 2011 Apr 15. 21(8):2505-9. [Content Brief]
[3]. Hazama R, et al. Effects of long-term administration of ambenonium chloride on motor end-plate fine structure and acetylcholine receptor in rat. J Neurol Sci. 1981 Jul. 51(1):69-79. [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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O | 1 mM | 1.6435 mL | 8.2173 mL | 16.4347 mL | 41.0867 mL |
| 5 mM | 0.3287 mL | 1.6435 mL | 3.2869 mL | 8.2173 mL | |
| 10 mM | 0.1643 mL | 0.8217 mL | 1.6435 mL | 4.1087 mL | |
| 15 mM | 0.1096 mL | 0.5478 mL | 1.0956 mL | 2.7391 mL | |
| 20 mM | 0.0822 mL | 0.4109 mL | 0.8217 mL | 2.0543 mL | |
| 25 mM | 0.0657 mL | 0.3287 mL | 0.6574 mL | 1.6435 mL | |
| 30 mM | 0.0548 mL | 0.2739 mL | 0.5478 mL | 1.3696 mL | |
| 40 mM | 0.0411 mL | 0.2054 mL | 0.4109 mL | 1.0272 mL | |
| 50 mM | 0.0329 mL | 0.1643 mL | 0.3287 mL | 0.8217 mL | |
| 60 mM | 0.0274 mL | 0.1370 mL | 0.2739 mL | 0.6848 mL | |
| 80 mM | 0.0205 mL | 0.1027 mL | 0.2054 mL | 0.5136 mL | |
| 100 mM | 0.0164 mL | 0.0822 mL | 0.1643 mL | 0.4109 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Ambenonium chloride Related Classifications
HY-100919 Related Classifications
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