| Bioactivity | 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)[1][2]. |
| Target | IC50: 0.7 nM (hAChE), 7 μM (hBChE) |
| Invitro | 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]. |
| In Vivo | Ambenonium chloride (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 chloride (6 mg/kg; p.o.; daily; 14 d) decreases the number of AChR in motorend-plates[3]. Animal Model: |
| Name | Ambenonium chloride |
| CAS | 115-79-7 |
| Formula | C28H42Cl4N4O2 |
| Molar Mass | 608.47 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. [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. [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. |
Ambenonium chloride
CAS: 115-79-7 F: C28H42Cl4N4O2 W: 608.47
Ambenonium (WIN 8077) chloride is an orally active and reversible inhibitor of Acetyicholinesterase (AChE) with high aff
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