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Oxybutynin

Name: Oxybutynin
Brand: Selleck Chemicals
SKU: S1754

Catalog No.S1754 Purity: 99.96%

Oxybutynin is a competitive antagonist of the M1, M2, and M3 subtypes of the muscarinic acetylcholine receptor, used to relieve urinary and bladder difficulties.

Oxybutynin Chemical Structure

CAS: 5633-20-5

Purity & Quality Control

Batch: Purity: 99.96%

99.96

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Biological Activity

Description

Oxybutynin is a competitive antagonist of the M1, M2, and M3 subtypes of the muscarinic acetylcholine receptor, used to relieve urinary and bladder difficulties.

Targets

AChR ^[1]

In vitro
In vitro	Oxybutynin N-deethylation in human liver microsomes in vitro is potently inhibited by ketoconazole (IC50 4.5 mM), less and variably by itraconazole and not by quinidine or several other reference inhibitors, suggesting that CYP3A enzymes are predominant catalysts of the reaction. Oxybutynin inhibits CYP3A4- and CYP2D6- associated activities (testosterone 6 beta-hydroxylase and dextromethorphan O- demethylase, respectively) in human liver microsomes. Oxybutynin is predominantly metabolized by CYP3A4 and CYP3A5 but not by CYP2D6. ^[1] Oxybutynin (30, 100 nM) competitively antagonizes acetylcholine-induced contractions but does not alter those induced by histamine. Oxybutynin (up to 10 mM) induces a non-competitive depression of responses to both agonists and causes a parallel shift to the right of the Ca2+-induced contractions in taenia caeci strips bathed in a Ca2+-free, high-K+ medium. Oxybutynin (1-10 mM) impairs rhythmic muscular contractions in normal medium and after CaCl2 addition in Ca2+-free medium. ^[2] Oxybutynin increases the perfusion pressure starting at 100 mM in perfused rat liver. Oxybutynin also increases the perfusion pressure in the hepatic artery. ^[3]

In Vivo
In vivo	Oxybutynin decreases significantly binding potential (BP) of (+)N-[(11)C]methyl-3-piperidyl benzilate ([(11)C](+)3-MPB) in the rat cerebral cortex and corpus striatum in a dose-dependent manner. ^[4] Oxybutynin induces a significant decrease in micturition pressure without changes in BVC in obstructed rats. ^[5]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT05637671	Recruiting	Vasomotor Symptoms	Cairo University	February 10 2022	Phase 3
NCT04526353	Unknown status	Male Urogenital Diseases	University Hospital Bordeaux	September 10 2020	Phase 2
NCT02522936	Withdrawn	Overactive Bladder\|Xerostomia\|Compliance	University of Southern California	August 1 2018	Phase 4
NCT02099695	Withdrawn	Hyperhidrosis	Cristália Produtos Químicos Farmacêuticos Ltda.\|Hospital Israelita Albert Einstein\|University of Sao Paulo	December 2015	Phase 3

References

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Chemical lnformation & Solubility

Molecular Weight	357.49	Formula	C₂₂H₃₁NO₃
CAS No.	5633-20-5	SDF	Download Oxybutynin SDF
Smiles	CCN(CC)CC#CCOC(=O)C(C1CCCCC1)(C2=CC=CC=C2)O
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 71 mg/mL ( (198.6 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 71 mg/mL

Water : Insoluble

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In vivo
Batch:

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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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