Art. -Nr.: HY-A0002

Solifenacin Succinate

(Synonyms: YM905)

3 Cited Publications

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Based on 3 publication(s) in Google Scholar

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

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Reinheit: 99.91%
CAS. Nr.: 242478-38-2
Formel: C₂₇H₃₂N₂O₆
Molecular Weight:480.55

Speicherung:

4°C, sealed storage, away from moisture

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

Solifenacin Succinate Chemical Structure

CAS. Nr.: 242478-38-2

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

IC₅₀ & Target

mAChR2

mAChR1

mAChR3

Alle mAChR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	IC₅₀	130.8 nM Compound: YM-905	Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting	[PMID: 21524581]
CHO-K1	IC₅₀	573.7 nM Compound: YM-905	Displacement of [3H]NMS from human muscarinic M2 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting Displacement of [3H]NMS from human muscarinic M2 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting	[PMID: 21524581]
CHO-K1	IC₅₀	63.5 nM Compound: YM-905	Displacement of [3H]NMS from human muscarinic M1 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting Displacement of [3H]NMS from human muscarinic M1 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting	[PMID: 21524581]

In Vitro

Solifenacin Succinate (YM905) is a novel muscarinic receptor antagonist with pK_is 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 Succinate and oxybutynin on Ca²⁺ mobilization evoked by varying doses of carbachol (CCh) are examined. Solifenacin Succinate 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 Succinate and 8.8±0.21 for oxybutynin^[1].

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

In Vivo

Solifenacin Succinate (YM905) 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 Succinate slightly increases saliva secretion^[1]. Solifenacin Succinate (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].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 242478-38-2
Appearance Solid
Molecular Weight 480.55
Formel C₂₇H₃₂N₂O₆
Color White to off-white
SMILES

O=C(O[C@H]1CN2CCC1CC2)N3[C@H](C4=C(CC3)C=CC=C4)C5=CC=CC=C5.O=C(CCC(O)=O)O
Synonyms

YM905
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

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

Publications (3)

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Journal Impact Factor

Int J Nanomedicine

Lactobacillus-Polydopamine System for Targeted Drug Delivery in Overactive Bladder: Evidence from Bladder Cell Spheroids, Rat Models, and Urinary Microbiome Profiling. [Abstract]

2024 Aug 15:19:8353-8371. PMID: 39161357
J Chem Neuroanat

Solifenacin promotes remyelination in cuprizone mouse model by inhibiting the Wnt/β-catenin signaling pathway. [Abstract]

2024 Mar:136:102375. PMID: 38123002
Neurourol Urodyn

Combined treatment with a β3 -adrenergic receptor agonist and a muscarinic receptor antagonist inhibits detrusor overactivity induced by cold stress in spontaneously hypertensive rats. [Abstract]

2017 Apr;36(4):1026-1033. PMID: 27367573

Lösungsmittel & Löslichkeit

In Vitro:

H₂O : 100 mg/mL (208.09 mM; Need ultrasonic)

DMSO : ≥ 100 mg/mL (208.09 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0809 mL

10.4047 mL

20.8095 mL

5 mM

0.4162 mL

2.0809 mL

4.1619 mL

10 mM

0.2081 mL

1.0405 mL

2.0809 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

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

Solubility: ≥ 2.5 mg/mL (5.20 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (5.20 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.20 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS

Solubility: 50 mg/mL (104.05 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact

MedChemExpress (MCE) .

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (418 KB)
- English - EN (418 KB)
- Français - FR (418 KB)
- Deutsch - DE (418 KB)
- Norwegian - NO (418 KB)
- Español - ES (418 KB)
- Swedish - SV (418 KB)
- Italian - IT (418 KB)
- Korean - KR (418 KB)
- Portuguese - PT (418 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

[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. [Content Brief]

[3]. Hoffstetter S, Leong FC.Solifenacin succinate for the treatment of overactive bladder.Expert Opin Drug Metab Toxicol. 2009 Mar;5(3):345-50. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	2.0809 mL	10.4047 mL	20.8095 mL	52.0237 mL
	5 mM	0.4162 mL	2.0809 mL	4.1619 mL	10.4047 mL
	10 mM	0.2081 mL	1.0405 mL	2.0809 mL	5.2024 mL
	15 mM	0.1387 mL	0.6936 mL	1.3873 mL	3.4682 mL
	20 mM	0.1040 mL	0.5202 mL	1.0405 mL	2.6012 mL
	25 mM	0.0832 mL	0.4162 mL	0.8324 mL	2.0809 mL
	30 mM	0.0694 mL	0.3468 mL	0.6936 mL	1.7341 mL
	40 mM	0.0520 mL	0.2601 mL	0.5202 mL	1.3006 mL
	50 mM	0.0416 mL	0.2081 mL	0.4162 mL	1.0405 mL
	60 mM	0.0347 mL	0.1734 mL	0.3468 mL	0.8671 mL
	80 mM	0.0260 mL	0.1301 mL	0.2601 mL	0.6503 mL
	100 mM	0.0208 mL	0.1040 mL	0.2081 mL	0.5202 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

Solifenacin Succinate

3 Cited Publications

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Solifenacin Succinate

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Publications Citing Use of MedChemExpress (MCE) Solifenacin Succinate

Alle mAChR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Solifenacin Succinate

NMPA-Approved Drug Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

FDA Approved & Pharmacopeial Drug Library

Drug-Induced Liver Injury (DILI) Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Mechanoreceptors Compound Library

Rare Diseases Drug Library

FDA-Approved Anticancer Drug Library

Anti-Prostate Cancer Compound Library

Heterocyclic Compound Library

Off-patent Drug Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Drug Repurposing Compound Library

Publications Citing Use of MedChemExpress (MCE) Solifenacin Succinate

Alle mAChR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Solifenacin Succinate Related Classifications

HY-A0002 Related Classifications