1. GPCR/G Protein Neuronal Signaling
  2. mAChR
  3. Fesoterodine fumarate

Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB).

For research use only. We do not sell to patients.

Fesoterodine fumarate Chemical Structure

Fesoterodine fumarate Chemical Structure

CAS No. : 286930-03-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO USD 70 In-stock
Solid
1 mg USD 30 In-stock
5 mg USD 60 In-stock
10 mg USD 96 In-stock
50 mg USD 190 In-stock
100 mg USD 290 In-stock
500 mg USD 560 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB)[1][2].

IC50 & Target

mAChR1

 

mAChR3

 

mAChR4

 

mAChR5

 

In Vitro

FFesoterodine Fumarate decreases micturition frequency, urgency severity and urgency incontinence episodes and increases the volume voided with each micturition[1].
After oral administration, Fesoterodine Fumarate is rapidly and extensively hydrolysed in plasma by nonspecific esterases to Desfesoterodine (5-hydroxymethyl tolterodine; SPM 7605; HY-76569; an active metabolite of Fesoterodine)[3][4].

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

In Vivo

Fesoterodine Fumarate (0.01-1 mg/kg; IV) reduces the micturition pressure and increases bladder capacity and ICIs (intercontraction intervas) at the lowest dose tested of 0.01 mg/kg[3].

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

Animal Model: Bladders from female Sprague-Dawley rats (225-275 g)[3]
Dosage: 0.01, 0.1 and 1 mg/kg
Administration: IV
Result: Reduced the micturition pressure and increased bladder capacity and ICIs at the lowest dose tested of 0.01 mg/kg.
Clinical Trial
Molecular Weight

527.65

Formula

C30H41NO7

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OCC1=CC([C@H](CCN(C(C)C)C(C)C)C2=CC=CC=C2)=C(C=C1)OC(C(C)C)=O.OC(/C=C/C(O)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (189.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 100 mg/mL (189.52 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8952 mL 9.4760 mL 18.9520 mL
5 mM 0.3790 mL 1.8952 mL 3.7904 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 (stored under nitrogen). 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

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

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C2

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Volume (final)

V2

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 (4.74 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 (4.74 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 (189.52 mM); Clear solution; Need ultrasonic

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

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

Purity: 99.73%

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 (stored under nitrogen). 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
DMSO / H2O 1 mM 1.8952 mL 9.4760 mL 18.9520 mL 47.3799 mL
5 mM 0.3790 mL 1.8952 mL 3.7904 mL 9.4760 mL
10 mM 0.1895 mL 0.9476 mL 1.8952 mL 4.7380 mL
15 mM 0.1263 mL 0.6317 mL 1.2635 mL 3.1587 mL
20 mM 0.0948 mL 0.4738 mL 0.9476 mL 2.3690 mL
25 mM 0.0758 mL 0.3790 mL 0.7581 mL 1.8952 mL
30 mM 0.0632 mL 0.3159 mL 0.6317 mL 1.5793 mL
40 mM 0.0474 mL 0.2369 mL 0.4738 mL 1.1845 mL
50 mM 0.0379 mL 0.1895 mL 0.3790 mL 0.9476 mL
60 mM 0.0316 mL 0.1579 mL 0.3159 mL 0.7897 mL
80 mM 0.0237 mL 0.1184 mL 0.2369 mL 0.5922 mL
100 mM 0.0190 mL 0.0948 mL 0.1895 mL 0.4738 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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Fesoterodine fumarate Related Classifications

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  • 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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