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Purity: ≥98%
Solifenacin succinate (formerly YM-905; YM905; Trade name: Vesikur; Vesicare), the succinate salt of solifenacin which is approved for treating overactive bladder, is a novel and potent muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
| ln Vitro |
Solifenacin Succinate (YM905) is a new type of muscarinic receptor antagonist. Its pKis for M1, M2, and M3 receptors are 7.6±0.056, 6.9±0.034, and 8.0±0.021, respectively. The antagonistic effects of oxybutynin and 100 nM solifenacin succinate on Ca2+ mobilization induced by different doses of carbachol (CCh) are investigated in murine submandibular gland cells. While oxybutynin exhibits unbreakable antagonistic interactions, solifenacin succinate does not alter the CCh dose-activation curve in a parallel fashion. For Solifenacin Succinate, the pKb values are 7.4±0.17 and for Oxybutynin, 8.8±0.21[1].
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| ln Vivo |
At 210 nmol/kg (0.1 mg/kg), solifenacin succinate (YM905) decreases bladder reflexes by 40%, and at 2100 nmol/kg (1 mg/kg), it completely eliminates them. On the other hand, at 630 nmol/kg (0.3 mg/kg), its inhibitory effects on salivary and cardiac responses are negligible, and at 2100 nmol/kg (1 mg/kg), they increase to 66% and 49%, respectively. Saliva secretion is marginally increased by solifenacin succinate at dosages of 63 and 210 nmol/kg (0.03 and 0.1 mg/kg)[1]. At dosages of 0.03 mg/kg iv or higher, solifenacin succinate (0.01 to 0.3 mg/kg iv) improves bladder capacity and voided volume in a dose-dependent manner; however, residual volume and micturition pressure are unaffected at any tested dose[2].
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| 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.
[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 overac [3]. Hoffstetter S, Leong FC.Solifenacin succinate for the treatment of overactive bladder.Expert Opin Drug Metab Toxicol. 2009 Mar;5(3):345-50. [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 Cli [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. |
| Molecular Formula |
C23H26N2O.C4H6O4
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| Molecular Weight |
480.55
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| CAS # |
242478-38-2
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| Related CAS # |
Solifenacin;242478-37-1;Solifenacin hydrochloride;180468-39-7;Solifenacin D5 hydrochloride;1426174-05-1;Solifenacin-d5 succinate
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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 |
YM 905 succinate; Solifenacin succinate; YM-905; YM905; Trade name: Vesikur; Vesicare.
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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 (5.20 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 (5.20 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 (5.20 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 50 mg/mL (104.05 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 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 |
*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.
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