Solifenacin Succinate
Based on 3 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 99.91%
- CAS No.: 242478-38-2
- Formula: C27H32N2O6
- Molecular Weight:480.55
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Solifenacin Succinate
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Biological Activity
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mAChR2 |
mAChR1 |
mAChR3 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | IC50 |
130.8 nM
Compound: YM-905
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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] |
Solifenacin Succinate (YM905) 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 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 pKb 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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 242478-38-2
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Appearance Solid
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Molecular Weight 480.55
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Formula C27H32N2O6
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Color White to off-white
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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
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Synonyms
YM905
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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
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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
Solvent & Solubility
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.
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.
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.
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 (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.
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 (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.
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.
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.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (104.05 mM); Clear solution; Need ultrasonic
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.
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.
Purity & Documentation
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Data Sheet (281 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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Handling Instructions (2659 KB)
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. [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]
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, 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.
| 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.