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Tolterodine tartrate

Name: Tolterodine tartrate
Brand: TargetMol
SKU: T0099
Price: 29 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T0099Cas No. 124937-52-6

Alias PNU-200583E, Kabi-2234, Detrol LA

Tolterodine tartrate (PNU-200583E) is a potent antagonist for muscarinic receptor. It show selectivity for the urinary bladder and salivary glands in vivo.

Tolterodine tartrate

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Purity: 99.95%

Catalog No. T0099Alias PNU-200583E, Kabi-2234, Detrol LACas No. 124937-52-6

Tolterodine tartrate (PNU-200583E) is a potent antagonist for muscarinic receptor. It show selectivity for the urinary bladder and salivary glands in vivo.

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$34	In Stock	In Stock
50 mg	$53	In Stock	In Stock
100 mg	$68	In Stock	In Stock
500 mg	$148	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$29	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.95%

Appearance:Solid

Color:White

Resource Download

COA HNMR LCMS

Product Introduction

Tolterodine tartrate AI Summary

Tolterodine tartrate exhibits a multifaceted bioactivity profile. It inhibits cell viability against SARS-CoV-2 infected Vero E6 cells at an MOI of 0.002 after 72 hours, with an inhibition index of 1.165, outperforming the arbidol control. The compound has diverse impacts on cell growth rates across various cell lines, such as HEK293T, U2OS, and human fibroblast cells, indicating differential cellular responses. In thermal shift assays, it shows variable effects on the stability of different protein domains, with both increases and decreases in melting temperatures observed. Additionally, Tolterodine tartrate modulates activity in GPCR beta-arrestin recruitment assays, inhibiting receptors such as C5AR1, APLNR, FFAR4, ADRB2, GPR119, FPR2, GLP1R, CX3CR1, AGTR1, and S1PR1, with significant inhibitory effects ranging from -37.69% to -254.51%. Conversely, it stimulates receptors like APLNR, GPR35, ADRA2A, and ADGRF1, with stimulation up to 34.56%. The compound also displays cytotoxicity towards human HepG2 cells with an IC50 value of 14,200 nM. These diverse interactions and effects suggest that Tolterodine tartrate has a complex and varied pharmacological profile..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Tolterodine tartrate (PNU-200583E) is a potent antagonist for muscarinic receptor. It show selectivity for the urinary bladder and salivary glands in vivo.
Targets&IC50	5-HM:5.7 nM
In vitro	Tolterodine is a novel muscarinic receptor antagonist for the treatment of symptoms such as overactive bladder and urge incontinence.Tolterodine effectively and competitively inhibited carbamylcholine-induced contractions in guinea pig bladder isolation strips in a concentration-dependent manner.Tolterodine has a high affinity for muscarinic receptors, and its Ki values were 2.7 nM, 1.6 nM, 0.75 nM, 4.8 nM, and 3.3 nM in the bladder, heart,, cortex and human bladder in guinea pigs, respectively. The Ki values of Tolterodine in guinea pig bladder, heart, cerebral cortex, parotid gland and human bladder were 2.7 nM, 1.6 nM, 0.75 nM, 4.8 nM and 3.3 nM, respectively.
In vivo	Tolterodine is a novel muscarinic receptor antagonist for the treatment of symptoms such as overactive bladder and urge incontinence.Tolterodine effectively and competitively inhibited carbamylcholine-induced contractions in guinea pig bladder isolation strips in a concentration-dependent manner.Tolterodine has a high affinity for muscarinic receptors, and its Ki values were 2.7 nM, 1.6 nM, 0.75 nM, 4.8 nM, and 3.3 nM in the bladder, heart,, cortex and human bladder in guinea pigs, respectively. The Ki values of Tolterodine in guinea pig bladder, heart, cerebral cortex, parotid gland and human bladder were 2.7 nM, 1.6 nM, 0.75 nM, 4.8 nM and 3.3 nM, respectively.
Synonyms	PNU-200583E, Kabi-2234, Detrol LA

Chemical Properties

Molecular Weight	475.58
Formula	C₂₂H₃₁NO·C₄H₆O₆
Cas No.	124937-52-6
Smiles	O[C@H]([C@@H](O)C(O)=O)C(O)=O.CC(C)N(CC[C@H](c1ccccc1)c1cc(C)ccc1O)C(C)C
Relative Density.	1.003 g/cm3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: 6 mg/mL (12.62 mM), Sonication is recommended.

H2O: 14 mg/mL (29.44 mM), Sonication is recommended.

DMSO: 88 mg/mL (185.04 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (6.94 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1027 mL	10.5135 mL	21.0270 mL	105.1348 mL
5 mM	0.4205 mL	2.1027 mL	4.2054 mL	21.0270 mL
10 mM	0.2103 mL	1.0513 mL	2.1027 mL	10.5135 mL

H2O/DMSO

	1mg	5mg	10mg	50mg
20 mM	0.1051 mL	0.5257 mL	1.0513 mL	5.2567 mL

DMSO

	1mg	5mg	10mg	50mg
50 mM	0.0421 mL	0.2103 mL	0.4205 mL	2.1027 mL
100 mM	0.0210 mL	0.1051 mL	0.2103 mL	1.0513 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc