| 货号 | 16407-100mg |
| 描述 | Ketoprofen (Item No. 10006661) is a non-selective, non-steroidal, anti-inflammatory drug exhibiting IC50 values of 0.5 and 2.33 µM for human recombinant COX-1 and COX-2 (Item No. 60122), respectively.1 Ketoprofen is commonly used in vivo as a racemic mixture of (R)- and (S)-enantiomers. (S)-Ketoprofen is a potent inhibitor of COX-1 and COX-2 (IC50s = 1.9 and 27 nM, respectively), whereas the (R)-enantiomer is 100 to 1,000 times less potent.2,3 Notably, (S)-ketoprofen is known to be formed from the (R)-enantiomer in several animal species, except in humans and guinea pigs.3 Also, the pharmacokinetics of ketoprofen enantiomers and their glucuronide metabolites are altered in humans with rheumatoid arthritis or renal disease.4,5 |
| 别名 | (S)-2-(3-benzoylphenyl)Propionic Acid;Dexketoprofen; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Barnett, J.,Chow, J.,Ives, D., et al. Purification, characterization and selective inhibition of human prostaglandin G/H synthase 1 and 2 expressed in the baculovirus system. Biochimica et Biophysica Acta 1209, 130-139 (1994). 2.Palomer, A.,Pérez, J.J.,Navea, S., et al. Modeling cyclooxygenase inhibition. Implication of active site hydration on the selectivity of ketoprofen analogues. Journal of Medicinal Chemistry 43(11), 2280-2284 (2000). 3.Ghezzi, P.,Melillo, G.,Meazza, C., et al. Differential contribution of R and S isomers in ketoprofen anti-inflammatory activity: Role of cytokine modulation. Journal of Pharmacology and Experimental Therapeutics 287, 969-974 (1998). 4.Glówka, F.,Karazniewicz-Lada, M.,Grzeskowiak, E., et al. Clinical pharmacokinetics of ketoprofen enantiomers in wild type of Cyp 2c8 and Cyp 2c9 patients with rheumatoid arthritis. European Journal of Drug Metabolism and Pharmacokinetics 36(3), 167-173 (2011). 5.Grubb, N.G.,Rudy, D.W.,Brater, D.C., et al. Stereoselective pharmacokinetics of ketoprofen and ketoprofen glucuronide in end-stage renal disease: Evidence for a futile cycle of elimination. British Journal of Clinical Pharmacology 48(4), 494-500 (1999). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 254.3 |
| 分子式 | C16H14O3 |
| CAS号 | 22161-81-5 |
| 稳定性 | ≥ 2 years |
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