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

Fesoterodine 

Cat. No.: HY-70053 Purity: 97.26%
Handling Instructions

Fesoterodine 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 is used for the overactive bladder (OAB).

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

Fesoterodine Chemical Structure

Fesoterodine Chemical Structure

CAS No. : 286930-02-7

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Based on 1 publication(s) in Google Scholar

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Description

Fesoterodine 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 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

Fesoterodine decreases micturition frequency, urgency severity and urgency incontinence episodes and increases the volume voided with each micturition[1].
After oral administration, Fesoterodine 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 (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.
Molecular Weight

411.58

Formula

C₂₆H₃₇NO₃

CAS No.

286930-02-7

SMILES

O=C(C(C)C)OC1=CC=C(CO)C=C1[[email protected]@H](C2=CC=CC=C2)CCN(C(C)C)C(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Pure form -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

Ethanol : 100 mg/mL (242.97 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4297 mL 12.1483 mL 24.2966 mL
5 mM 0.4859 mL 2.4297 mL 4.8593 mL
10 mM 0.2430 mL 1.2148 mL 2.4297 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% EtOH    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.75 mg/mL (6.68 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.75 mg/mL (6.68 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.75 mg/mL (6.68 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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Product Name:
Fesoterodine
Cat. No.:
HY-70053
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