Sudoxicam 是一种可逆的口服活性的 COX 拮抗剂，是烯醇-羧酰胺类的非甾体抗炎剂 (NSAID)。Sudoxicam 具有有效的抗炎，抗浮肿和退热作用。 Sudoxicam and Meloxicam are nonsteroidal, anti-inflammatory drugs (NSAIDs) from the enol-carboxamide class. Biological activity： Sudoxicam is a reversible and orally active COX antagonist and a non-steroidal anti-inflammatory drug (NSAID) from the enol-carboxamide class. Sudoxicam has potent anti-inflammatory, anti-edema and antipyretic activity In vitro research： Sudoxicam demonstrates NADPH-dependent covalent binding to human liver microsomes. With addition of glutathione (GSH) in microsomal incubations, about half of the covalent incorporation of Sudoxicam is blocked by addition of GSH. Metabolite identification studies on [14C]-Sudoxicam in NADPH-supplemented human liver microsomes indicated that the primary route of metabolism involved a P450-mediated thiazole ring scission to the corresponding acylthiourea metabolite (S3), a well-established pro-toxin In vitro, Sudoxicam underwent the oxidative thiazole-open biotransformation, resulting in the formation of an acylthiourea and the subsequent hydroxylated metabolite In vivo research： Sudoxicam (1-10 mg/kg; oral administration; daily; for 7 days; rats) treatment effective reduces plasma inflammation units, reduces the swelling of inflamed hind-paws and restores toward normal the daily gain in body weight In the intact rat, Sudoxicam significantly inhibited edema formation at doses as low as 0.1 mg/kg, p.o Sudoxicam inhibits the erythema caused by ultraviolet irradiation in the guinea pig. Sudoxicam (3.3 mg/kg, i.p.) is capable of counteracting the pyrexia induced by the intraperitoneal injection of typhoid/paratyphoid vaccine in rats, maintaining body temperature about that of uninjected control rats The plasma half-life of Sudoxicam ranged between 8 hours (monkey), 13 hours (rat), and 60 hours (dog) Animal Model: Rats injected with ,i>M. butyrieum Dosage:1 mg/kg, 3.3 mg/kg, 10 mg/kg Administration:Oral administration; daily; for 7 days Result:Were both effective in reducing plasma inflammation units, in reducing the swelling of inflamed hind-paws.
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Sudoxicam
CAS number：34042-85-8 molecular formula：C13H11N3O4S2
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| Chinese alias | - | ||
| English alias | SUDOXICAM | Sudoxicam (USAN/INN) | HY-106628 | CP-15,973 | Sudoxicamum [INN-Latin] | MS-25117 | DTXSID50187653 | SUDOXICAM [USAN] | BRN 0628704 | N-(2-Thiazolyl)-4-hydroxy-2-methyl-2H-1,2-benzothiazine-3-carboxamide 1,1-Dioxide | NSC615046 | NSC-615046 | | ||
| CAS number | 34042-85-8 | molecular formula | C13H11N3O4S2 |
| molecular weight | 337.37 g/mol | Exact mass | - |
| PSA | 136.000 Ų | logp | 1.600 |
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