Solifenacin
Based on 3 publication(s) in Google Scholar
Solifenacin (YM905 free base) 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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- Pureza: 99.51%
- No. CAS: 242478-37-1
- Fòrmula: C23H26N2O2
- Peso molecular:362.46
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Solifenacin
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Actividad biológica
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mAChR2 |
mAChR1 |
mAChR3 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BV-2 | EC50 |
1300 nM
Compound: 1
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Increase of PGRN level in mouse microglial BV-2 cell relative to control
Increase of PGRN level in mouse microglial BV-2 cell relative to control
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[PMID: 34153473] |
| BV-2 | EC50 |
1300 nM
Compound: Solifenacin
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Induction of progranulin secretion in mouse BV-2 cells
Induction of progranulin secretion in mouse BV-2 cells
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[PMID: 36368496] |
| CHO | IC50 |
4.3 μM
Compound: solifenacin
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Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
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[PMID: 23812503] |
Solifenacin is a novel muscarinic receptor antagonist with pKis 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 and oxybutynin on Ca2+ mobilization evoked by varying doses of carbachol (CCh) are examined. Solifenacin does not shift the CCh dose-activation curve in a parallel manner whereas oxybutynin shows insurmountable antagonism. The pKb values are obtained as 7.4±0.17 for Solifenacin and 8.8±0.21 for oxybutynin[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 242478-37-1
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Appearance Solid
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Peso molecular 362.46
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Fòrmula C23H26N2O2
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Color White to off-white
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SMILES
O=C(O[C@@]1([H])C[N@]2CC[C@@H]1CC2)N3CCC4=CC=CC=C4[C@@H]3C5=CC=CC=C5
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Synonyms
YM905 free base
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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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
Solvente y solubilidad
DMSO : ≥ 50 mg/mL (137.95 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.90 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.90 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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
Cytosolic Ca2+ mobilization is determined in guinea pig detrusor cells. Briefly, single detrusor cells are prepared from epithelium-free bladders, loaded with Fura 2, and suspended in phenol red-free Hanks’ balanced salt solution supplemented with 20 mM HEPES (pH=7.4) and 0.1% bovine serum albumin (HBSS-H/B). A 490 μL aliquot of the cell suspension is continuously stirred, kept at 28°C and monitored for the ratio of fluorescence at 500 nm with excitation at 340 nm to that at 380 nm. To each aliquot, 5 μL of test drug (including Solifenacin) and stimulant solutions are serially added with a 2 min interval, and the peak increase over the level just before stimulation is used for data analysis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Male rats (270 to 320 g) are used in this study. After the measurement of neurological deficits, cystometry is performed. Briefly, conscious rats showing a moderate to severe neurological deficit (score: 4 to13) are placed in a restraining cage. To facilitate drug (including Solifenacin) evaluation, only those animals showing urinary frequency are eligible for study. The bladder is emptied by drainage of urine through the catheter and then continuously re-infused with saline. After stable voiding cycles are established, each rat receives a single intravenous administration of test drug (including Solifenacin) at a volume of 1 ml/kg[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (282 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Ikeda K, et al. 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. [Content Brief]
[2]. Suzuki M, et al. Effects of solifenacin succinate (YM905) on detrusor overactivity in conscious cerebral infarctedrats. Eur J Pharmacol. 2005 Apr 4;512(1):61-6. [Content Brief]
Complete Stock Solution Preparation Table
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7589 mL | 13.7946 mL | 27.5893 mL | 68.9731 mL |
| 5 mM | 0.5518 mL | 2.7589 mL | 5.5179 mL | 13.7946 mL | |
| 10 mM | 0.2759 mL | 1.3795 mL | 2.7589 mL | 6.8973 mL | |
| 15 mM | 0.1839 mL | 0.9196 mL | 1.8393 mL | 4.5982 mL | |
| 20 mM | 0.1379 mL | 0.6897 mL | 1.3795 mL | 3.4487 mL | |
| 25 mM | 0.1104 mL | 0.5518 mL | 1.1036 mL | 2.7589 mL | |
| 30 mM | 0.0920 mL | 0.4598 mL | 0.9196 mL | 2.2991 mL | |
| 40 mM | 0.0690 mL | 0.3449 mL | 0.6897 mL | 1.7243 mL | |
| 50 mM | 0.0552 mL | 0.2759 mL | 0.5518 mL | 1.3795 mL | |
| 60 mM | 0.0460 mL | 0.2299 mL | 0.4598 mL | 1.1496 mL | |
| 80 mM | 0.0345 mL | 0.1724 mL | 0.3449 mL | 0.8622 mL | |
| 100 mM | 0.0276 mL | 0.1379 mL | 0.2759 mL | 0.6897 mL |
Solifenacin Related Classifications
HY-A0034 Related Classifications
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