Solifenacin (YM905)

Alias: YM905; YM 905; YM-905; Solifenacin succinate; Trade name: Vesikur; Vesicare.

Cat No.:V3721 Purity: ≥98%

COA Product Data Instructions for use SDS

Solifenacin (YM-905; Vesikur; Vesicare) is a novel and potent muscarinic receptor antagonist that has beenapproved for the treatment of overactive bladder.

Solifenacin (YM905) Chemical Structure CAS No.: 242478-37-1
Product category: mAChR

This product is for research use only, not for human use. We do not sell to patients.

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Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

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J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

MSDS

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information

Product Description

Solifenacin (YM-905; Vesikur; Vesicare) is a novel and potent muscarinic receptor antagonist that has been approved for the treatment of overactive bladder. It blocks muscarinic M1, M2 and M3 receptors with pKis of 7.6, 6.9 and 8.0, respectively.

Biological Activity I Assay Protocols (From Reference)

Targets

M₁ receptor ( Kd = 2.9 nM ); M₂ receptor ( Kd = 6.9 ); M₃ receptor ( Kd = 8.0 )

ln Vitro

In vitro activity: Solifenacin (formerly known as YM905) is a novel muscarinic receptor antagonist that has pK_is values for the M1, M2, and M3 receptors of 7.6±0.056, 6.9±0.034, and 8.0±0.021, respectively. In murine submandibular gland cells, the antagonistic effects of 100 nM Solifenacin and oxybutynin on Ca²⁺ mobilization evoked by varying doses of carbachol (CCh) are examined. Solifenacin does not exhibit parallel shifts in the CCh dose-activation curve, while oxybutynin exhibits unbreakable antagonistic interactions. For Solifenacin and Oxybutynin, the pK_b values are 7.4±0.17 and 8.8±0.21, respectively[1].

ln Vivo

Solifenacin eliminates bladder responses at 2100 nmol/kg (1 mg/kg) and reduces them by 40% at 210 nmol/kg (0.1 mg/kg). By contrast, at 630 nmol/kg (0.3 mg/kg), its inhibitory effects on salivary and cardiac responses are negligible, reaching 66% and 49%, respectively, at 2100 nmol/kg (1 mg/kg). Solifenacin slightly increases salivary secretion at doses of 63 and 210 nmol/kg (0.03 and 0.1 mg/kg)[1]. When administered intravenously at doses of 0.03 mg/kg or higher, solifenacin (0.01 to 0.3 mg/kg) increases bladder capacity and voided volume in a dose-dependent manner. However, it has no effect on residual volume or micturition pressure at any tested dose[2].

Cell Assay

In guinea pig detrusor cells, the mobilization of cytosolic Ca²⁺ is measured. In summary, phenol red-free Hanks' balanced salt solution supplemented with 20 mM HEPES (pH=7.4) and 0.1% bovine serum albumin (HBSS-H/B) is used to prepare single detrusor cells from epithelium-free bladders, load them with Fura 2, and suspend them in the solution. A 490 μL portion of the cell suspension is constantly mixed, maintained at 28°C, and observed for the ratio of fluorescence at 500 nm to that at 380 nm when excited at 340 nm. Five microliters of test drug (such as Solifenacin) and stimulant solutions are successively added to each aliquot at intervals of two minutes. The peak increase over the level immediately prior to stimulation is utilized for data analysis[1].

Animal Protocol

In this study, male rats weighing between 270 and 320 grams are employed. Cystometry is done following the assessment of neurological deficits. In summary, conscious rats with a neurological deficit ranging from 4 to 13 are housed in a restraining cage. Only animals exhibiting frequency of urination are eligible for study, in order to facilitate drug evaluation (including Solifenacin). Urine is drained from the bladder through the catheter, and saline is then continuously infused back into the bladder. A single intravenous injection of the test drug, such as Solifenacin, at a volume of 1 ml/kg is given to each rat once stable voiding cycles have been established[2].

References

[1]. M(3) receptor antagonism by the novel antimuscarinic agent solifenacin in the urinary bladder and salivary gland. Naunyn Schmiedebergs Arch Pharmacol. 2002 Aug;366(2):97-103.

[2]. Effects of solifenacin succinate (YM905) on detrusor overactivity in conscious cerebral infarctedrats. Eur J Pharmacol. 2005 Apr 4;512(1):61-6.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula	C23H26N2O2
Molecular Weight	362.46
Exact Mass	362.2
CAS #	242478-37-1
Related CAS #	Solifenacin Succinate; 242478-38-2; Solifenacin hydrochloride; 180468-39-7; Solifenacin D5 hydrochloride; 1426174-05-1
Appearance	Solid
SMILES	C1CN2CCC1[C@H](C2)OC(=O)N3CCC4=CC=CC=C4[C@@H]3C5=CC=CC=C5
InChi Key	FBOUYBDGKBSUES-VXKWHMMOSA-N
InChi Code	InChI=1S/C23H26N2O2/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/h1-9,18,21-22H,10-16H2/t21-,22-/m0/s1
Chemical Name	[(3R)-1-azabicyclo[2.2.2]octan-3-yl] (1S)-1-phenyl-3,4-dihydro-1H-isoquinoline-2-carboxylate
Synonyms	YM905; YM 905; YM-905; Solifenacin succinate; Trade name: Vesikur; Vesicare.
Storage	Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: ~72 mg/mL (198.6 mM)

Water: <1mg/mL

Ethanol: <1mg/mL

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (6.90 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (6.90 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (6.90 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.7589 mL	13.7946 mL	27.5893 mL
	5 mM	0.5518 mL	2.7589 mL	5.5179 mL
	10 mM	0.2759 mL	1.3795 mL	2.7589 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

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Desired Reconstitution Concentration

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01530373	Active Recruiting	Drug: solifenacin Drug: Clonidine	Hot Flashes Breast Cancer	University of Arkansas	February 2012	Phase 2
NCT05494567	Active Recruiting	Drug: Tadalafil 5mg Drug: solifenacin 10 mg	Benign Prostatic Hyperplasia Overactive Bladder	Mansoura University	November 8, 2021	Phase 4
NCT04023253	Recruiting	Drug: Mirabegron Drug: Solifenacin	Overactive Bladder Syndrome	Far Eastern Memorial Hospital	August 1, 2019	Phase 3
NCT05490082	Completed	Drug: Mirabegron, Propevirine, Solifenacin	Voiding Disorders	Mansoura University	March 1, 2022	Phase 3
NCT04819360	Completed	Drug: VESIcare 10Mg Tablet Drug: Botox 100 UNT Injection	Urinary Bladder, Neurogenic Multiple Sclerosis	Brigitte Schürch	June 1, 2021	Phase 4