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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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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Because there is no published experience with solifenacin during breastfeeding and it has a long half-life averaging 55 hours, an alternate drug may be preferred, especially while nursing a newborn or preterm infant. Long-term use of solifenacin might reduce milk production or milk letdown. During long-term use, observe the infant for signs of decreased milk production (e.g., insatiety, poor weight gain) and for anticholinergic symptoms (e.g., constipation, urinary retention, UTI, dry mouth). ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Anticholinergics can inhibit lactation in animals, apparently by inhibiting growth hormone and oxytocin secretion. Anticholinergic drugs can also reduce serum prolactin in nonnursing women. The prolactin level in a mother with established lactation may not affect her ability to breastfeed. |
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| References |
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| Additional Infomation |
Solifenacin succinate is a member of isoquinolines.
A quinuclidine and tetrahydroisoquinoline derivative and selective M3 MUSCARINIC ANTAGONIST. It is used as a UROLOGIC AGENT in the treatment of URINARY INCONTINENCE. See also: Solifenacin (has active moiety). Drug Indication Treatment of neurogenic detrusor overactivity |
| Molecular Formula |
C23H26N2O.C4H6O4
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|---|---|
| Molecular Weight |
480.55
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| Exact Mass |
480.226
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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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| PubChem CID |
216457
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| Appearance |
White to off-white solid powder
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| Density |
1.24g/cm3
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| Boiling Point |
505.5ºC at 760 mmHg
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| Melting Point |
147 °C
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| Flash Point |
259.5ºC
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| Vapour Pressure |
2.41E-10mmHg at 25°C
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| Index of Refraction |
1.648
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| LogP |
3.676
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
35
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| Complexity |
617
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C1CN2CCC1[C@H](C2)OC(=O)N3CCC4=CC=CC=C4[C@@H]3C5=CC=CC=C5.C(CC(=O)O)C(=O)O
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| InChi Key |
RXZMMZZRUPYENV-VROPFNGYSA-N
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| InChi Code |
InChI=1S/C23H26N2O2.C4H6O4/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;5-3(6)1-2-4(7)8/h1-9,18,21-22H,10-16H2;1-2H2,(H,5,6)(H,7,8)/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;butanedioic acid
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| Synonyms |
YM 905 succinate; Solifenacin succinate; YM-905; YM905; 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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05798403 | Recruiting | Device: electroacupuncture Drug: Solifenacin Succinate Tablets |
Overactive Bladder | Shanghai University of Traditional Chinese Medicine |
July 7, 2023 | Not Applicable |
| NCT01981954 | Completed Has Results | Drug: Solifenacin succinate | Neurogenic Detrusor Overactivity Pediatric |
Astellas Pharma Europe B.V. | September 25, 2013 | Phase 3 |
| NCT01655069 | Completed Has Results | Drug: Solifenacin succinate suspension | Urinary Bladder, Overactive | Astellas Pharma Europe B.V | October 4, 2012 | Phase 3 |
| NCT01371994 | Completed Has Results | Drug: solifenacin succinate Drug: Placebo |
Urinary Incontinence | Astellas Pharma Inc | August 2, 2011 | Phase 4 |
| NCT01777217 | Terminated Has Results | Drug: Solifenacin succinate Drug: Placebo | Over-Active Bladder | Advanced Research Network | February 2013 | Phase 4 |
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