| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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Solifenacin HCl, the hydrochloride salt of Solifenacin (YM-905; YM905; Vesikur; Vesicare), which is an approved medication for the treatment of overactive bladder. It is a muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
| ln Vitro |
Solifenacin Hydrochloride (YM905 HydroHClide) is a novel muscarinic receptor antagonist with pKs of 7.6±0.056, 6.9±0.034, and 8.0±0.021 for M1, M2, and M3 receptors, respectively. The antagonistic effects of 100 nM solifenacin hydrochloride and oxybutynin on Ca2+ mobilization generated by various carbachol (CCh) dosages were investigated in mouse submandibular gland cells. Solifenacin hydrochloride did not modify the CCh dosage activation curve in a similar manner, however oxybutynin demonstrated insurmountable antagonism. Solifenacin hydrochloride has a pKb value of 7.4±0.17, while oxybutynin's is 8.8±0.21 [1].
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| ln Vivo |
At 210 nmol/kg (0.1 mg/kg), solifenacin hydrochloride (YM905 hydrochloride) decreased bladder reactions by 40%, and at 2100 nmol/kg (1 mg/kg), it abolished them. Conversely, at 630 nmol/kg (0.3 mg/kg), its inhibitory effects on the cardiac and salivary responses were negligible, and at 2100 nmol/kg (1 mg/kg), they increased to 66% and 49%, respectively. When solifenacin hydrochloride is administered at doses of 63 and 210 nmol/kg (0.03 and 0.1 mg/kg), salivation is modestly increased [1]. At dosages of 0.03 mg/kg IV and above, solifenacin hydrochloride (0.01 to 0.3 mg/kg IV) improved bladder capacity and urine output in a dose-dependent manner; residual volume and urinary pressure were unaffected[2].
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| References |
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| Molecular Formula |
C₂₃H₂₇CLN₂O₂
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|---|---|
| Molecular Weight |
398.93
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| Exact Mass |
398.176
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| CAS # |
180468-39-7
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| Related CAS # |
Solifenacin Succinate;242478-38-2;Solifenacin;242478-37-1;Solifenacin D5 hydrochloride;1426174-05-1;Solifenacin-d7 hydrochloride
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| PubChem CID |
154058
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| Appearance |
Light yellow to yellow solid powder
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| Boiling Point |
505.5ºC at 760mmHg
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| Melting Point |
120-122ºC
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| Flash Point |
259.5ºC
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| Vapour Pressure |
2.41E-10mmHg at 25°C
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| LogP |
4.542
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
28
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| Complexity |
525
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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.Cl
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| InChi Key |
YAUBKMSXTZQZEB-VROPFNGYSA-N
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| InChi Code |
InChI=1S/C23H26N2O2.ClH/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;1H/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;hydrochloride
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| Synonyms |
YM905 hydrochloride YM-905
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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) |
DMSO : ~50 mg/mL (~125.34 mM)
H2O : ~50 mg/mL (~125.34 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (6.89 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 27.5 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: ≥ 2.75 mg/mL (6.89 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 27.5 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: ≥ 2.75 mg/mL (6.89 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: 100 mg/mL (250.67 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 | 2.5067 mL | 12.5335 mL | 25.0671 mL | |
| 5 mM | 0.5013 mL | 2.5067 mL | 5.0134 mL | |
| 10 mM | 0.2507 mL | 1.2534 mL | 2.5067 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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