2. GPCR/G Protein Neuronal Signaling Metabolic Enzyme/Protease
  3. mAChR Cytochrome P450
  4. Tolterodine tartrate

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

Cat. No.: HY-90010 Purity: 98.64%
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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.

Tolterodine tartrate

Tolterodine tartrate Chemical Structure

CAS No. : 124937-52-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
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50 mg In-stock
100 mg In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Tolterodine tartrate:

Tolterodine tartrate Related Antibodies

Top Publications Citing Use of Products

View All mAChR Isoform Specific Products:

View All Isoforms
mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

View All Cytochrome P450 Isoform Specific Products:

View All Isoforms
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

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[1][2][3].

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.

Tolterodine tartrate Related Antibodies

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.
Molecular Weight

475.57

Formula

C26H37NO7
CAS No.
Appearance

Solid

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
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1027 mL 10.5137 mL 21.0274 mL
5 mM 0.4205 mL 2.1027 mL 4.2055 mL
View the 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 (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

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo:

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.

  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: 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
References

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 (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.

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 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tolterodine124937-52-6Kabi-2234 PNU-200583EKabi2234Kabi 2234mAChRCytochrome P450Muscarinic acetylcholine receptorCYPsmuscarinicreceptorurinarybladdersalivaryglandsInhibitorinhibitorinhibit

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