Sudoxicam

(Synonyms: 舒多昔康)
目录号: PL01575 纯度: ≥99%
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药 (NSAID)。Sudoxicam 具有有效的抗炎,抗浮肿和退热作用。
CAS No. :34042-85-8
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中文名称
Sudoxicam
中文别名
舒多昔康;4-(5-甲基-3-苯基-4-异恶唑)苯磺酰氯;戊地昔布杂质F
英文名称
Sudoxicam
英文别名
Sudoxicam;4-hydroxy-2-methyl-1,1-dioxo-N-(1,3-thiazol-2-yl)-1λ6,2-benzothiazine-3-carboxamide;2H-1,2-Benzothiazine-3-carboxamide,4-hydroxy-2-methyl-N-2-thiazolyl-,1,1-dioxide;4-hydroxy-2-methyl-N-(2-thiazole)-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide;4-hydroxy-2-methyl-N-(2-thiazolyl)-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide;EINECS 251-808-7;N-(2-thiazolyl)-4-hydroxy-2-methyl-2H,1,2-benzothiazine-3-carboxamide 1,1-dioxide;Sudoxicamum;Sudoxicamum [INN-Latin]
Cas No.
34042-85-8
分子式
C13H11N3O4S2
分子量
337.37
包装储存
Powder -20°C 3 years;4°C 2 years
详情描述
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药 (NSAID)。Sudoxicam 具有有效的抗炎,抗浮肿和退热作用。
产品详情
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药 (NSAID)。Sudoxicam 具有有效的抗炎,抗浮肿和退热作用。
生物活性
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.
性状
Solid
IC50 & Target[1][2]
COX
体外研究(In Vitro)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
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). has not independently confirmed the accuracy of these methods.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Obach RS, et al. In vitro metabolism and covalent binding of enol-carboxamide derivatives and anti-inflammatory agents sudoxicam and meloxicam: insights into the hepatotoxicity of sudoxicam. Chem Res Toxicol. 2008 Sep;21(9):1890-9.
[2]. Wiseman EH, et al. Anti-inflammatory and pharmacokinetic properties of sudoxicam N-(2-thiazolyl)-4-hydroxy-2-methyl-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide. Biochem Pharmacol. 1972 Sep 1;21(17):2323-34.
溶解度数据
In Vitro: DMSO : 83.33 mg/mL (247.00 mM; ultrasonic and warming and heat to 80°C)配制储备液
搜索质检报告(COA)
[1]. Obach RS, et al. In vitro metabolism and covalent binding of enol-carboxamide derivatives and anti-inflammatory agents sudoxicam and meloxicam: insights into the hepatotoxicity of sudoxicam. Chem Res Toxicol. 2008 Sep;21(9):1890-9.
[2]. Wiseman EH, et al. Anti-inflammatory and pharmacokinetic properties of sudoxicam N-(2-thiazolyl)-4-hydroxy-2-methyl-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide. Biochem Pharmacol. 1972 Sep 1;21(17):2323-34.

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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