Art. -Nr.: HY-A0024

Tolterodine

(Synonyms: (R)-(+)-Tolterodine; (+)-Tolterodine; (R)-Tolterodine; PNU-200583)

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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.

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Reinheit: 98.61%
CAS. Nr.: 124937-51-5
Formel: C₂₂H₃₁NO
Molecular Weight:325.49

Speicherung:

Pure form -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Tolterodine Chemical Structure

CAS. Nr.: 124937-51-5

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle mAChR Isoform-spezifische Produkte anzeigen :

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Ventricular myocyte	IC₅₀	0.143 μM Compound: Tolterodine	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	[PMID: 22761000]

In Vitro

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.

ELISA Assay^[2]

Cell Line:

LPS-challenged hBEC 5637
Concentration:

20 μM, 40 μM (co-treated with 10 mg/L LPS)
Incubation Time:

24 h
Result:

Reduced LPS-increased IL-6 levels.
Reduced LPS-increased IL-1β levels.
Reduced LPS-increased TNF-α levels.

Western Blot Analysis^[2]

Cell Line:

LPS-challenged hBEC 5637
Concentration:

20 μM, 40 μM (co-treated with 10 mg/L LPS)
Incubation Time:

24 h
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.

In Vivo

Tolterodine (04-40 mg/kg; oral gavage, oral, intravenous tail vein infusion; single dose, daily for 5 days, daily for 3 months, daily for 7 days) demonstrates rapid, almost complete oral absorption, extensive metabolism with dose-dependent metabolite profiles, rapid elimination (half-life <2 h), and primarily faecal/urinary excretion in CD-1 mice, with no evidence of reduced serum levels with 3 months of repeat dosing^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 124937-51-5
Appearance Oil
Molecular Weight 325.49
Formel C₂₂H₃₁NO
Color Colorless to light yellow
SMILES

CC(C)N(C(C)C)CC[C@H](C1=CC=CC=C1)C2=C(O)C=CC(C)=C2
Synonyms

(R)-(+)-Tolterodine; (+)-Tolterodine; (R)-Tolterodine; PNU-200583
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Pure form	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (6.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (291 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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Tolterodine

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Alle mAChR Isoform-spezifische Produkte anzeigen

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Tolterodine Related Classifications

HY-A0024 Related Classifications