Fesoterodine Fumarate

Catalog No.S2240 Synonyms: SPM 907

Fesoterodine Fumarate  Chemical Structure

Molecular Weight(MW): 527.65

Fesoterodine Fumarate is a prodrug of 5-hydroxymethyl tolterodine that is a muscarinic AChR receptor antagonist, used to treat overactive bladder syndrome.

Size Price Stock Quantity  
In DMSO USD 420 In stock
USD 97 In stock
USD 127 In stock
USD 470 In stock
USD 970 In stock

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Notes:

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4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description Fesoterodine Fumarate is a prodrug of 5-hydroxymethyl tolterodine that is a muscarinic AChR receptor antagonist, used to treat overactive bladder syndrome.
Targets
AChR [1]
In vitro

Fesoterodine is rapidly and extensively converted to 5-HMT, such that the pharmacologic activity appears to be primarily attributable to 5-HMT. [1] Fesoterodine is a competitive antagonist of cholinergic agonist-stimulated responses in human M1-M5 cell lines and has a similar potency and selectivity profile to the radioligand-binding studies. Fesoterodine causes a rightward shift of the concentration-response curve for carbachol with no depression of the maximum in rat bladder strips, and concentration-dependently reduces contractions induced by electrical field stimulation (EFS). [2] Fesoterodine is hydrolyzed by nonspecific esterases to 5-hydroxmethyl tolterodine (5-HMT), which is the active metabolite and is responsible for all its antimuscarinic activity. [3]

Protocol

Solubility (25°C)

In vitro DMSO 100 mg/mL (189.51 mM)
Water 100 mg/mL (189.51 mM)
Ethanol 100 mg/mL (189.51 mM)
In vivo

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 527.65
Formula

C26H37NO3.C4H4O4

CAS No. 286930-03-8
Storage powder
in solvent
Synonyms SPM 907

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02240459 Not yet recruiting Overactive Bladder|Mild Cognitive Impairment University of Alberta|Pfizer May 2016 Phase 2
NCT02676154 Recruiting Autonomic Dysreflexia University of British Columbia|Pfizer|International Collaboration On Repair Discoveries (ICORD)|Vancouver Coastal Health February 2016 Phase 2
NCT02614482 Recruiting Overactive Bladder Stéphane Bolduc|Pfizer|Centre Hospitalier Universitaire de Québec, CHU de Québec October 2015 Phase 3
NCT02501928 Recruiting Urinary Bladder, Neurogenic Pfizer June 2015 Phase 3
NCT02385500 Not yet recruiting Urinary Bladder, Overactive|Parkinson Disease Sir Mortimer B. Davis - Jewish General Hospital March 2015 Phase 4
NCT02327936 Enrolling by invitation Overactive Bladder Stéphane Bolduc|Pfizer|Centre Hospitalier Universitaire de Québec, CHU de Québec December 2014 Phase 3

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AChR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID