Nimesulide

Nimesulide Structure
Nimesulide
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Common Name Nimesulide
CAS Number 51803-78-2 Molecular Weight 308.310
Density 1.5±0.1 g/cm3 Boiling Point 442.0±55.0 °C at 760 mmHg
Molecular Formula C13H12N2O5S Melting Point 140-146°C
MSDSNimesulide MSDS|SDS|pdf download Chinese USA Flash Point 221.1±31.5 °C
Symbol GHS06
GHS06
Signal Word Danger

 Use of Nimesulide


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.

 Names

Name nimesulide
Synonym More Synonyms

 Nimesulide Biological Activity

Description 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.
Related Catalog
Target

COX-2:0.07-70 μM (IC50)

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].
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].
Solvent
In Vitro:

10 mM in DMSO

Solubility
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
Cell Assay 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].
Animal Admin 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].
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping Room temperature in continental US; may vary elsewhere
SMILES CS(=O)(NC1=CC=C([N+]([O-])=O)C=C1OC2=CC=CC=C2)=O
References

[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.

[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.

[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.

Related Molecules 4-Acetamidophenol | Aspirin | Paradol | Ginsenoside Rg3 | Ginsenoside C-K | Xanthohumol | Ibuprofen | Diclofenac | NS-398 | Meloxicam | Flufenamic Acid | (-)-Epicatechin | Salicylic acid | ketoprofen | Naproxen
Related Doc

SDS |COA |HNMR |LCMS

*The above documents are provided by Medchemexpress and are for scientific research only.

 Chemical & Physical Properties

Density 1.5±0.1 g/cm3
Boiling Point 442.0±55.0 °C at 760 mmHg
Melting Point 140-146°C
Molecular Formula C13H12N2O5S
Molecular Weight 308.310
Flash Point 221.1±31.5 °C
Exact Mass 308.046692
PSA 109.60000
LogP 3.79
Vapour Pressure 0.0±1.1 mmHg at 25°C
Index of Refraction 1.638
Storage condition 2-8°C
Stability Stable. Incompatible with strong oxidizing agents.

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
PB0970000
CHEMICAL NAME :
Methanesulfonanilide, 4'-nitro-2'-phenoxy-
CAS REGISTRY NUMBER :
51803-78-2
LAST UPDATED :
199612
DATA ITEMS CITED :
4
MOLECULAR FORMULA :
C13-H12-N2-O5-S
MOLECULAR WEIGHT :
308.33
WISWESSER LINE NOTATION :
WS1&MR BOR& DNW

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
200 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
FEPRA7 Federation Proceedings, Federation of American Societies for Experimental Biology. (Bethesda, MD) V.1-46, 1942-87. Volume(issue)/page/year: 34,759,1975
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
163 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
YAKUD5 Gekkan Yakuji. Pharmaceuticals Monthly. (Yakugyo Jihosha, Inaoka Bldg., 2-36 Jinbo-cho, Kanda, Chiyoda-ku, Tokyo 101, Japan) V.1- 1959- Volume(issue)/page/year: 17,1254,1975
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
392 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
YAKUD5 Gekkan Yakuji. Pharmaceuticals Monthly. (Yakugyo Jihosha, Inaoka Bldg., 2-36 Jinbo-cho, Kanda, Chiyoda-ku, Tokyo 101, Japan) V.1- 1959- Volume(issue)/page/year: 17,1254,1975
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
216 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
YAKUD5 Gekkan Yakuji. Pharmaceuticals Monthly. (Yakugyo Jihosha, Inaoka Bldg., 2-36 Jinbo-cho, Kanda, Chiyoda-ku, Tokyo 101, Japan) V.1- 1959- Volume(issue)/page/year: 17,1254,1975

 Safety Information

Symbol GHS06
GHS06
Signal Word Danger
Hazard Statements H301
Precautionary Statements P301 + P310
Personal Protective Equipment dust mask type N95 (US);Eyeshields;Faceshields;Gloves
Hazard Codes Xn: Harmful;Xi: Irritant;
Risk Phrases R22
Safety Phrases S36
RIDADR UN 2811 6.1/PG 3
WGK Germany 3
RTECS PB0970000
Packaging Group III

 Synthetic Route

(2-Phenoxy)Methylsulfonylaniline结构式

CAS#:51765-51-6

(2-Phenoxy)Meth...

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Nimesulide Structure

CAS#:51803-78-2

Nimesulide

Literature: Lunghi, Angelo; Alos, Miquel A.; Gigante, Lucia; Feixas, Joan; Sironi, Eugenio; Feliu, Josep A.; Cardillo, Paolo Organic Process Research and Development, 2002 , vol. 6, # 6 p. 926 - 932

 Articles64

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