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

Fesoterodine fumarate 

Cat. No.: HY-A0030
Handling Instructions

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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10 mM * 1  mL in DMSO USD 92 In-stock
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5 mg USD 79 In-stock
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10 mg USD 119 In-stock
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50 mg USD 390 In-stock
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100 mg USD 540 In-stock
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500 mg USD 1140 In-stock
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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

pKi: 8.0 (M1), 7.7 (M2), 7.4 (M3), 7.3 (M4) and 7.5 (M5)[3]

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].

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].

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.

286930-03-8

SMILES

OCC1=CC([[email protected]](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)

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
10 mM 0.1895 mL 0.9476 mL 1.8952 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.74 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

FesoterodinemAChRMuscarinic acetylcholine receptorantimuscarinicoveractivebladderOABorallyM1M2M3M4M55-HMTDesfesoterodineSPM7605muscarinicreceptorInhibitorinhibitorinhibit

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Fesoterodine fumarate
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