Ambenonium dichloride tetrahydrate
Ambenonium (WIN 8077) dichloride tetrahydrate is an orally active and reversible inhibitor of Acetyicholinesterase (AChE) with high affinity. Ambenonium dichloride tetrahydrate inhibits human AChE with an IC50 value of 0.7 nM (hAChE).
For research use only. We do not sell to patients.
- CAS No.: 52022-31-8
- Formula: C28H50Cl4N4O6
- Molecular Weight:680.53
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
IC50: 0.7 nM (hAChE), 7 μM (hBChE)[1]
Ambenonium dichloride tetrahydrate inhibits Acetyicholinesterase (AChE) in a rapidly reversible method, and shows strong inhibition with inhibition constant Ki of 0.12 nM against hAChE[1].
Ambenonium dichloride tetrahydrate 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.
Ambenonium dichloride tetrahydrate (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 day 360.
Chemical Information
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CAS No. 52022-31-8
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Molecular Weight 680.53
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Formula C28H50Cl4N4O6
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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-].O.O.O.O
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Synonyms
WIN 8077 dichloride tetrahydrate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Ambenonium dichloride tetrahydrate Related Classifications
HY-118533A Related Classifications
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