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

Cat. No.: HY-90010 Purity: 99.96%: FAQs
Data Sheet SDS COA Handling Instructions

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Tolterodine Tartrate (Kabi-2234; PNU-200583E) is a potent muscarinic receptor antagonist and shows selectivity for the urinary bladder over salivary glands in vivo.

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

Tolterodine tartrate Chemical Structure

CAS No. : 124937-52-6

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 61	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 61	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 35	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 55	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 165	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 231	In-stock	Estimated Time of Arrival: December 31
250 mg	USD 429	In-stock	Estimated Time of Arrival: December 31
500 mg		Get quote
1 g		Get quote

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Purity & Documentation
References
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Description

Tolterodine Tartrate (Kabi-2234; PNU-200583E) is a potent muscarinic receptor antagonist and shows selectivity for the urinary bladder over salivary glands in vivo.

In Vitro

Carbachol-induced contractions of isolated guinea pig bladder were effectively inhibited by tolterodine (IC50 14 nM) and 5-HM (IC50 5.7 nM). The IC50 values were in the microM range and the antimuscarinic potency of tolterodine was 27, 200 and 370-485 times higher, respectively, than its potency in blocking histamine receptors, alpha-adrenoceptors and calcium channels. The active metabolite, 5-HM, was >900 times less potent at these sites than at bladder muscarinic receptors^[1].

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

In Vivo

Tolterodine was extensively metabolized in vivo^[2]. In the passive-avoidance test, tolterodine at 1 or 3 mg/kg had no effect on memory; the latency to cross and percentage of animals crossing were comparable to controls. In contrast, scopolamine induced a memory deficit; the latency to cross was decreased, and the number of animals crossing was increased^[3].

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

Clinical Trial

Molecular Weight

475.57

Formula

C₂₆H₃₇NO₇

CAS No.

124937-52-6

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
10 mM	0.2103 mL	1.0514 mL	2.1027 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.
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

mg/kg

Animal weight
(per animal)

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

Purity: 99.96%

Select Batch:

Data Sheet (273 KB) SDS (727 KB)

COA (248 KB) LCMS (88 KB)

Handling Instructions (2659 KB)

References

[1]. Nilvebrant L. Tolterodine and its active 5-hydroxymethyl metabolite: pure muscarinic receptor antagonists. Pharmacol Toxicol. 2002 May;90(5):260-7. [Content Brief]

[2]. Andersson SH, et al. Biotransformation of tolterodine, a new muscarinic receptor antagonist, in mice, rats, and dogs. Drug Metab Dispos. 1998 Jun;26(6):528-35. [Content Brief]

[3]. Cappon GD, et al. Tolterodine does not affect memory assessed by passive-avoidance response test in mice. Eur J Pharmacol. 2008 Jan 28;579(1-3):225-8. [Content Brief]

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.

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 2234mAChRMuscarinic acetylcholine receptormuscarinicreceptorurinarybladdersalivaryglandsInhibitorinhibitorinhibit

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