Size | Price | Stock | Qty |
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100mg |
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250mg |
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500mg |
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1g |
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2g |
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10g |
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Purity: ≥98%
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.
Targets |
M1 receptor ( Kd = 2.9 nM ); M2 receptor ( Kd = 6.9 ); M3 receptor ( Kd = 8.0 )
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ln Vitro |
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ln Vivo |
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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].
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Animal Protocol |
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References |
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Molecular Formula |
C23H26N2O2
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Molecular Weight |
362.46
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Exact Mass |
362.2
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CAS # |
242478-37-1
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Related CAS # |
Solifenacin Succinate; 242478-38-2; Solifenacin hydrochloride; 180468-39-7; Solifenacin D5 hydrochloride; 1426174-05-1
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Appearance |
Solid
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SMILES |
C1CN2CCC1[C@H](C2)OC(=O)N3CCC4=CC=CC=C4[C@@H]3C5=CC=CC=C5
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InChi Key |
FBOUYBDGKBSUES-VXKWHMMOSA-N
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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
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Chemical Name |
[(3R)-1-azabicyclo[2.2.2]octan-3-yl] (1S)-1-phenyl-3,4-dihydro-1H-isoquinoline-2-carboxylate
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Synonyms |
YM905; YM 905; YM-905; Solifenacin succinate; Trade name: Vesikur; Vesicare.
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HS Tariff Code |
2934.99.9001
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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)
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Solubility (In Vitro) |
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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. View More
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. |
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.
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.
(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.
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 |