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Solifenacin succinate

Muscarinic receptor antagonist CAS# 242478-38-2

Solifenacin succinate

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Chemical structure

Solifenacin succinate

3D structure

Chemical Properties of Solifenacin succinate

Cas No. 242478-38-2 SDF Download SDF
PubChem ID 443937 Appearance Powder
Formula C27H32N2O6 M.Wt 480.55
Type of Compound N/A Storage Desiccate at -20°C
Synonyms YM905
Solubility H2O : 100 mg/mL (208.09 mM; Need ultrasonic)
DMSO : ≥ 100 mg/mL (208.09 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 1-azabicyclo[2.2.2]octan-3-yl (1S)-1-phenyl-3,4-dihydro-1H-isoquinoline-2-carboxylate;butanedioic acid
SMILES C1CN2CCC1C(C2)OC(=O)N3CCC4=CC=CC=C4C3C5=CC=CC=C5.C(CC(=O)O)C(=O)O
Standard InChIKey RXZMMZZRUPYENV-DZSUWJOWSA-N
Standard InChI InChI=1S/C23H26N2O2.C4H6O4/c26-23(27-21-16-24-13-10-18(21)11-14-24)25-15-12-17-6-4-5-9-20(17)22(25)19-7-2-1-3-8-19;5-3(6)1-2-4(7)8/h1-9,18,21-22H,10-16H2;1-2H2,(H,5,6)(H,7,8)/t21?,22-;/m0./s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Solifenacin succinate

DescriptionSolifenacin Succinate(YM905; Vesicare) is a muscarinic receptor antagonist. IC50 value: Target: muscarinic receptor Solifenacin succinate (YM905; Vesicare) is a prescription medication used to treat certain bladder problems.

References:
[1]. Krishna SR, Rao BM, Rao NS.A validated rapid stability-indicating method for the determination of related substances in solifenacin succinate by ultra-fast liquid chromatography.J Chromatogr Sci. 2010 Nov;48(10):807-10. [2]. Ohtake A, Sato S, Sasamata M, Miyata K.The forefront for novel therapeutic agents based on the pathophysiology of lower urinary tract dysfunction: ameliorative effect of solifenacin succinate (Vesicare), a bladder-selective antimuscarinic agent, on overactive bladder symptoms, especially urgency episodes.J Pharmacol Sci. 2010;112(2):135-41. Epub 2010 Feb 4. [3]. Hoffstetter S, Leong FC.Solifenacin succinate for the treatment of overactive bladder.Expert Opin Drug Metab Toxicol. 2009 Mar;5(3):345-50. [4]. Choo MS, Lee JZ, Lee JB, Kim YH, Jung HC, Lee KS, Kim JC, Seo JT, Paick JS, Kim HJ, Na YG, Lee JG.Efficacy and safety of solifenacin succinate in Korean patients with overactive bladder: a randomised, prospective, double-blind, multicentre study.Int J Clin Pract. 2008 Nov;62(11):1675-83. [5]. Imamura T, et al.Combined treatment with a β3 -adrenergic receptor agonist and a muscarinic receptor antagonist inhibits detrusor overactivity induced by cold stress in spontaneously hypertensive rats. Neurourol Urodyn. 2017 Apr;36(4):1026-1033.

Solifenacin succinate Dilution Calculator

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Preparing Stock Solutions of Solifenacin succinate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.0809 mL 10.4047 mL 20.8095 mL 41.619 mL 52.0237 mL
5 mM 0.4162 mL 2.0809 mL 4.1619 mL 8.3238 mL 10.4047 mL
10 mM 0.2081 mL 1.0405 mL 2.0809 mL 4.1619 mL 5.2024 mL
50 mM 0.0416 mL 0.2081 mL 0.4162 mL 0.8324 mL 1.0405 mL
100 mM 0.0208 mL 0.104 mL 0.2081 mL 0.4162 mL 0.5202 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Solifenacin succinate

Solifenacin Succinate(YM905; Vesicare) is a muscarinic receptor antagonist.Solifenacin succinate (YM905; Vesicare) is a prescription medication used to treat certain bladder problems.

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References on Solifenacin succinate

Efficacy and safety of tamsulosin hydrochloride 0.2 mg and combination of tamsulosin hydrochloride 0.2 mg plus solifenacin succinate 5 mg after transurethral resection of the prostate: a prospective, randomized controlled trial.[Pubmed:27698559]

Clin Interv Aging. 2016 Sep 19;11:1301-1307.

OBJECTIVE: The objective of this study was to evaluate the safety and efficacy of tamsulosin hydrochloride 0.2 mg (TAM) and its combination with Solifenacin succinate 5 mg (SOL) after transurethral resection of the prostate (TURP). PATIENTS AND METHODS: The patients were randomized into three groups: TURP (group 1), TURP plus TAM (group 2), and TURP plus TAM + SOL (group 3). Patients in group 2 and group 3 received medication for 4 weeks. The primary efficacy end points were the mean change in total International Prostate Symptom Score (IPSS) and IPSS subscores. The secondary end points included quality-of-life score, Overactive Bladder Symptom Score, and short-form voiding and storage score of International Continence Society. RESULTS: In total, 37 men (31.8%) in group 1, 37 men (31.8%) in group 2, and 42 men (36.2%) in group 3 completed the study. In total IPSS, no significant improvement was seen from baseline to the end of treatment in groups 2 and 3 compared with group 1. However, in group 2, the decrement in the IPSS storage score was smaller than group 1 (P=0.02), and in group 3, the decrement in the IPSS voiding score was smaller than group 1 (P=0.05). In groups 2 and 3 compared with group 1, improvements in the quality of life score, total score of Overactive Bladder Symptom Score, and short-form voiding score and storage score of International Continence Society were not statistically significant. CONCLUSION: Treatment with TAM and combination of TAM and SOL did not have significant additional benefits for lower urinary tract symptoms during the early recovery period after TURP.

Long-term prospective study of the persistence of solifenacin succinate in previously untreated Japanese female patients with overactive bladder.[Pubmed:27520420]

Int J Urol. 2016 Oct;23(10):866-872.

OBJECTIVES: To prospectively evaluate the persistence of solifenacin treatment in previously untreated Japanese female patients with overactive bladder. METHODS: A total of 73 previously untreated Japanese female patients diagnosed with overactive bladder were given 5 mg of solifenacin once daily and prospectively followed for 3 years with periodic evaluations. The drug persistence rate was estimated using the Kaplan-Meier method. If solifenacin had to be terminated or a patient did not come to the hospital to receive a prescription, the reason was determined. RESULTS: After solifenacin treatment, the overactive bladder symptom score and average voided volume were significantly improved and maintained for 3 years. The 6-month, 1-year, 2-year and 3-year persistence rates were 50.7%, 41.1%, 32.9% and 23.3%, respectively. The major reasons for solifenacin therapy discontinuation were symptom resolution (27.4%) and adverse events (20.5%). Patients with nocturia three times or more at baseline had lower persistence than those with nocturia more than three times. Patients without detrusor overactivity at baseline had lower drug persistence than those with detrusor overactivity. CONCLUSIONS: Approximately one-quarter of previously untreated Japanese overactive bladder female patients continue solifenacin treatment for 3 years. Many patients discontinue solifenacin for various reasons, including symptom resolution and adverse events.

Efficacy and Safety of Gabapentin in Comparison to Solifenacin Succinate in Adult Overactive Bladder Treatment.[Pubmed:28150436]

Low Urin Tract Symptoms. 2018 May;10(2):135-142.

OBJECTIVE: To evaluate the efficacy and safety of gabapentin in comparison to Solifenacin succinate and placebo for the treatment of adult patients with overactive bladder (OAB). METHOD: A 12-week, randomized, double-blind, double dummy placebo-controlled, clinical trial was conducted between October 2010 and August 2014 at a tertiary medical center. Eligible and consenting patients included were randomized into three treatment groups (placebo, gabapentin and solifenacin). After a 12-week treatment period, an intention to treat analysis was applied to assess between group differences on the micturitions and urgency episodes per 24 h; which were evaluated by 3-day micturition diary mean change from baseline to post treatment. Health related quality of life (HRQOL) domains were likewise assessed by OAB questionnaire (OAB-q). Adverse event were monitored and summarized. Study results were analyzed at statistical significance of 0.05. (ClinicalTrials.gov ID NCT01486706) RESULT: A total of 94 participants were included for end-study efficacy and safety analysis. Compared to placebo, gabapentin and solifenacin have statistically significant improvement in mean number of micturitions per 24 h (adjusted mean difference [AMD] -1.179, 95%CI -1.98, -0.38; P < 0.001; -1.706, 95%CI -2.52, -0.09; P < 0.001; respectively), and in mean number of urgency episodes per 24 h (AMD -0.903, 95%CI -1.44, -0.37; P < 0.001; -0.896, 95%CI -1.44, -0.35; P < 0.001). Gabapentin also demonstrated significant improvement over the solifenacin in the mean number of nocturia episodes/24 h (AMD -0.607, 95%CI -1.04, -0.18; P < 0.001). Adverse event related to gabapentin treatment was lesser than solifenacin, and comparable to placebo. CONCLUSION: Gabapentin treatment with acceptable safety profile, improves OAB symptoms and HRQOL domains.

Description

Solifenacin Succinate (YM905) is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.

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