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Oxybutynin AChR antagonist

Name: Oxybutynin
Brand: Selleck Chemicals
SKU: S1754
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S1754

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

Chemical Structure

Molecular Weight: 357.49

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.96%

99.96

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Chemical Information, Storage & Stability

Molecular Weight	357.49	Formula	C₂₂H₃₁NO₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	5633-20-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CCN(CC)CC#CCOC(=O)C(C1CCCCC1)(C2=CC=CC=C2)O

Solubility

In vitro
Batch:

DMSO : 71 mg/mL (198.6 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 71 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10.000mg/ml (27.97mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	AChR ^[1]
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. This compound inhibits CYP3A4- and CYP2D6- associated activities (testosterone 6 beta-hydroxylase and dextromethorphan O- demethylase, respectively) in human liver microsomes. It is predominantly metabolized by CYP3A4 and CYP3A5 but not by CYP2D6. ^[1] This chemical (30, 100 nM) competitively antagonizes acetylcholine-induced contractions but does not alter those induced by histamine. It (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. It (1-10 mM) impairs rhythmic muscular contractions in normal medium and after CaCl2 addition in Ca2+-free medium. ^[2] This compound increases the perfusion pressure starting at 100 mM in perfused rat liver. It also increases the perfusion pressure in the hepatic artery. ^[3]
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] This compound induces a significant decrease in micturition pressure without changes in BVC in obstructed rats. ^[5]
References	[1] https://pubmed.ncbi.nlm.nih.gov/9584328/ [2] https://pubmed.ncbi.nlm.nih.gov/2881993/ [3] https://pubmed.ncbi.nlm.nih.gov/12969440/ [4] https://pubmed.ncbi.nlm.nih.gov/20598326/ [5] https://pubmed.ncbi.nlm.nih.gov/1956871/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
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

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