1. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel
  2. mAChR Potassium Channel
  3. Oxybutynin chloride

Oxybutynin chloride is an oral active and competitive mAChR antagonist with Kis of 14.3 and 5.55 nM for specific [3H]NMS binding in the mouse bladder and cerebral cortex, respectively. Oxybutynin chloride inhibits vascular Kv channels in a manner independent of anticholinergic effect, with an IC50 value of 11.51 μM. Oxybutynin chloride reduces muscle spasm in the bladder and urinary tract, can be used in study of overactive bladder syndrome (OAB). Oxybutynin (chloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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Oxybutynin chloride Chemical Structure

Oxybutynin chloride Chemical Structure

CAS No. : 1508-65-2

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Description

Oxybutynin chloride is an oral active and competitive mAChR antagonist with Kis of 14.3 and 5.55 nM for specific [3H]NMS binding in the mouse bladder and cerebral cortex, respectively. Oxybutynin chloride inhibits vascular Kv channels in a manner independent of anticholinergic effect, with an IC50 value of 11.51 μM. Oxybutynin chloride reduces muscle spasm in the bladder and urinary tract, can be used in study of overactive bladder syndrome (OAB)[1][2]. Oxybutynin (chloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

In Vitro

Oxybutynin chloride (0.1, 0.3, 1, 3, 10, 30, 100 μM; 200 ms) inhibits vascular Kv channels in a concentration-dependent manner independent of anticholinergic effect in coronary arterial smooth muscle cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Coronary arterial smooth muscle cells (from Male New Zealand White rabbits)
Concentration: 10 μM
Incubation Time: 200 ms
Result: Rapidly inhibited the Kv current within 2 min and reduced the Kv current by 44% at +60 Mv.
Inhibited the Kv current by changing the gating properties of Kv channels.

Cell Viability Assay[1]

Cell Line: Coronary arterial smooth muscle cells (from male New Zealand White rabbits)
Concentration: 0.1, 0.3, 1, 3, 10, 30, 100 μM
Incubation Time: 200 ms
Result: Reduced the Kv current amplitude in a concentration-dependent manner, with an IC50 value of 11.51 μM.
In Vivo

Oxybutynin chloride (27.2 mg/kg; p.o.; single) exhibits significant binding of mouse brain muscarinic receptors that about a 2-fold increase in Kd values for specific [3H]N-methylscopolamine binding 0.5 and 2 h later[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male ddY strain mice (9 to 13-week-old)[2].
Dosage: 27.2 mg/kg (76.1 µmol/kg)
Administration: Oral administration; single.
Result: Significant increased Kd values for specific [3H]NMS binding in mouse bladder with values of 54.7% and 40.6% when at 0.5 and 2 hours, respectively.
Significant increased Kd values for specific [3H]NMS binding in mouse cerebral cortex with values of 120% and 71.2% when at 0.5 and 2 hours, respectively.
Clinical Trial
Molecular Weight

393.95

Formula

C22H32ClNO3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C(O)(C1=CC=CC=C1)C2CCCCC2)OCC#CCN(CC)CC.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (253.84 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 33.33 mg/mL (84.60 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5384 mL 12.6920 mL 25.3839 mL
5 mM 0.5077 mL 2.5384 mL 5.0768 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.35 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.35 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 100 mg/mL (253.84 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.5384 mL 12.6920 mL 25.3839 mL 63.4598 mL
5 mM 0.5077 mL 2.5384 mL 5.0768 mL 12.6920 mL
10 mM 0.2538 mL 1.2692 mL 2.5384 mL 6.3460 mL
15 mM 0.1692 mL 0.8461 mL 1.6923 mL 4.2307 mL
20 mM 0.1269 mL 0.6346 mL 1.2692 mL 3.1730 mL
25 mM 0.1015 mL 0.5077 mL 1.0154 mL 2.5384 mL
30 mM 0.0846 mL 0.4231 mL 0.8461 mL 2.1153 mL
40 mM 0.0635 mL 0.3173 mL 0.6346 mL 1.5865 mL
50 mM 0.0508 mL 0.2538 mL 0.5077 mL 1.2692 mL
60 mM 0.0423 mL 0.2115 mL 0.4231 mL 1.0577 mL
80 mM 0.0317 mL 0.1586 mL 0.3173 mL 0.7932 mL
DMSO 100 mM 0.0254 mL 0.1269 mL 0.2538 mL 0.6346 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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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Oxybutynin chloride
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