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Nimesulide

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Catalog No. T1133Cas No. 51803-78-2
Alias R805

Nimesulide (R805) is a relatively COX-2 selective inhibitor with analgesic and antipyretic properties.

Nimesulide

Nimesulide

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Purity: 99.91%
Catalog No. T1133Alias R805Cas No. 51803-78-2
Nimesulide (R805) is a relatively COX-2 selective inhibitor with analgesic and antipyretic properties.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
25 mg$30In StockIn Stock
50 mg$38In StockIn Stock
100 mg$50In StockIn Stock
200 mg$60In StockIn Stock
1 mL x 10 mM (in DMSO)$48In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.91%
Color:White
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Product Introduction

Nimesulide AI Summary
Nimesulide demonstrates notable bioactivity across multiple biological systems and assays. Primarily, it exhibits significant inhibitory effects on cyclooxygenase enzymes (COX-1 and COX-2). For COX-2, it shows potent inhibition with IC50 values ranging from 15.0 nM to 700.0 nM in various assays, including LPS-stimulated human whole blood and U937 cells. Its selectivity for COX-2 over COX-1 is indicated by several selectivity ratios, suggesting higher affinity and potency for COX-2 inhibition. Beyond COX inhibition, Nimesulide also displays significant anti-inflammatory properties, effectively reducing carrageenan-induced paw edema and ear edema in animal models. It achieves different levels of inflammation inhibition, with notable percentages at various dosages, highlighting its potent anti-inflammatory potential. Additionally, Nimesulide demonstrates analgesic effects, reducing pain in mouse and rat models subjected to formalin-induced pain and carrageenan-induced paw edema. Its hepatotoxicity has been noted across different liver toxicity categories, emphasizing cautious therapeutic application. In vitro studies show that Nimesulide possesses moderate to high binding affinity towards human serum albumin and demonstrates selective inhibition of sodium fluorescein uptake in OATP-transfected CHO cells. It also impacts cell proliferation, showing significant antiproliferative activity against certain human cancer cell lines. Overall, Nimesulide displays a broad spectrum of biological activities, including anti-inflammatory, analgesic, enzyme inhibition, anti-proliferative, and potential hepatotoxic effects, making it a compound of interest for further research in anti-inflammatory and analgesic drug development..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
Nimesulide (R805) is a relatively COX-2 selective inhibitor with analgesic and antipyretic properties.
Targets&IC50
COX-2:26 μM
SynonymsR805
Chemical Properties
Molecular Weight308.31
FormulaC13H12N2O5S
Cas No.51803-78-2
SmilesO(C1=C(NS(C)(=O)=O)C=CC(N(=O)=O)=C1)C2=CC=CC=C2
Relative Density.1.451 g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 250 mg/mL (810.87 mM), Sonication is recommended.
Ethanol: 7.7 mg/mL (24.97 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.49 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/DMSO
1mg5mg10mg50mg
1 mM3.2435 mL16.2174 mL32.4349 mL162.1744 mL
5 mM0.6487 mL3.2435 mL6.4870 mL32.4349 mL
10 mM0.3243 mL1.6217 mL3.2435 mL16.2174 mL
20 mM0.1622 mL0.8109 mL1.6217 mL8.1087 mL
DMSO
1mg5mg10mg50mg
50 mM0.0649 mL0.3243 mL0.6487 mL3.2435 mL
100 mM0.0324 mL0.1622 mL0.3243 mL1.6217 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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
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g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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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

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