[CAS NO. 286930-03-8] Fesoterodinefumarate

Name: Fesoterodinefumarate
Brand: Arctom Scientific
SKU: AS904877

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PRODUCTS SPECIFICATIONS [286930-03-8]

Distributor

Catalog

AS904877

Brand

Arctom Scientific

CAS

286930-03-8

DESCRIPTION [286930-03-8]

Overview

MDL	MFCD12756004
Molecular Weight	527.65
Molecular Formula	C30H41NO7
SMILES	OCC1=CC([C@H](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

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

Summary

Fesoterodine Fumarate 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 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] .

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

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] .

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

Appearance

Solid

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)

H ₂ O : 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: PBS

Solubility: 100 mg/mL (189.52 mM); Clear solution; Need ultrasonic
2.

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
3.

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
4.

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 available by MCE.

References

Synonyms

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

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

Fesoterodine fumarate

SMP 8272

SPM 907

Toviaz