[CAS NO. 180468-39-7] Solifenacin hydrochloride

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PRODUCTS SPECIFICATIONS [180468-39-7]

Catalog

AS942627

Brand

Arctom Scientific

CAS

180468-39-7

DESCRIPTION [180468-39-7]

Overview

MDL	-
Molecular Weight	398.93
Molecular Formula	C23H27ClN2O2
SMILES	O=C(O[C@H]1CN2CCC1CC2)N3[C@H](C4=C(CC3)C=CC=C4)C5=CC=CC=C5.Cl

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

1 Publications Citing Use of MCE

[1]Neurourol Urodyn. 2017 Apr;36(4):1026-1033.

Summary

Solifenacin hydrochloride (YM905 hydrochloride) is a muscarinic receptor antagonist, with pK _i s of 7.6, 6.9 and 8.0 for M ₁ , M ₂ and M ₃ receptors, respectively.

IC50 & Target

Muscarinic receptor

In Vitro

Solifenacin hydrochloride (YM905 hydrochloride) is a novel muscarinic receptor antagonist with pK _i s of 7.6±0.056, 6.9±0.034 and 8.0±0.021 for M1, M2 and M3 receptors, respectively. In murine submandibular gland cells, the antagonistic effects of 100 nM Solifenacin hydrochloride and oxybutynin on Ca ²⁺ mobilization evoked by varying doses of carbachol (CCh) are examined. Solifenacin hydrochloride does not shift the CCh dose-activation curve in a parallel manner whereas oxybutynin shows insurmountable antagonism. The pK _b values are obtained as 7.4±0.17 for Solifenacin hydrochloride and 8.8±0.21 for oxybutynin ^[1] .

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

In Vivo

Solifenacin hydrochloride (YM905 hydrochloride) reduces bladder responses by 40% at a dose of 210 nmol/kg (0.1 mg/kg) and abolishes them at 2100 nmol/kg (1 mg/kg). In contrast, its inhibitory effects on salivary and cardiac responses are only slight at 630 nmol/kg (0.3 mg/kg), and reach 66% and 49%, respectively, at 2100 nmol/kg (1 mg/kg). At doses of 63 and 210 nmol/kg (0.03 and 0.1 mg/kg), Solifenacin hydrochloride slightly increases saliva secretion ^[1] . Solifenacin hydrochloride (0.01 to 0.3 mg/kg i.v.) dose-dependently increases bladder capacity and voided volume at doses of 0.03 mg/kg i.v. or more, but does not affect residual volume or micturition pressure at any dose tested ^[2] .

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01981954	Astellas Pharma Europe B.V.\|Astellas Pharma Inc	Neurogenic Detrusor Overactivity\|Pediatric	September 25, 2013	Phase 3
NCT01565694	Astellas Pharma Europe B.V.\|Astellas Pharma Inc	Neurogenic Detrusor Overactivity	August 14, 2012	Phase 3
NCT00189800	Astellas Pharma Inc\|Astellas Pharma Korea, Inc.	Overactive Bladder		Phase 3
NCT01764893	Bay State Clinical Trials, Inc.	Overactive Bladder	January 2013	Phase 4
NCT00852696	Cleveland Clinic Florida\|Astellas Pharma US, Inc.\|The Cleveland Clinic	Overactive Bladder	February 2008	Not Applicable
NCT01972841	Astellas Pharma Europe B.V.\|Astellas Pharma Inc	Urinary Bladder Overactive\|Urinary Bladder DiseasesUrologic Diseases\|Overactive Bladder\|Urgency Incontinence	November 5, 2013	Phase 3
NCT01126424	Astellas Pharma Inc	Cognition	April 2010	Phase 4
NCT00463541	Astellas Pharma Inc	Urinary Bladder, Overactive	June 2004	Phase 3
NCT00801944	Astellas Pharma Inc	Urinary Bladder, Overactive	April 2004	Phase 3
NCT02294396	Astellas Pharma Inc	Overactive Bladder (OAB)	October 28, 2014	Phase 4
NCT00909428	Loyola University\|Astellas Pharma Inc	Overactive Bladder Syndrome	January 2007	Phase 4
NCT02667470	Astellas Pharma Inc	Overactive Bladder	September 2009	Phase 4
NCT00985387	Astellas Pharma Inc\|Astellas Pharma Korea, Inc.	Urinary Bladder, Overactive\|Overactive Bladder	August 2009
NCT01539707	Astellas Pharma Inc	Overactive Bladder\|Neurogenic Detrusor Overactivity	March 13, 2012	Phase 1
NCT01565707	Astellas Pharma Europe B.V.\|Astellas Pharma Inc	Urinary Bladder, Overactive	June 7, 2012	Phase 3
NCT00629642	Astellas Pharma Inc	Multiple Sclerosis\|Neurogenic Bladder\|Spinal Cord Diseases	March 14, 2008	Phase 4
NCT01747577	Astellas Pharma Korea, Inc.\|Astellas Pharma Inc	Overactive Bladder\|Benign Prostate Hyperplasia\|Transurethral Resection of Prostate\|Photoselective Vaporization Prostatectomy	December 4, 2012	Phase 4
NCT00441428	University of L´Aquila	Overactive Bladder\|Detrusor Underactivity	February 2006
NCT01777217	Advanced Research Network\|Astellas Pharma US, Inc.	Over-Active Bladder	February 2013	Phase 4
NCT00821184	Lahey Clinic\|Astellas Pharma US, Inc.	Overactive Bladder	September 2006	Phase 3
NCT01833663	Peking Union Medical College Hospital\|Astellas Pharma China, Inc.\|Beijing CAT Science Co., Ltd.	Overactive Bladder\|Postmenopausal Disorder\|Urination Disorders	October 2011	Phase 4
NCT01437670	Asan Medical Center\|Samsung Medical Center\|Seoul National University Hospital\|The Catholic University of Korea\|Ajou University\|Severance Hospital\|Cheil General Hospital and Women´s Healthcare Center\|SMG-SNU Boramae Medical Center\|Pusan National University Yangsan Hospital	Overactive Bladder	September 2011
NCT02494349	Jeil Pharmaceutical Co., Ltd.	LUTS(Lower Urinary Tract Symptoms)\|Benign Prostatic Hyperplasia\|Overactive Bladder	August 2015	Phase 1
NCT01880619	Mansoura University	Relieve of Ureteral Stent Symptoms	January 2013	Phase 4
NCT01457573	Timothy Boone, MD, PhD\|Astellas Pharma US, Inc.\|The Methodist Hospital Research Institute	Lower Urinary Tract Symptoms	October 2011	Phase 4
NCT01638000	Astellas Pharma Europe Ltd.\|Astellas Pharma Inc	Urologic Diseases\|Urinary Bladder, Overactive\|Urinary Bladder Diseases	June 12, 2012	Phase 3
NCT03787654	Guang´anmen Hospital of China Academy of Chinese Medical Sciences	Mixed Urinary Incontinence\|Urgency-predominant Mixed Urinary Incontinence	March 1, 2019	Not Applicable
NCT02180997	Jeil Pharmaceutical Co., Ltd.	LUTS\|Benign Prostatic Hyperplasia\|Overactive Bladder	July 2014	Phase 1
NCT01166438	NICHD Pelvic Floor Disorders Network\|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)	Urge Urinary Incontinence\|Overactive Bladder	March 2010	Phase 3
NCT01371994	Astellas Pharma Inc	Urinary Incontinence	August 2, 2011	Phase 4
NCT01876186	National Taiwan University Hospital	Overactive Bladder Syndrome	May 2013	Phase 4
NCT01799902	Astellas Pharma Europe B.V.\|Veeda Clinical Research\|Astellas Pharma Inc	Lower Urinary Tract Predominant Storage Symptoms	December 2011
NCT04477265	Far Eastern Memorial Hospital	Overactive Bladder	June 16, 2016	Not Applicable
NCT02127034	Astellas Pharma Europe B.V.\|Astellas Pharma Inc	Healthy Subjects\|Pharmacokinetics\|Drug-Drug Interaction (DDI)	March 2014	Phase 1
NCT04437108	Mansoura University	Overactive Bladder\|Urinary Incontinence, Urge\|Urgency-frequency Syndrome\|Post Prostatectomy	July 4, 2020	Not Applicable
NCT04023253	Far Eastern Memorial Hospital	Overactive Bladder Syndrome	August 1, 2019	Phase 3
NCT00802373	Astellas Pharma Inc	Urinary Bladder, Overactive	July 2003	Phase 3
NCT01953887	Astellas Pharma Europe B.V.\|Astellas Pharma Inc	EC905\|Pharmacokinetics\|Healthy Subjects	March 2010	Phase 1
NCT01314781	Cantonal Hospital, Frauenfeld\|Astellas Pharma Inc	Overactive Bladder	January 2012	Phase 4
NCT05490082	Mansoura University	Voiding Disorders	March 1, 2022	Phase 3
NCT01028014	University of Alabama at Birmingham\|Astellas Pharma Inc	Urethral Sphincter Activity	April 2010	Not Applicable
NCT01737411	Klinikum der Universität Köln	Urge Urinary Incontinence	January 2013	Phase 1\|Phase 2
NCT02805452	Center Eugene Marquis	Overactive Bladder	July 2016	Phase 3
NCT01093534	Astellas Pharma Inc	Detrusor Overactivity\|Overactive Bladder	January 2010	Phase 4
NCT01018264	University of South Florida	Overactive Bladder in Parkinson´s Disease	January 2010	Phase 4
NCT05040984	Far Eastern Memorial Hospital	Overactive Bladder Syndrome	April 30, 2021
NCT01092624	Hartford Hospital\|Astellas Pharma Inc	Pelvic Organ Prolapse	March 2010	Phase 4
NCT01262391	Astellas Pharma Inc	Urinary Bladder, Overactive	October 20, 2010	Phase 1
NCT02045862	Astellas Pharma Europe B.V.\|Astellas Pharma Inc	Urinary Bladder Overactive\|Overactive Bladder\|Urgency Incontinence\|Urinary Bladder DiseasesUrologic Diseases	March 17, 2014	Phase 3
NCT01745094	Astellas Pharma Inc	Overactive Bladder	October 1, 2012	Phase 4
NCT00979472	Asan Medical Center\|Astellas Pharma Korea, Inc.	Urinary Bladder, Overactive\|Overactive Bladder	April 2009	Phase 4
NCT01559389	Loyola University\|Astellas Pharma US, Inc.	Urge Urinary Incontinence	March 9, 2012	Phase 4
NCT00431041	Astellas Pharma Inc\|Astellas Pharma Canada, Inc.	Overactive Bladder	December 2006	Phase 4
NCT00368706	Astellas Pharma Inc	Urinary Bladder, Overactive	September 2006	Phase 3
NCT05282069	Dong-A ST Co., Ltd.	Overactive Bladder	May 12, 2022	Phase 3
NCT02087098	Astellas Pharma Europe B.V.\|Astellas Pharma Inc	Urinary Bladder, Overactive	June 2014
NCT02169713	Astellas Pharma Europe B.V.\|Astellas Pharma Inc	Healthy Subjects\|Pharmacokinetics\|Drug-Drug Interaction (DDI)	May 2014	Phase 1
NCT02540707	National Taiwan University Hospital	Overactive Bladder Syndrome	September 2015	Phase 4
NCT00510406	Astellas Pharma Inc	Lower Urinary Tract Symptoms\|Prostatic Hyperplasia	January 2007	Phase 2
NCT00699049	KYU-SUNG LEE\|Astellas Pharma Korea, Inc.\|Samsung Medical Center	Urinary Bladder, Overactive	June 2008	Phase 4
NCT01737918	Klinikum der Universität Köln	Surgical Treatment of Urge Incontinence	January 2013	Phase 1\|Phase 2
NCT03106623	Ono Pharmaceutical Co. Ltd	Overactive Bladder	April 7, 2017	Phase 2
NCT01627145	National Taiwan University Hospital	Overactive Bladder Syndrome	August 2012	Not Applicable
NCT01406158	Astellas Pharma Inc	Pharmacokinetics of Solifenacin Succinate\|Healthy Volunteers	May 2011	Phase 1
NCT04064619	Beni-Suef University	Voiding Disorders	January 1, 2018	Not Applicable
NCT01122563	Astellas Pharma Inc\|Astellas Pharma Indonesia Inc.	Overactive Bladder	September 2009
NCT01423838	Adana Numune Training and Research Hospital\|Kocaeli University\|Akdeniz University\|Cukurova University\|Baskent University\|Ankara University\|University of Gaziantep\|Inonu University\|Gaziosmanpasa University\|Kahramanmaras Sutcu Imam University	Overactive Bladder	September 2011	Phase 4
NCT05494567	Mansoura University	Benign Prostatic Hyperplasia\|Overactive Bladder	November 8, 2021	Phase 4
NCT03602508	Astellas Pharma Singapore Pte. Ltd.\|Astellas Pharma Inc	Overactive Bladder (OAB)	July 20, 2018
NCT01533597	Soonchunhyang University Hospital	Overactive Bladder	December 2010	Phase 4
NCT03572231	Astellas Pharma Singapore Pte. Ltd.\|Astellas Pharma Inc	Overactive Bladder (OAB)	July 19, 2018
NCT03468465	Fundacion para la Formacion e Investigacion Sanitarias de la Region de Murcia	Urinary Incontinence	May 4, 2018	Phase 4
NCT02634489	Astellas Pharma Europe B.V.\|Astellas Pharma Inc	Phase 1\|Healthy\|Benign Prostatic Hyperplasia\|Lower Urinary Tract Symptoms	March 2009	Phase 1
NCT01595152	Rambam Health Care Campus	Urinary Bladder, Overactive	May 2012	Not Applicable
NCT01470001	University of Wisconsin, Madison	Post-micturition Incontinence\|Incontinence	November 2011	Not Applicable
NCT01015040	Astellas Pharma Inc	Bioavailability of Solifenacin Succinate\|Pharmacokinetics of Solifenacin Succinate\|Healthy Volunteers	September 2009	Phase 1
NCT04693897	Chang Gung Memorial Hospital	Overactive Bladder Syndrome\|Detrusor Overactivity	March 1, 2021
NCT02972268	Jeil Pharmaceutical Co., Ltd.	Lower Urinary Tract Symptoms\|Benign Prostatic Hyperplasia	February 1, 2016	Phase 3
NCT01503580	National Taiwan University Hospital	Antimuscarinic Drug	August 2008	Not Applicable
NCT01381120	Barrie Urology Associates\|Astellas Pharma Canada, Inc.	Flank Pain\|Urinary Bladder, Overactive	October 2010	Phase 4
NCT04909255	China Medical University Hospital	Sjogren´s Syndrome\|Overactive Bladder Syndrome	March 23, 2021	Phase 4
NCT00454740	Astellas Pharma Inc	Urinary Bladder, Overactive	June 2004	Phase 3
NCT02452879	Guang´anmen Hospital of China Academy of Chinese Medical Sciences\|Capital Medical University\|Beijing Hospital	Overactive Bladder	October 2014	Not Applicable
NCT01318837	Astellas Pharma Inc\|Astellas Pharma Korea, Inc.	Over Active Bladder	April 2010	Phase 4
NCT00573508	Astellas Pharma Inc	Urinary Bladder, Overactive	August 2007	Phase 4
NCT03558919	Bangabandhu Sheikh Mujib Medical University, Dhaka, Bangladesh	Overactive Bladder	January 1, 2017	Phase 4
NCT00337558	Astellas Pharma Inc\|Astellas Pharma Europe B.V.	Overactive Bladder\|Urinary Incontinence\|Urge Incontinence	May 2006	Phase 4
NCT00771394	Astellas Pharma Inc	Benign Prostatic Hyperplasia\|Benign Prostatic Hypertrophy\|Overactive Bladder	October 2008	Phase 4
NCT03566134	Dong-A ST Co., Ltd.	Overactive Bladder	July 10, 2018	Phase 2
NCT01297192	Astellas Pharma Inc	Healthy Volunteers\|Pharmacokinetics of Mirabegron	March 2009	Phase 1
NCT00832650	Pfizer	Healthy	April 2009	Phase 1
NCT05240456	Mansoura University	Voiding Disorders\|Overactive Bladder	February 2022	Phase 1\|Phase 2
NCT01767519	Allergan	Overactive Bladder\|Urinary Incontinence	March 1, 2013	Phase 3
NCT03632772	Buddhist Tzu Chi General Hospital	Overactive Bladder Syndrome	August 1, 2018	Phase 2
NCT01908829	Astellas Pharma Europe Ltd.\|Astellas Pharma Inc	Urinary Bladder Diseases\|Urinary Bladder Overactive\|Urologic Diseases	July 10, 2013	Phase 3
NCT01655069	Astellas Pharma Europe B.V.\|Astellas Pharma Inc	Urinary Bladder, Overactive	October 4, 2012	Phase 3
NCT00507455	Astellas Pharma Inc	Lower Urinary Tract Symptoms\|Bladder Outlet Obstruction	June 2007	Phase 2
NCT00759577	NYU Langone Health	Overactive Bladder	September 2008	Phase 4
NCT00826527	Seattle Urology Research Center	Urinary Frequency\|Urinary Urgency\|Nocturia	January 2007	Phase 4
NCT01642277	Loyola University\|Astellas Pharma US, Inc.	Overactive Bladder	July 2012	Phase 2
NCT01530373	University of Arkansas	Hot Flashes\|Breast Cancer	February 2012	Phase 2
NCT00884104	KYU-SUNG LEE\|Astellas Pharma Korea, Inc.\|Samsung Medical Center	Overactive Bladder	March 2009	Phase 4
NCT04325880	Mansoura University	Ureteral Stent\|Stent Related Symptoms	December 1, 2021	Phase 3
NCT02827578	IlDong Pharmaceutical Co Ltd	Benign Prostate Hyperplasia	January 2016	Phase 3
NCT01340027	Astellas Pharma Europe B.V.\|Astellas Pharma Inc	Urologic Diseases\|Urinary Bladder Diseases\|Urological Manifestations\|Signs and Symptoms\|Urinary Bladder, Overactive	March 29, 2011	Phase 2
NCT02715024	Astellas Pharma Taiwan, Inc.\|Astellas Pharma Inc	Lower Urinary Tract Symptoms\|Overactive Bladder\|Benign Prostatic Hyperplasia (BPH)	September 2007	Phase 4
NCT00333112	Astellas Pharma Inc	Urinary Incontinence	May 2006	Phase 4
NCT01486706	Michael E. Chua\|St. Luke´s Medical Center, Philippines	Urinary Urgency\|Urinary Frequency\|Nocturia\|Incontinence\|Detrusor Uninhibited Activity\|Quality of Life	October 2010	Phase 2\|Phase 3
NCT00773552	Stamford Hospital	Urinary Urge\|Urge Incontinence\|Overactive Bladder	November 2008	Phase 4
NCT01639794	Astellas Pharma Europe Ltd.\|Astellas Pharma Inc	Lower Urinary Tract Symptoms (LUTS)\|Overactive Bladder (OAB)	February 2012
NCT03149809	VA Office of Research and Development	Overactive Bladder\|Parkinson Disease	March 1, 2018	Phase 3
NCT02094703	Dr Cipto Mangunkusumo General Hospital\|Astellas Pharma Indonesia Inc.\|Pharos Life Corporation	Urinary Tract Infection	April 2013	Phase 4
NCT02549196	Chase Pharmaceuticals Corporation, an affiliate of Allergan plc	Dementia of Alzheimer´s Type	October 7, 2015	Phase 2
NCT01505439	Jeong Gu Lee\|Astellas Pharma Korea, Inc.\|Korea University Anam Hospital	Stress Urinary Incontinence\|Urgency Urinary Incontinence	June 2011	Phase 4
NCT00584090	University of South Florida	Urinary Incontinence\|Parkinson´s Disease	November 2007	Phase 4
NCT02047032	Guang´anmen Hospital of China Academy of Chinese Medical Sciences	Urinary Incontinence	April 2014	Not Applicable
NCT02010944	Astellas Pharma Europe B.V.\|Astellas Pharma Inc	Phase 1\|Bioavailability\|Healthy Subjects	September 2012	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL ( 125.34 mM ; Need ultrasonic)

H ₂ O : 50 mg/mL ( 125.34 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5067 mL	12.5335 mL	25.0671 mL
5 mM	0.5013 mL	2.5067 mL	5.0134 mL
10 mM	0.2507 mL	1.2534 mL	2.5067 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 (250.67 mM); Clear solution; Need ultrasonic
2.

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

Solubility: ≥ 2.75 mg/mL (6.89 mM); Clear solution
3.

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

Solubility: ≥ 2.75 mg/mL (6.89 mM); Clear solution
4.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.75 mg/mL (6.89 mM); Clear solution

* All of the co-solvents are available by MCE.