| CAS NO: | 51803-78-2 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| 2g | 电议 |
| 5g | 电议 |
| 10g | 电议 |
| 25g | 电议 |
| Molecular Weight (MW) | 308.31 |
|---|---|
| Formula | C13H12N2O5S |
| CAS No. | 51803-78-2 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 62 mg/mL (201.1 mM) |
| Water: <1 mg/mL | |
| Ethanol: <1 mg/mL | |
| Other info | Chemical Name: N-(4-Nitro-2-phenoxyphenyl)methanesulfonamide InChi Key: HYWYRSMBCFDLJT-UHFFFAOYSA-N InChi Code: InChI=1S/C13H12N2O5S/c1-21(18,19)14-12-8-7-10(15(16)17)9-13(12)20-11-5-3-2-4-6-11/h2-9,14H,1H3 SMILES Code: CS(=O)(NC1=CC=C([N+]([O-])=O)C=C1OC2=CC=CC=C2)=O |
| Synonyms | R-805; R 805; R805 |
| In Vitro | In vitro activity: Nimesulide is a selective COX-2 inhibitor used in a variety of inflammatory, pain and fever states. After healthy volunteers received oral nimesulide 100 mg in tablet, granule or suspension form the drug was rapidly and extensively absorbed. Mean peak concentrations (Cmax) of 2.86 to 6.50 mg/L were achieved within 1.22 to 2.75 hours of administration. Nimesulide is an NSAID which exerts its analgesic, anti-inflammatory and antipyretic activities thanks to unique chemical and pharmacokinetic characteristics, and to a multifactorial mechanism of action, which goes beyond its preferential inhibitory activity on the COX-2 enzyme. Nimesulide was found to be at least as effective, or superior, to placebo and other NSAIDs, with a particularly fast onset of analgesic action. nimesulide remains an effective and safe therapeutic choice for the treatment of various painful inflammatory conditions, with a rapid onset of analgesic activity and an overall positive benefit/risk profile. 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 |
|---|---|
| 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% |
| Animal model | Rats: 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 |
| Formulation & Dosage | 1, 3 or 10 mg/kg; i.p. |
| References | Curr Med Res Opin. 2006 Jun;22(6):1161-70; Clin Pharmacokinet. 1998 Oct;35(4):247-74. |
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