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Tolmetin

Name: Tolmetin
Brand: TargetMol
SKU: T2550
Price: 29 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T2550Cas No. 26171-23-3

Alias Tolectin

Tolmetin (Tolectin) is a Nonsteroidal Anti-inflammatory Drug. The mechanism of action of tolmetin is as a Cyclooxygenase Inhibitor. The chemical classification of tolmetin is Nonsteroidal Anti-inflammatory Compounds.

Tolmetin

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Purity: 99.74%

Catalog No. T2550Alias TolectinCas No. 26171-23-3

Pack Size	Price	USA Warehouse	Global Warehouse
50 mg	$33	In Stock	In Stock
100 mg	$48	In Stock	In Stock
200 mg	$68	In Stock	In Stock
500 mg	$117	-	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]

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

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:99.74%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

Tolmetin AI Summary

Tolmetin exhibits multiple bioactivities and pharmacokinetic properties. It demonstrates bioactivity related to ester hydrolysis in human plasma with a half-life of 19.0 hours for methyl ester hydrolysis and 0.2233 hours for N,N-diethylglycolamide ester hydrolysis under in vitro conditions (80% human plasma, pH 7.4, 37°C). The compound shows notable anti-inflammatory and antiplatelet activities by inhibiting adjuvant arthritis, collagen-induced platelet aggregation, and serotonin release from platelets. In terms of pharmacodynamics, Tolmetin displays significant analgesic activity with ED50 values of 22.0 mg/kg (phenylquinone writhing assay) and 20.0 mg/kg (carrageenan assay), although it also has ulcerogenic properties (UD50 = 63.0 mg/kg). Remarkably, it shows a low neurotoxic risk with an NTD50 value greater than 1000.0 mg/kg. Pharmacokinetic features include a low partition coefficient (LogD = -0.21) and a significant increase in logD between pH 6.5 and 7.4 (delta logD = 0.9), as well as high plasma protein binding (PPB = 99.7%) and moderate lipophilicity (LogP = 2.7). Its intrinsic solubility in water is 21.0 µg/mL, with a pKa value of 3.5, suggesting acidic properties. It exhibits high oral bioavailability in humans (F >= 80.0%) and varied intrinsic clearance values in human liver microsomes and hepatocytes. The compound binds highly to human serum albumin (Ki ~ 416869383470336.4 nM), inhibiting glyoxalase 1 (Ki = 1014000.0 nM and 87800.0 nM) and aldose reductase (IC50 = 2153.0 nM). It also inhibits human HDAC6 enzyme activity and CXCL8-induced chemotaxis in human polymorphonuclear leukocytes (IC50 = 90.0 nM), showcasing potential anti-inflammatory and transporter inhibition properties. However, Tolmetin exhibits moderate hepatotoxicity with an observed rate of 14.6% and dose-dependent ulcerogenic effects. Despite showing some inhibitory actions against SARS-CoV-2-induced cytotoxicity in VERO-6 cells at 10 µM, its antiviral potency is moderate to low (IC50 > 19952.62 nM). Overall, Tolmetin is a bioactive substance with diverse pharmacological effects, significant protein binding, moderate lipophilicity, and potential for adverse effects at higher doses..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Tolmetin (Tolectin) is a Nonsteroidal Anti-inflammatory Drug. The mechanism of action of tolmetin is as a Cyclooxygenase Inhibitor. The chemical classification of tolmetin is Nonsteroidal Anti-inflammatory Compounds.
Targets&IC50	COX-2(human):0.82 μM (IC50), COX-1 (human):0.35 μM (IC50)
Synonyms	Tolectin

Chemical Properties

Molecular Weight	257.28
Formula	C₁₅H₁₅NO₃
Cas No.	26171-23-3
Smiles	CN1C(CC(O)=O)=CC=C1C(=O)C1=CC=C(C)C=C1
Relative Density.	1.1391 g/cm3 (Estimated)

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

DMSO: 50 mg/mL (194.34 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (7.77 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

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.8868 mL	19.4341 mL	38.8682 mL	194.3408 mL
5 mM	0.7774 mL	3.8868 mL	7.7736 mL	38.8682 mL
10 mM	0.3887 mL	1.9434 mL	3.8868 mL	19.4341 mL
20 mM	0.1943 mL	0.9717 mL	1.9434 mL	9.7170 mL
50 mM	0.0777 mL	0.3887 mL	0.7774 mL	3.8868 mL
100 mM	0.0389 mL	0.1943 mL	0.3887 mL	1.9434 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