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| Nimesulide Basic information |
| Nimesulide Chemical Properties |
| Melting point | 140-146°C | | Boiling point | 442.0±55.0 °C(Predicted) | | density | 1.451±0.06 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | Practically insoluble in water, freely soluble in acetone, slightly soluble in anhydrous ethanol. | | form | neat | | pka | pKa 6.56± 0.03(H2O,t =25,I=0.02)(Approximate) | | color | Light orange to Yellow to Green | | Water Solubility | Soluble in water (<50 µg/ml), 1:10 DMSO:PBS (pH 7.2) (<200 µg/ml), ethanol (1 mg/ml), DMSO (15 mg/ml), DMF (15 mg/ml), chloroform, dichloromethane, acetone (freely soluble), and 1N NaOH. | | λmax | 391nm(H2O)(lit.) | | Merck | 14,6548 | | Stability: | Stable. Incompatible with strong oxidizing agents. | | InChIKey | HYWYRSMBCFDLJT-UHFFFAOYSA-N | | CAS DataBase Reference | 51803-78-2(CAS DataBase Reference) | | EPA Substance Registry System | Methanesulfonamide, N-(4-nitro-2-phenoxyphenyl)- (51803-78-2) |
| Hazard Codes | Xn,Xi | | Risk Statements | 22-36/37/38 | | Safety Statements | 36-26 | | RIDADR | UN 2811 6.1/PG 3 | | WGK Germany | 3 | | RTECS | PB0970000 | | HazardClass | 6.1 | | PackingGroup | III | | Toxicity | LD50 orally in rats: 324 mg/kg (Swingle, Moore) |
| Nimesulide Usage And Synthesis |
| Description | Nimesulide is a relatively COX-2 selective, non-steroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties. It is indicated for the treatment of acute pain, symptomatic treatment of osteoarthritis and primary dysmenorrhoea in adolescents and adults. However, due to the risk of causing hepatotoxicity, it should not be taken long-term. It has also been withdrawn from the markets in many countries. It mechanism of action is through targeting on various key mediators in the inflammatory process such as COX-2 mediated prostaglandins, free radicals, proteolytic enzymes and histamine.
| | Description | Nimesulide is a non-steroidal anti-inflammatory drug (NSAID) and COX-2 inhibitor (IC50s = 1.27 and 0.03 μM for the human and ovine enzymes, respectively). It is selective for COX-2 over COX-1 (IC50s = 70 and 22 μM for the human and ovine enzymes, respectively). Nimesulide also inhibits sodium-dependent neutral amino acid transporter (B0AT1) with an IC50 value of 23 μM for the rat kidney transporter. It inhibits infection-induced increases in brain prostaglandin E2 (PGE2; ) levels, as well as reduces pyresis (ED50 = 0.3 mg/kg), in yeast-infected rats. Nimesulide (2.9 mg/kg) inhibits formalin-induced hindpaw thermal hyperalgesia in rats. | | Chemical Properties | Yellow Needle-Like Crystals | | Originator | Riker (USA) | | Uses | Antiinflammatory agent. Preferentially inhibits COX-2 over COX-1. Suppresses chemical-induced carcinogenesis in mice and rats. Inhibits LPS-induced TNF-alpha production | | Uses | Labelled Nimesulide (N477500). Antiinflammatory agent. Preferentially inhibits COX-2 over COX-1. Suppresses chemical-induced carcinogenesis in mice and rats. Inhibits LPS-induced TNF-α production. | | Uses | Antiinflammatory;'Cyclooxygenase 2 inhibitor | | Uses | For the treatment of acute pain, the symptomatic treatment of osteoarthritis and primary dysmenorrhoea in adolescents and adults above 12 years old. | | Uses | Labelled Nimesulide . Antiinflammatory agent. Preferentially inhibits COX-2 over COX-1. Suppresses chemical-induced carcinogenesis in mice and rats. Inhibits LPS-induced TNF-α production.;Labeled Nimesulide, intended for use as an internal standard for th | | Uses | Nimesulide is a selective inhibitor of COX-2. The IC50 values are 70 and 1.27 μM for human recombinant COX-1 and -2 (at 20 μM arachidonic acid), respectively, and 22 and 0.03 μM for ovine COX-1 and -2 (at 100 μM arachidonic acid), respectively.[Cayman Chemical] | | Brand name | Nimulid. | | General Description | Nimesulide, a nonsteroidal anti-inflammatory drug (NSAID) belongs to the sulfonanilide class. | | Biological Activity | Selective, orally active cyclooxygenase-2 (COX-2) inhibitor. Produces potent analgesic, anti-inflammatory and antipyretic activities in vivo . Reported to produce fewer gastrointestinal side effects than standard NSAIDs. | | Biochem/physiol Actions | Highly selective cyclooxygenase-2 inhibitor. | | Clinical Use | Nimesulide is a nonsteroidal antiinflammatory/analgesic agent useful in the
treatment of rheumatoid arthritis, as well as acute inflammation such as that
induced by periodontal surgery or urinary tract infections. | | References | https://en.wikipedia.org/wiki/Nimesulide
https://www.drugbank.ca/drugs/DB04743
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| Nimesulide Preparation Products And Raw materials |
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