Home Neuronal Signaling AChR antagonist Diphemanil Methylsulfate

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Diphemanil Methylsulfate AChR antagonist

Cat.No.S4034

Diphemanil Methylsulfate is a quaternary ammonium anticholinergic, it binds muscarinic acetycholine receptors (mAchR).
Diphemanil Methylsulfate AChR antagonist Chemical Structure

Chemical Structure

Molecular Weight: 389.51

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Quality Control

Batch: S403401 DMSO]25 mg/mL]false]Water]18 mg/mL]false]Ethanol]Insoluble]false Purity: 99.78%
99.78

Chemical Information, Storage & Stability

Molecular Weight 389.51 Formula

C20H24N.CH3O4S

 Storage (From the date of receipt)
CAS No. 62-97-5 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C[N+]1(CCC(=C(C2=CC=CC=C2)C3=CC=CC=C3)CC1)C.COS(=O)(=O)[O-]

Solubility

In vitro
Batch:

DMSO : 25 mg/mL (64.18 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 18 mg/mL

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
mAChR [1]
In vitro
Diphemanil Methylsulfate exerts its action by primarily binding the muscarinic M3 receptor. In addition to its well known antimuscarinic effects, this compound also possesses direct smooth muscle spasmolytic activity.
In vivo
The pharmacokinetic experiments show that absorption of diphemanil methylsulphate is slow (tmax = 2 to 4 h), the mean half-life is 8.35 h, and the amount of the drug recovered in urine within 48 h ranges from 0.6 to 7.4% of the administered dose[1]. This compound is poorly absorbed from the gastrointestinal tract with an absolute bioavailability of 15 to 25%.
References

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