Disopain (mofezolac) / Tanabe Pharma - LARVOL DELTA

A further pocket or conformational plasticity by mapping COX-1 catalytic site through modified-mofezolac structure-inhibitory activity relationships and their antiplatelet behavior. (PubMed, Eur J Med Chem) - "Quantitative structure activity relationship (QSAR) models and molecular modelling (Ligand and Structure based virtual screening procedures) provide key information on the physicochemical and pharmacokinetic properties of the COX-1 inhibitors as well as new insights into the mechanisms of inhibition that will be used to guide the development of more effective and selective compounds. X-ray analysis was used to confirm the chemical structure of 14 (MSA17)."

Journal • Cardiovascular • CNS Disorders • Hematological Disorders • Oncology

SC-560 and mofezolac isosteres as new potent COX-1 selective inhibitors with antiplatelet effect. (PubMed, Arch Pharm (Weinheim)) - "Moreover, docking simulations were performed to reveal key interactions within the COX-1 binding pocket. Furthermore, the toxicity of the selected compounds was tested using the normal human kidney HK-2 cell line."

Journal • Oncology

Inhibition of cyclooxygenase-1 does not reduce mortality in post-ischemic stroke rats. (PubMed, Neurosci Lett) - "Overall, these results suggest that chronic treatment with the selective COX-1 inhibitor mofezolac did not reduce morbidity or mortality in post-stroke rats."

Journal • Preclinical • Cardiovascular • Immunology • Ischemic stroke • IL6 • TNFA

Effect of mofezolac-galactose distance in conjugates targeting cyclooxygenase (COX)-1 and CNS GLUT-1 carrier. (PubMed, Eur J Med Chem) - "Furthermore, Galmof0 (3) powerfully inhibits PGE2 release higher than mofezolac (1) in LPS-stimulated mouse BV2 microglial cell line, a worldwide recognized neuroinflammation model. In addition, Fingerprints for Ligands and Proteins (FLAP) was used to explain the different binding interactions of Galmofs with the COX-1 active site."

Journal • Biosimilar • Immunology

Targeting COX-1 by mofezolac-based fluorescent probes for ovarian cancer detection. (PubMed, Eur J Med Chem) - "Fingerprints for Ligands and Proteins (FLAP) software calculations were performed to justify 11 higher COX-1 inhibitory potency than mofezolac (COX-1 IC = 5.1 nM), which in turn is a moiety of 11. Specifically, the two compounds bind differently in the COX-1 active site."

Biomarker • Journal