[CAS NO. 286930-02-7] Fesoterodine

Name: Fesoterodine
Brand: Arctom Scientific
SKU: AS904087

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PRODUCTS SPECIFICATIONS [286930-02-7]

Distributor

Catalog

AS904087

Brand

Arctom Scientific

CAS

286930-02-7

DESCRIPTION [286930-02-7]

Overview

MDL	-
Molecular Weight	411.58
Molecular Formula	C26H37NO3
SMILES	O=C(C(C)C)OC1=CC=C(CO)C=C1[C@@H](C2=CC=CC=C2)CCN(C(C)C)C(C)C

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

Summary

Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pK _i 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] .

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

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] .

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

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01091519	Pfizer	Urinary Bladder, Overactive	December 2010
NCT01786967	University of North Carolina, Chapel Hill\|National Institute on Aging (NIA)	Urge Urinary Incontinence	September 2012	Phase 3
NCT01566760	Pfizer	Urinary Bladder, Overactive	May 2012	Phase 1
NCT02262936	Mount Sinai Hospital, Canada\|Baycrest\|The Physicians´ Services Incorporated Foundation	Nocturia	July 2015	Phase 2\|Phase 3
NCT00713921	Saint Thomas Health\|Pfizer	Urinary Incontinence\|Bladder Dysfunction	September 15, 2009	Early Phase 1
NCT00806494	Pfizer	Urinary Bladder, Overactive	February 2009	Phase 4
NCT02501928	Pfizer	Urinary Bladder, Neurogenic	June 5, 2015	Phase 3
NCT01054222	Pfizer	Urinary Bladder, Overactive	May 2010	Phase 4
NCT00862745	University of California, San Francisco\|Pfizer	Urge Urinary Incontinence\|Overactive Bladder	January 2009	Phase 4
NCT02327936	Stéphane Bolduc\|Pfizer\|CHU de Quebec-Universite Laval	Overactive Bladder	December 2014	Phase 3
NCT00561951	Pfizer	Overactive Bladder	November 2007	Phase 2
NCT03946124	University of Pennsylvania\|Pfizer	Overactive Bladder	July 25, 2015	Phase 4
NCT00798434	Pfizer	Urinary Bladder, Overactive	June 2008	Phase 4
NCT04090190	Brigham and Women´s Hospital\|Medical University of Silesia	Urinary Incontinence\|Urgency Urinary	October 30, 2019	Phase 4
NCT01936870	Pfizer	Overactive Bladder (OAB)	October 1, 2013
NCT00943735	Pfizer	Overactive Bladder	July 2009
NCT02614482	Stéphane Bolduc\|Pfizer\|CHU de Quebec-Universite Laval	Overactive Bladder	October 2015	Phase 3
NCT00658684	Pfizer	Overactive Bladder	February 2008	Phase 3
NCT00857896	Pfizer	Overactive Bladder\|Neurogenic Detrusor Overactivity	March 2009	Phase 2
NCT02676154	University of British Columbia\|Pfizer\|International Collaboration On Repair Discoveries (ICORD)\|Vancouver Coastal Health	Autonomic Dysreflexia	February 25, 2016	Phase 2
NCT01161472	Pfizer	Healthy	July 2010	Phase 1
NCT03572231	Astellas Pharma Singapore Pte. Ltd.\|Astellas Pharma Inc	Overactive Bladder (OAB)	July 19, 2018
NCT02385500	Sir Mortimer B. Davis - Jewish General Hospital	Urinary Bladder, Overactive\|Parkinson Disease	September 2016	Phase 4
NCT03602508	Astellas Pharma Singapore Pte. Ltd.\|Astellas Pharma Inc	Overactive Bladder (OAB)	July 20, 2018
NCT01260311	Pfizer	Over Active Bladder	February 2011
NCT00786240	Pfizer	Healthy	January 2009	Phase 1
NCT00536484	Pfizer	Overactive Bladder	August 2007	Phase 3
NCT01042236	Pfizer	Stress Urinary Incontinence	January 2009	Phase 2
NCT00928070	Pfizer	Overactive Bladder	September 2009	Phase 4
NCT04452838	Pfizer	Neurogenic Detrusor Overactivity	June 26, 2020	Phase 1
NCT00546637	Pfizer	Overactive Bladder Syndrome	November 2007	Phase 3
NCT00611026	Pfizer	Overactive Bladder	February 2008	Phase 3
NCT00691093	Pfizer	Overactive Bladder\|Urinary Incontinence	July 2008
NCT04478357	Pfizer	Neurogenic Detrusor Overactivity	November 12, 2019	Phase 1
NCT00807118	Pfizer	Therapeutic Equivalency\|Food	October 2008	Phase 1
NCT01605617	Mayo Clinic	Overactive Bladder	June 2012	Phase 4
NCT00832650	Pfizer	Healthy	April 2009	Phase 1
NCT00911937	Pfizer	Overactive Bladder	August 2009	Phase 4
NCT00425100	Pfizer	Overactive Bladder	January 2007	Phase 3
NCT01302054	Pfizer	Urinary Bladder, Overactive	May 2011	Phase 4
NCT00911235	Pfizer	Overactive Bladder With Symptoms of Frequency, Urgency, and Urge Urinary Incontinence	May 2009	Phase 1
NCT01302067	Pfizer	Overactive Bladder	May 2011	Phase 4
NCT01578304	LG Life Sciences\|Kyorin Pharmaceutical Co.,Ltd	Overactive Bladder	December 2010	Phase 4
NCT01557244	Pfizer	Urinary Bladder, Neurogenic	July 2, 2012	Phase 3
NCT00914667	Pfizer	Urinary Bladder, Overactive	July 2009	Phase 1
NCT02160158	Pfizer	Healthy	July 2014	Phase 1
NCT00605319	Weill Medical College of Cornell University\|Pfizer	Bladder Outlet Obstruction	January 2010	Phase 4
NCT01286454	Pfizer	Overactive Bladder (OAB) With Symptoms of Frequency, Urgency, and Urgency	December 2010	Phase 1
NCT00902187	Pfizer	Treatment of Overactive Bladder	May 2009	Phase 1
NCT01661166	Abramson Cancer Center of the University of Pennsylvania	Prostate Adenocarcinoma	January 2012	Phase 4
NCT01595152	Rambam Health Care Campus	Urinary Bladder, Overactive	May 2012	Not Applicable
NCT01367886	Washington University School of Medicine	Overactive Bladder	August 2010	Not Applicable
NCT00444925	Pfizer	Overactive Bladder	April 2007	Phase 3
NCT00902681	Pfizer	Treatment of Overactive Bladder	June 2009	Phase 1
NCT02240459	University of Alberta\|Pfizer	Overactive Bladder\|Mild Cognitive Impairment	August 2016	Phase 2

Appearance

Oil

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

* The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility

In Vitro:

Ethanol : 50 mg/mL ( 121.48 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 available by MCE.

References

Synonyms

Propanoic acid, 2-methyl-, 2-[(1R)-3-[bis(1-methylethyl)amino]-1-phenylpropyl]-4-(hydroxymethyl)phenyl ester

Fesoterodine

(R)-2-(3-Diisopropylamino-1-phenylpropyl)-4-hydroxymethylphenyl isobutyrate