Nimesulid

Bezeichnung:Nimesulid

CAS-Nr51803-78-2

Englisch Name:Nimesulide

CBNumberCB0138084

SummenformelC13H12N2O5S

Molgewicht308.31

MOL-Datei51803-78-2.mol

Synonyma

Nimesulid

Nimesulid physikalisch-chemischer Eigenschaften

Schmelzpunkt	140-146°C
Siedepunkt	442.0±55.0 °C(Predicted)
Dichte	1.451±0.06 g/cm3(Predicted)
storage temp.	2-8°C
Löslichkeit	Practically insoluble in water, freely soluble in acetone, slightly soluble in anhydrous ethanol.
pka	pKa 6.56± 0.03(H2O,t =25,I=0.02)(Approximate)
Farbe	Light orange to Yellow to Green
Wasserlöslichkeit	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.
maximale Wellenlänge (λmax)	391nm(H2O)(lit.)
Merck	14,6548
Stabilität	Stable. Incompatible with strong oxidizing agents.
InChIKey	HYWYRSMBCFDLJT-UHFFFAOYSA-N
CAS Datenbank	51803-78-2(CAS DataBase Reference)
EPA chemische Informationen	Methanesulfonamide, N-(4-nitro-2-phenoxyphenyl)- (51803-78-2)

Sicherheit

Kennzeichnung gefährlicher	Xn,Xi
R-Sätze:	22-36/37/38
S-Sätze:	36-26
RIDADR	UN 2811 6.1/PG 3
WGK Germany	3
RTECS-Nr.	PB0970000
HS Code	2935.90.9500
HazardClass	6.1
PackingGroup	III
Toxizität	LD50 orally in rats: 324 mg/kg (Swingle, Moore)

Gefahreninformationscode (GHS)

Nimesulide Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R22:Gesundheitsschädlich beim Verschlucken.
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
S-Sätze Betriebsanweisung:
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
Beschreibung
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.
Beschreibung
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.
Chemische Eigenschaften
Yellow Needle-Like Crystals
Originator
Riker (USA)
Verwenden
For the treatment of acute pain, the symptomatic treatment of osteoarthritis and primary dysmenorrhoea in adolescents and adults above 12 years old.
Verwenden
Antiinflammatory;'Cyclooxygenase 2 inhibitor
Verwenden
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]
Verwenden
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
Verwenden
Antiinflammatory agent. Preferentially inhibits COX-2 over COX-1. Suppresses chemical-induced carcinogenesis in mice and rats. Inhibits LPS-induced TNF-alpha production
Verwenden
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.
Definition
ChEBI: Nimesulide is an aromatic ether having phenyl and 2-methylsulfonamido-5-nitrophenyl as the two aryl groups. It has a role as a cyclooxygenase 2 inhibitor and a non-steroidal anti-inflammatory drug. It is a C-nitro compound, a sulfonamide and an aromatic ether. It is functionally related to a nitrobenzene.
Trademarks
Nimulid.
Allgemeine Beschreibung
Nimesulide, a nonsteroidal anti-inflammatory drug (NSAID) belongs to the sulfonanilide class.
Biologische Aktivität
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.
Einzelnachweise
https://en.wikipedia.org/wiki/Nimesulide
https://www.drugbank.ca/drugs/DB04743

Nimesulide Upstream-Materialien And Downstream Produkte

Nimesulid Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

51803-78-2, Nimesulide Verwandte Suche:

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