FR122047

FR122047 is a **selective cyclooxygenase-1 (COX-1) inhibitor** with potent **anti-inflammatory**, **analgesic**, and **antiplatelet** properties. It is a small molecule that, both in vitro and in vivo, inhibits COX-1-derived prostaglandin and thromboxane synthesis much more potently than COX-2 (COX-1 IC50 = 0.028 μM; COX-2 IC50 = 65 μM)[7][13][15]. FR122047 is orally active and shows dose-dependent anti-inflammatory activity in animal models of collagen-induced arthritis, reducing prostaglandin E2 (PGE2) and thromboxane B2 (TXB2) at inflamed sites, without observable gastric mucosal damage typical of non-selective NSAIDs[1][4][8][9][10][12]. Its analgesic efficacy in chemical nociception models is significant, though somewhat less potent than non-selective NSAIDs like indomethacin[4]. FR122047 is also a highly potent antiplatelet agent, being 100 times more effective than aspirin in vitro[3][13]. In cell studies, it induces growth arrest and apoptosis in breast cancer cell lines, suggesting potential as a research tool in cancer biology[6]. Topically, it inhibits PGE2 elevation in experimental ocular inflammation[2]. FR122047 was developed by Fujisawa Pharmaceutical[4]. There is no indication it has reached or advanced into clinical development in humans.

Other names

1-[(4,5-bis(4-methoxyphenyl)-2-thiazoyl)carbonyl]-4-methylpiperazine hydrochloride