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

Fesoterodine L-mandelate 

Cat. No.: HY-70053A Purity: 98.92%
Handling Instructions

Fesoterodine L-mandelate 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 L-mandelate is used for the overactive bladder (OAB).

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

Fesoterodine L-mandelate Chemical Structure

Fesoterodine L-mandelate Chemical Structure

CAS No. : 1206695-46-6

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Based on 1 publication(s) in Google Scholar

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Description

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

563.72

Formula

C₃₄H₄₅NO₆

CAS No.

1206695-46-6

SMILES

O[[email protected]](C(O)=O)C1=CC=CC=C1.O=C(C(C)C)OC2=CC=C(CO)C=C2[[email protected]@H](C3=CC=CC=C3)CCN(C(C)C)C(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
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Keywords:

FesoterodinemAChRMuscarinic acetylcholine receptorantimuscarinicoveractivebladderOABorallyM1M2M3M4M55-HMTDesfesoterodineSPM7605muscarinicreceptorInhibitorinhibitorinhibit

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Fesoterodine L-mandelate
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