Sudoxicam

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Sudoxicam 是一种可逆的 COX 拮抗剂，具有抗炎、抗水肿和解热作用。

Sudoxicam is a reversible antagonist of COX with anti-inflammatory, anti-edema, and antipyretic properties.(In Vitro):Sudoxicam binds covalently to NADPH-dependent human liver microsomes. When glutathione (GSH) was added to the microsomal incubation, about half of the covalent binding of sudoxicam was blocked by glutathione.(In Vivo):Sudoxicam (0.1 mg/kg, p.o) significantly inhibits edema formation. In rats, Sudoxicam (1, 3.3 and 10 mg/kg; orally) effectively reduces plasma inflammation units, decreases the inflamed hind-paws swelling and restores toward normal the daily gain in body weight. Sudoxicam (3.3 mg/kg, i.p.) counteracts the pyrexia induced by the intraperitoneal injection of typhoid/paratyphoid vaccine and maintains body temperature. In the guinea pig, Sudoxicam inhibits the erythema caused by ultraviolet irradiation. The plasma half-life of Sudoxicam is 8, 13 and hours for monkey, rat and dog.

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.

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.

4-Hydroxy-2-methyl-N-2-thiazolyl-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide

Chromatin/Epigenetic

COX

LXRα| LXRβ

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34042-85-8

337.37

C13H11N3O4S2

>98% (HPLC)

In Vitro:?DMSO : 83.33 mg/mL (247.00 mM)

CN1C(C(=O)Nc2nccs2)=C(O)c2ccccc2S1(=O)=O

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(-20℃)

With Ice Pack

≥ 2 years