| Bioactivity | Mofezolac, a non-steroidal anti-inflammatory drug (NSAID), is a selective, reversible and orally active COX-1 inhibitor with an IC50 of 1.44 nM. Mofezolac shows weak inhibitory activity on COX-2 (IC50 of 447 nM). Mofezolac can relieve pain and has anti-inflammatory activities[1]. | |||||||||
| Invitro | Mofezolac inhibits platelet aggregation with an IC50 of 0.45 μM in human platelet rich plasma (hPRP) assay[2]. Mofezolac slightly increase Bortezomib cytotoxic effect on multiple myeloma (MM) cell lines (NCI-H929 and RPMI-8226) and affects MM cell cycle and apoptosis when co-administered with the proteasome inhibitor Bortezomib[2]. | |||||||||
| In Vivo | Mofezolac (1-30 mg/kg; oral administration; once) treatment results in the suppression of writhing induced by the intraperitoneal injection of phenyl-p-benzoquinone in mice[1]. Animal Model: | |||||||||
| Name | Mofezolac | |||||||||
| CAS | 78967-07-4 | |||||||||
| Formula | C19H17NO5 | |||||||||
| Molar Mass | 339.34 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. K Goto, et al. Analgesic effect of mofezolac, a non-steroidal anti-inflammatory drug, against phenylquinone-induced acute pain in mice. Prostaglandins Other Lipid Mediat. 1998 Jul;56(4):245-54. [2]. Maria Laura Pati, et al. Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability. Eur J Med Chem. 2019 Feb 15;164:59-76. |