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(S)-Ibuprofen is a non-steroidal anti-inflammatory drug (NSAID) and a COX-1 and COX-2 inhibitor (IC50s = 2.6 and 1.53 µM, respectively).1 It inhibits NF-κB transactivation in a reporter assay using Jurkat T cells (IC50 = 61.7 µM).2 (S)-Ibuprofen reduces aggregation in platelet-rich plasma and washed isolated human platelets (IC50s = 88 and 0.6 µM, respectively).3 It decreases superoxide formation and β-glucuronidase release induced by N-formyl-Met-Leu-Phe (fMLP; Item No. 21495), as well as leukotriene B4 (LTB4; Item No. 20110) formation induced by calcimycin (A23187; Item No. 11016), in human polymorphonuclear (PMN) cells (IC50s = 0.50, 0.53, and 0.14 µM, respectively). (S)-Ibuprofen increases the latency to withdrawal in hot plate and tail-flick tests in mice (ED50s = 64 and 54 mg/kg, respectively), as well as reduces paw swelling in a mouse model of carrageenan-induced paw edema (ED50 = 57 mg/kg).4 Formulations containing (±)-ibuprofen have been used in the treatment of fever and mild-to-severe pain.
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1. Purification, characterization and selective inhibition of human prostaglandin G/H synthase 1 and 2 expressed in the baculovirus system. Biochim. Biophys. Acta 1209(1), 130-139 (1994).
2. Modulation of transcription factor NF-
3. Equipotent inhibition by R(−)-
4. Dexibuprofen (S+-