Potent and reversible fatty acid desaturase 1 (FADS1; Δ5 desaturase) inhibitor (IC50 values are 1.9 nM and 2.1 nM in human and rat hepatocyte cell lines, respectively). Exhibits >300 fold selectivity for FADS1 over FADS2 (Δ6 desaturase). Inhibits arachidonic acid production in rat and human hepatocyte cell lines. Orally bioavailable.
Miyahisa et al (2016) T-3364366 targets the desaturase domain of delta-5 desaturase with nanomolar potency and a multihour residence time. ACS Med.Chem.Lett. 7 868 PMID:27660693