产品说明书

Suprofen

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Chemical Structure| 40828-46-4 同义名 : TN-762;NSC 303611;Profenal;Suprofenum;(±)-Suprofen;R 25061
CAS号 : 40828-46-4
货号 : A867270
分子式 : C14H12O3S
纯度 : 99%+
分子量 : 260.308
MDL号 : MFCD00079572
存储条件:

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(403.37 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
靶点
  • COX-1

描述 Suprofen (sutoprofen) is a non-steroidal anti-inflammatory analgesic. Suprofen appears to be a useful alternative to mild analgesics, analgesic combinations or the older more established non-steroidal anti-inflammatory drugs in the treatment of patients with acute or chronic pain[3]. Suprofen is a potent, peripherally-acting, non-narcotic analgesic agent. The mechanism of action of the compound involves inhibition of prostaglandin biosynthesis and, perhaps, direct antagonism of the peripheral, pain inducing actions of prostaglandins, bradykinin and other pain mediators. Suprofen at a dose of 200 mg appears to be equal or greater in efficacy as an analgesic modality than those of ibuprofen, propoxyphene, naproxen and diflunisal or a combination of 650 mg aspirin plus 60 mg codeine[4]. Suprofen is 50 times more potent than acetaminophen, five times more potent than codeine and equipotent to the new peripheral analgesics, zomepirac and diflunisal. In other hyperalgesic assays, suprofen is an extremely potent inhibitor of arachidonate-induced writhing and is equipotent to morphine in the yeast-induced paw edema (Randall-Selitto) assay. Activity on prostaglandin biosynthesis from several species and tissues suggests that suprofen is a tissue selective inhibitor of prostaglandin synthesis[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.84mL

0.77mL

0.38mL

19.21mL

3.84mL

1.92mL

38.42mL

7.68mL

3.84mL

参考文献

[1]O'Donnell JP, Dalvie DK, et al. Mechanism-based inactivation of human recombinant P450 2C9 by the nonsteroidal anti-inflammatory drug suprofen. Drug Metab Dispos. 2003 Nov;31(11):1369-77.

[2]Yang MC, Lung FW. Neuroprotection of paliperidone on SH-SY5Y cells against β-amyloid peptide(25-35), N-methyl-4-phenylpyridinium ion, and hydrogen peroxide-induced cell death. Psychopharmacology (Berl). 2011 Oct;217(3):397-410.

[3]Todd PA, Heel RC. Suprofen. A review of its pharmacodynamic and pharmacokinetic properties, and analgesic efficacy. Drugs. 1985 Dec;30(6):514-38

[4]Tolman EL, Rosenthale ME, Capetola RJ, McGuire JL. Suprofen: the pharmacology and clinical efficacy of a new non-narcotic peripheral analgesic. Clin Rheum Dis. 1984 Aug;10(2):353-68

[5]Capetola RJ, Shriver DA, Rosenthale ME. Suprofen, a new peripheral analgesic. J Pharmacol Exp Ther. 1980 Jul;214(1):16-23