Cat. No.: HY-90010

Tolterodine tartrate

(Synonyms: Kabi-2234; PNU-200583E)

Customer Review

Based on 1 Customer Validation

Tolterodine tartrate (Kabi-2234) is a mAChR inhibitor and substrate for cytochrome P450 enzymes. Tolterodine tartrate competitively binds acetylcholine, reduces sympathetic excitation, and inhibits involuntary bladder muscle contraction. Tolterodine tartrate restores the Nrf2/NF-κB signaling pathway, mediates protection against inflammatory response and ferroptosis. Tolterodine tartrate ameliorates LPS (HY-D1056)-induced reactive oxygen species production and lipid oxidation. Tolterodine tartrate can be used for the research of urinary tract infections and overactive bladder.

For research use only. We do not sell to patients.

Purity: 98.64%
CAS No.: 124937-52-6
Formula: C₂₆H₃₇NO₇
Molecular Weight:475.57

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Tolterodine tartrate Chemical Structure

CAS No.: 124937-52-6

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Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All mAChR Isoforms :

All Cytochrome P450 Isoforms :

In Vitro

Tolterodine (0-500 μM; 4 h) tartrate 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) tartrate 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) tartrate 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) tartrate 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) tartrate 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) tartrate 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) tartrate 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.

Chemical Information

CAS No. 124937-52-6
Appearance Solid
Molecular Weight 475.57
Formula C₂₆H₃₇NO₇
Color White to off-white
SMILES

OC1=CC=C(C=C1[C@H](CCN(C(C)C)C(C)C)C2=CC=CC=C2)C.O=C([C@@H]([C@H](C(O)=O)O)O)O
Synonyms

Kabi-2234; PNU-200583E
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (210.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 16.67 mg/mL (35.05 mM; Need ultrasonic)

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

2.1027 mL

10.5137 mL

21.0274 mL

5 mM

0.4205 mL

2.1027 mL

4.2055 mL

10 mM

0.2103 mL

1.0514 mL

2.1027 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

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Volume _(final) Volume _(final)

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: ≥ 2.5 mg/mL (5.26 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.26 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.26 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact

MedChemExpress (MCE) .

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (288 KB)
SDS (787 KB)
- English - EN (787 KB)
- Français - FR (787 KB)
- Deutsch - DE (787 KB)
- Norwegian - NO (787 KB)
- Español - ES (787 KB)
- Swedish - SV (787 KB)
- Italian - IT (787 KB)
- Korean - KR (787 KB)
- Portuguese - PT (787 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)

References

[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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	2.1027 mL	10.5137 mL	21.0274 mL	52.5685 mL
	5 mM	0.4205 mL	2.1027 mL	4.2055 mL	10.5137 mL
	10 mM	0.2103 mL	1.0514 mL	2.1027 mL	5.2568 mL
	15 mM	0.1402 mL	0.7009 mL	1.4018 mL	3.5046 mL
	20 mM	0.1051 mL	0.5257 mL	1.0514 mL	2.6284 mL
	25 mM	0.0841 mL	0.4205 mL	0.8411 mL	2.1027 mL
	30 mM	0.0701 mL	0.3505 mL	0.7009 mL	1.7523 mL
DMSO	40 mM	0.0526 mL	0.2628 mL	0.5257 mL	1.3142 mL
	50 mM	0.0421 mL	0.2103 mL	0.4205 mL	1.0514 mL
	60 mM	0.0350 mL	0.1752 mL	0.3505 mL	0.8761 mL
	80 mM	0.0263 mL	0.1314 mL	0.2628 mL	0.6571 mL
	100 mM	0.0210 mL	0.1051 mL	0.2103 mL	0.5257 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Tolterodine tartrate

Bioactive Compound Library Max

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All mAChR Isoforms

All Cytochrome P450 Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Tolterodine tartrate Related Classifications

HY-90010 Related Classifications