Art. -Nr.: HY-B0363

Nimesulide

(Synonyms: R805)

10 Cited Publications

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Based on 10 publication(s) in Google Scholar

Nimesulide is a selective COX-2 inhibitor, with IC₅₀s of 70 nM-70 μM in a time-dependent manner, but it shows no effect on COX-1 (IC₅₀ >100 μM). Nimesulide has potent anti-inflammatory, analgesic and antipyretic properties.

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Reinheit: 99.89%
CAS. Nr.: 51803-78-2
Formel: C₁₃H₁₂N₂O₅S
Molecular Weight:308.31

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Nimesulide Chemical Structure

CAS. Nr.: 51803-78-2

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (10)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

COX-2

0.07-70 μM (IC₅₀)

Alle COX Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	67.81 μM Compound: A	Growth inhibition of human A549 cells after 48 hrs by MTT assay Growth inhibition of human A549 cells after 48 hrs by MTT assay	[PMID: 28011214]
HepG2	IC₅₀	35.21 μM Compound: A	Growth inhibition of human HepG2 cells after 48 hrs by MTT assay Growth inhibition of human HepG2 cells after 48 hrs by MTT assay	[PMID: 28011214]
LNCaP	IC₅₀	26.69 μM Compound: Nimesulide	Antiproliferative activity against human LNCAP cells after 48 hrs by MTT assay Antiproliferative activity against human LNCAP cells after 48 hrs by MTT assay	[PMID: 28666860]
MCF7	IC₅₀	>100 μM Compound: Nimesulide	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 28666860]
RAW264.7	IC₅₀	<0.078 μM Compound: Nimesulide	Inhibition of LPS/IFN-gamma-induced PGE2 production in mouse RAW264.7 cells after 17 to 20 hrs by enzyme immunoassay Inhibition of LPS/IFN-gamma-induced PGE2 production in mouse RAW264.7 cells after 17 to 20 hrs by enzyme immunoassay	[PMID: 27040659]
Sf21	IC₅₀	231.4 μM Compound: Nimesulide	Inhibition of human recombinant COX2 expressed in baculovirus infected SF21 cell Inhibition of human recombinant COX2 expressed in baculovirus infected SF21 cell	[PMID: 20974503]
SK-BR-3	IC₅₀	100 μM Compound: Nimesulide	Antiproliferative activity against human SKBR3 cells after 48 hrs by MTT assay Antiproliferative activity against human SKBR3 cells after 48 hrs by MTT assay	[PMID: 23767669]
SK-BR-3	IC₅₀	27 μM Compound: nimesulide	Inhibition of aromatase in SK-BR-3 cells by tritiated water release assay Inhibition of aromatase in SK-BR-3 cells by tritiated water release assay	[PMID: 17315855]
U-937	IC₅₀	<0.078 μM Compound: Nimesulide	Inhibition of LPS/IFN-gamma-induced PGE2 production in PMA-treated human U937 cells after 17 to 20 hrs by enzyme immunoassay Inhibition of LPS/IFN-gamma-induced PGE2 production in PMA-treated human U937 cells after 17 to 20 hrs by enzyme immunoassay	[PMID: 27040659]

In Vitro

Nimesulide is a selective COX-2 inhibitor, with IC₅₀s of 70 nM-70 μM in a time-dependent manner, but it shows weak effect on COX-1 (IC₅₀ >100 μM)^[1]. Nimesulide (10 μM) effectively decreases VEGF in endometrium cancer cells, and shows no effect on that in normal cells. Nimesulide (10 and 50 μM) dramatically decreases MCP-1 levels in normal cell, and such an effect is also observed with 10 μM in cancer cells. In addition, Nimesulide (50 μM) potently affects IL-8 level in normal cells, but causes no changes in cancer cells^[3].

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

In Vivo

Nimesulide (3 and 10 mg/kg, i.p.) effectively blocks fever induced by i.p. injection of LPS in rats. Nimesulide (3 mg/kg, i.p.) potently reduces fever response induced by IL-1β, IL-6 or TNF-α, but does not prevent the initial rise in the febrile response induced by arachidonic acid. Nimesulide also significantly reduces PGE2 levels and PGF2α levels in the cerebrospinal fluid of the LPS-stimulated animals, and inhibits the increase in plasma TNF-α by 97%^[2].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 51803-78-2
Appearance Solid
Molecular Weight 308.31
Formel C₁₃H₁₂N₂O₅S
Color Light yellow to yellow
SMILES

CS(=O)(NC1=CC=C([N+]([O-])=O)C=C1OC2=CC=CC=C2)=O
Synonyms

R805
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (10)

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Journal Impact Factor

J Hazard Mater

Microwave-assisted activated carbon from cocoa shell as adsorbent for removal of sodium diclofenac and nimesulide from aqueous effluents. [Abstract]

2015 May 30;289:18-27. PMID: 25702636
J Hazard Mater Lett

2025 Nov.
J Ethnopharmacol

Involvement of p38 MAPK/cPLA2 and arachidonic acid metabolic pathway in Shengmai injection-induced pseudo-allergic reactions. [Abstract]

2023 Jun 12:309:116357. PMID: 36906156
Chem Biol Interact

Regulatory effects of non-steroidal anti-inflammatory drugs on cardiac ion channels Nav1.5 and Kv11.1. [Abstract]

2021 Apr 1:338:109425. PMID: 33617802
J Phys Chem Solids

2017 October;109:117-123.
Heliyon

Screening chondrocyte necroptosis-related genes in the diagnosis and treatment of osteoarthritis. [Abstract]

2024 Jul 31;10(15):e35263. PMID: 39170298
Biotechnol Bioeng

An integrated biomimetic array chip for establishment of collagen-based 3D primary human hepatocyte model for prediction of clinical drug-induced liver injury. [Abstract]

2021 Dec;118(12):4687-4698. PMID: 34478150
Phys Chem Chem Phys

Adsorption of anti-inflammatory nimesulide by graphene materials: a combined theoretical and experimental study. [Abstract]

2017 Aug 23;19(33):22099-22110. PMID: 28795704
Infect Immun

Annexin A1 Attenuates Neutrophil Migration and IL-6 Expression through Fpr2 in a Mouse Model of Streptococcus suis-Induced Meningitis. [Abstract]

2021 Feb 16;89(3):e00680-20. PMID: 33318141
Federal University of Rio Grande do Sul

2017 Nov.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (324.35 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.2435 mL

16.2174 mL

32.4349 mL

5 mM

0.6487 mL

3.2435 mL

6.4870 mL

10 mM

0.3243 mL

1.6217 mL

3.2435 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 (8.11 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (8.11 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Cell Assay^[3]

5×10⁵ viable cells are carefully dislodged with sterile Pasteur pipettes, transferred into new flasks and incubated with two different doses of Nimesulide (10 and 50 µM) for another 24 h. Incubations for different doses of Nimesulide are repeated three times. The culture supernatant is then collected and stored in small aliquots at -70°C until studied. VEGF, MCP-1 and IL-8 concentrations are determined by sandwich quantitative enzyme immunoassay (ELISA) using commercial kits^[3].

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

Animal Administration^[2]

Rats^[2]
In the initial experiments, rats are pre-treated with intraperitoneal injections of 1, 3 or 10 mg/kg doses of Nimesulide, diluted in a 5% cremophor vehicle, or 2 mg/kg of indomethacin diluted in tris(hydroximetyl)-aminomethane-HCl (TRIS), pH 8.2, 30 min prior to an i.p. injection of LPS (50 μg/kg). Control animals receive the appropriate vehicle plus saline (1 mL/200 g, i.p.). The dose of 3 mg/kg of Nimesulide is chosen for the remaining experiments. In another set of experiments, rats are pretreated with an i.p. injection of Nimesulide (3 mg/kg) or indomethacin (2 mg/kg), diluted in the appropriate vehicles, 30 min prior to an i.c.v. injection (2 μL over 1 min) of IL-1β (3.12 ng), IL-6 (300 ng), TNF-α (250 ng), arachidonic acid (50 μg), MIP-1α (500 ng), PGE2 (250 ng), PGF2α (250 ng), CRF (2 μg) or ET-1 (1 pmol). Control animals receive the appropriate vehicles (1 mL/200 g, i.p.) and sterile saline (2 μL over 1 min, i.c.v.). All the drugs are injected between 10:00 and 11:00 AM to avoid circadian rhythm variations^[2].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Vago T, et al. Effect of nimesulide action time dependence on selectivity towards prostaglandin G/H synthase/cyclooxygenase activity. Arzneimittelforschung. 1995 Oct;45(10):1096-8. [Content Brief]

[2]. Werner MF, et al. Nimesulide-induced antipyresis in rats involves both cyclooxygenase-dependent and independent mechanisms. Eur J Pharmacol. 2006 Aug 14;543(1-3):181-9. [Content Brief]

[3]. Genç S, et al. The effect of COX-2 inhibitor, nimesulide, on angiogenetic factors in primary endometrial carcinoma cell culture. Clin Exp Med. 2007 Mar;7(1):6-10. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.2435 mL	16.2174 mL	32.4349 mL	81.0872 mL
	5 mM	0.6487 mL	3.2435 mL	6.4870 mL	16.2174 mL
	10 mM	0.3243 mL	1.6217 mL	3.2435 mL	8.1087 mL
	15 mM	0.2162 mL	1.0812 mL	2.1623 mL	5.4058 mL
	20 mM	0.1622 mL	0.8109 mL	1.6217 mL	4.0544 mL
	25 mM	0.1297 mL	0.6487 mL	1.2974 mL	3.2435 mL
	30 mM	0.1081 mL	0.5406 mL	1.0812 mL	2.7029 mL
	40 mM	0.0811 mL	0.4054 mL	0.8109 mL	2.0272 mL
	50 mM	0.0649 mL	0.3243 mL	0.6487 mL	1.6217 mL
	60 mM	0.0541 mL	0.2703 mL	0.5406 mL	1.3515 mL
	80 mM	0.0405 mL	0.2027 mL	0.4054 mL	1.0136 mL
	100 mM	0.0324 mL	0.1622 mL	0.3243 mL	0.8109 mL

Keywords

Nimesulide

10 Cited Publications

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Nimesulide

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Publications Citing Use of MedChemExpress (MCE) Nimesulide

Alle COX Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (10)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Nimesulide Related Classifications

HY-B0363 Related Classifications