| Bioactivity | Loxoprofen is a non-steroidal, orally active anti-inflammatory agent with analgesic and anti-pyretic properties. Loxoprofen is a nonselective COX inhibitor with IC50s of 6.5 and 13.5 μM for COX-1 and COX-2, respectively. Loxoprofen can reduce atherosclerosis and shows antitumor activity[1][2][3][4]. | ||||||||||||
| Invitro | Loxoprofen, an anti-inflammatory prodrug (NSAID), is a nonselective COX inhibitor with IC50s of 6.5 and 13.5 μM for COX-1 and COX-2 in human whole blood assays, respectively[1].Loxoprofen (LOX) is a non-selective cyclooxygenase inhibitor that is widely used for the reasearch of pain and inflammation caused by chronic and transitory conditions. Its alcoholic metabolites are formed by carbonyl reductase (CR) and they consist of trans-LOX, which is active, and cis-LOX, which is inactive. In addition, LOX can also be converted into an inactive hydroxylated metabolite (OH-LOXs) by cytochrome P450 (CYP)[2]. | ||||||||||||
| In Vivo | Loxoprofen sodium (4 mg/kg/day; p.o.; 1 or 8 weeks) reduces atherosclerosis in mice by reducing inflammation[3].Loxoprofen sodium (60 μg/mL; p.o.; 24 days) suppresses mouse tumor growth by inhibiting VEGF[4]. Animal Model: | ||||||||||||
| Name | Loxoprofen | ||||||||||||
| CAS | 68767-14-6 | ||||||||||||
| Formula | C15H18O3 | ||||||||||||
| Molar Mass | 246.30 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Riendeau D, et al. Evaluation of loxoprofen and its alcohol metabolites for potency and selectivity of inhibition of cyclooxygenase-2. Bioorg Med Chem Lett. 2004;14(5):1201-1203. [2]. Paudel S, et al. Assessing Drug Interaction and Pharmacokinetics of Loxoprofen in Mice Treated with CYP3A Modulators. Pharmaceutics. 2019;11(9):479. Published 2019 Sep 16. [3]. Hamaguchi M, et al. Loxoprofen Sodium, a Non-Selective NSAID, Reduces Atherosclerosis in Mice by Reducing Inflammation. J Clin Biochem Nutr. 2010 Sep;47(2):138-47. [4]. Kanda A, et al. Loxoprofen sodium suppresses mouse tumor growth by inhibiting vascular endothelial growth factor. Acta Oncol. 2003;42(1):62-70. |