Fenoprofen (Calcium hydrate)

Fenoprofen (LILLY-53858) Calcium hydrate is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen Calcium hydrate is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen Calcium hydrate also increases ERK1/2 activation in HEK293T cells. Fenoprofen Calcium hydrate has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis^[1][2]. In Vitro:In HEK293T cells, Fenoprofen Calcium hydrate stimulates ERK1/2 activation at MC3-5R in a biphasic manner, with the highest ERK1/2 activation observed at concentrations of 3 and 10 µM for MC3R, 1 µM for MC4R, and 3 µM for MC5R. No significant difference of Fenoprofen Calcium hydrate-induced pERK1/2 levels was observed in cells transfected with the empty vector pcDNA3.1 as well as MC1R. Fenoprofen Calcium hydrate induces biased signaling at MC3-5R, as it selectively activated ERK1/2 cascade but not the canonical cAMP signaling^[1].
In Vivo:Fenoprofen (10 mg/kg; i.p.; twice per day from day 2; for 7 days) Calcium hydrate presents anti-arthritic actions on cartilage integrity and synovitis, effects markedly attenuated in Mc3r^-/- mice^[2].