1. Neuronal Signaling
  2. Cholinesterase (ChE)
  3. Ambenonium dichloride tetrahydrate

Ambenonium dichloride tetrahydrate  (Synonyms: WIN 8077 dichloride tetrahydrate)

Cat. No.: HY-118533A
Handling Instructions

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).

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Ambenonium dichloride tetrahydrate Chemical Structure

Ambenonium dichloride tetrahydrate Chemical Structure

CAS No. : 52022-31-8

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Description

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)[1][2].

IC50 & Target

IC50: 0.7 nM (hAChE), 7 μM (hBChE)[1]

In Vitro

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.

In Vivo

Ambenonium dichloride tetrahydrate (6 mg/kg; p.o.; daily; 30-60 d) results an adverse effect on neuromuscular transmission in long-term administration, and induces hypersensitivity to stimulation in myasthenia gravis mice modle[3].
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.

Animal Model: Female Sprague Dawley rats (weight 250 g) with myasthenia gravis[3]
Dosage: 6 mg/kg
Administration: Oral gavage; daily; 14, 30, 60, 90, 360 days (Stop administration 24 h in advance)
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.
Molecular Weight

680.53

Formula

C28H50Cl4N4O6

CAS No.
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Ambenonium dichloride tetrahydrate Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Ambenonium dichloride tetrahydrate
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