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Purity: ≥98%
Tolterodine (also known as PNU-200583E) is a tartrate salt of tolterodine that is a potent and competitive muscarinic receptor antagonist. Tolterodines is an antimuscarinic medication used to treat urinary incontinence symptoms. While older antimuscarinic treatments for overactive bladder specifically target M3 receptors, tolterodine acts on both the M2 and M3 subtypes of muscarinic receptors. Tolterodine targets the bladder more than other parts of the body, so even though it acts on all types of receptors, it has fewer side effects than oxybutynin (which is selective for M3 and M1, but more so in the parotid than in the bladder).
| References |
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| Molecular Formula |
C22H31NO
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|---|---|
| Molecular Weight |
325.48764
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| Exact Mass |
325.24
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| Elemental Analysis |
C, 81.18; H, 9.60; N, 4.30; O, 4.92
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| CAS # |
124937-51-5
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| Related CAS # |
Tolterodine tartrate; 124937-52-6; Tolterodine-d14 hydrochloride; 1217645-16-3
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| Appearance |
Solid powder
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| SMILES |
CC1=CC(=C(C=C1)O)[C@H](CCN(C(C)C)C(C)C)C2=CC=CC=C2
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| InChi Key |
OOGJQPCLVADCPB-HXUWFJFHSA-N
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| InChi Code |
InChI=1S/C22H31NO/c1-16(2)23(17(3)4)14-13-20(19-9-7-6-8-10-19)21-15-18(5)11-12-22(21)24/h6-12,15-17,20,24H,13-14H2,1-5H3/t20-/m1/s1
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| Chemical Name |
2-[(1R)-3-[di(propan-2-yl)amino]-1-phenylpropyl]-4-methylphenol
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| Synonyms |
Detrusitol; Tolterodine; Detrol; PHA-686464B
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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 |
| 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) |
Ethanol: ~120 mg/mL (~368.7 mM)
DMSO: ~100 mg/mL (~307.2 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.39 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 20.8 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: ≥ 2.08 mg/mL (6.39 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 20.8 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: ≥ 2.08 mg/mL (6.39 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0723 mL | 15.3615 mL | 30.7229 mL | |
| 5 mM | 0.6145 mL | 3.0723 mL | 6.1446 mL | |
| 10 mM | 0.3072 mL | 1.5361 mL | 3.0723 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 |
| NCT05362292 | Recruiting | Drug: Tolterodine Tartrate ER Drug: Mirabegron Drug: Placebo |
Incontinence Incontinence, Urinary |
University of California, San Francisco |
October 4, 2022 | Phase 4 |
| NCT05946902 | Recruiting | Drug: Recruiting Drug: mirabegron Drug: tolterodine , mirabegron |
Female Patients With Overactive Bladder Syndrome |
Far Eastern Memorial Hospital | September 12, 2023 | Phase 4 |
| NCT00703703 | Completed | Drug: Darifenacin Drug: Tolterodine Drug: Placebo |
Healthy | Novartis | May 2008 | Phase 1 |
| NCT00413790 | Completed | Drug: Darifenacin Drug: Tolterodine Drug: Placebo |
Healthy | Novartis | November 2006 | Phase 4 |
| November 2006 | Completed | Drug: tolterodine, solifenacin | Antimuscarinic Drug | National Taiwan University Hospital |
August 2008 | Not Applicable |
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