Tolterodine
Based on 1 Customer Validation
Tolterodine ((R)-(+)-Tolterodine) is a mAChR inhibitor and substrate for cytochrome P450 enzymes. Tolterodine competitively binds acetylcholine, reduces sympathetic excitation, and inhibits involuntary bladder muscle contraction. Tolterodine restores the Nrf2/NF-κB signaling pathway, mediates protection against inflammatory response and ferroptosis. Tolterodine ameliorates LPS (HY-D1056)-induced reactive oxygen species production and lipid oxidation. Tolterodine can be used for the research of urinary tract infections and overactive bladder.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.61%
- No. CAS: 124937-51-5
- Fòrmula: C22H31NO
- Peso molecular:325.49
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Almacenamiento:Pure form -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Ventricular myocyte | IC50 |
0.143 μM
Compound: Tolterodine
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Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
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[PMID: 22761000] |
Tolterodine (0-500 μM; 4 h) induced a concentration-dependent reduction in viability of HepG2-CYP3A4 cells, with a TC50 of 414 μM[1].
Tolterodine (20-40 μM; 24 h, co-treated with 10 mg/L LPS) dose-dependently ameliorates LPS-induced oxidative stress in hBEC 5637 cells by reducing intracellular ROS and lipid oxidation (MDA) levels after 24 h of co-treatment with LPS[2].
Tolterodine (20-40 μM; 24 h, co-treated with 10 mg/L LPS) dose-dependently inhibits LPS-induced production of IL-6, IL-1β, and TNF-α in hBEC 5637 cells after 24 h of co-treatment with LPS[2].
Tolterodine (20-40 μM; 24 h, co-treated with 10 mg/L LPS) reduces LPS-induced intracellular Fe2+ accumulation and reverses dysregulated iron homeostasis markers (Ferritin, TFR1) in hBEC 5637 cells after 24 h of co-treatment with LPS[2].
Tolterodine (20-40 μM; 24 h, co-treated with 10 mg/L LPS) dose-dependently attenuates LPS-induced ferroptosis in hBEC 5637 cells by normalizing ferroptosis marker levels and restoring cell viability after 24 h of co-treatment with LPS[2].
Tolterodine (20-40 μM; 24 h, co-treated with 10 mg/L LPS) restores the Nrf2/NF-κB signaling balance in LPS-challenged hBEC 5637 cells after 24 h of co-treatment with LPS[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LPS-challenged hBEC 5637
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Concentration:20 μM, 40 μM (co-treated with 10 mg/L LPS)
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Incubation Time:24 h
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Result:Reduced LPS-increased IL-6 levels.
Reduced LPS-increased IL-1β levels.
Reduced LPS-increased TNF-α levels.
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Cell Line:LPS-challenged hBEC 5637
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Concentration:20 μM, 40 μM (co-treated with 10 mg/L LPS)
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Incubation Time:24 h
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Result:Reversed LPS-induced downregulation of Nrf2 protein levels at 20 and 40 μM.
Reversed LPS-induced upregulation of p-NF-κB p65 protein levels at 20 and 40 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 124937-51-5
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Appearance Oil
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Peso molecular 325.49
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Fòrmula C22H31NO
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Color Colorless to light yellow
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SMILES
CC(C)N(C(C)C)CC[C@H](C1=CC=CC=C1)C2=C(O)C=CC(C)=C2
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Synonyms
(R)-(+)-Tolterodine; (+)-Tolterodine; (R)-Tolterodine; PNU-200583
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Pure form -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (307.23 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 2.08 mg/mL (6.39 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (6.39 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (291 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Stock V, et al. Tolterodine is a novel candidate for assessing CYP3A4 activity through metabolic volatiles to predict drug responses. Sci Rep. 2025;15(1):2462. Published 2025 Jan 20. [Content Brief]
[2]. Wang X, et al. Tolterodine ameliorates inflammatory response and ferroptosis against LPS in human bladder epithelial cells. J Biochem Mol Toxicol. 2024;38(1):e23517. [Content Brief]
[3]. Påhlman I, et al. Pharmacokinetics of tolterodine, a muscarinic receptor antagonist, in mouse, rat and dog. Interspecies relationship comparing with human pharmacokinetics. Arzneimittelforschung. 2001 Feb;51(2):134-44. [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. 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0723 mL | 15.3615 mL | 30.7229 mL | 76.8073 mL |
| 5 mM | 0.6145 mL | 3.0723 mL | 6.1446 mL | 15.3615 mL | |
| 10 mM | 0.3072 mL | 1.5361 mL | 3.0723 mL | 7.6807 mL | |
| 15 mM | 0.2048 mL | 1.0241 mL | 2.0482 mL | 5.1205 mL | |
| 20 mM | 0.1536 mL | 0.7681 mL | 1.5361 mL | 3.8404 mL | |
| 25 mM | 0.1229 mL | 0.6145 mL | 1.2289 mL | 3.0723 mL | |
| 30 mM | 0.1024 mL | 0.5120 mL | 1.0241 mL | 2.5602 mL | |
| 40 mM | 0.0768 mL | 0.3840 mL | 0.7681 mL | 1.9202 mL | |
| 50 mM | 0.0614 mL | 0.3072 mL | 0.6145 mL | 1.5361 mL | |
| 60 mM | 0.0512 mL | 0.2560 mL | 0.5120 mL | 1.2801 mL | |
| 80 mM | 0.0384 mL | 0.1920 mL | 0.3840 mL | 0.9601 mL | |
| 100 mM | 0.0307 mL | 0.1536 mL | 0.3072 mL | 0.7681 mL |
Tolterodine Related Classifications
HY-A0024 Related Classifications
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- Tolterodine
- 124937-51-5
- (R)-(+)-Tolterodine
- (+)-Tolterodine
- (R)-Tolterodine
- PNU-200583
- PNU200583
- PNU 200583
- PNU-200583
- mAChR
- Cytochrome P450
- CYP3A4
- Nrf2/nuclear factor κB signaling pathway
- acetylcholine
- ferroptosis
- hBEC 5637 cells
- HepG2-CYP3A4 cells
- muscarinic choline receptor
- cytochrome P450 enzymes
- CYP2D6
- CYP2C9
- Inhibitor
- inhibitor
- inhibit