tak-828f

Description: TAK-828F is a novel, potent, selective, and orally bioavailable retinoic acid receptor-related orphan receptor gammat (RORgammat) inverse agonist with binding IC50 of 1.9 nM and reporter gene IC50 of 6.1 nM. TAK-828F shows excellent RORgammat isoforms selectivity (> 5000-fold selectivity against human RORalpha and RORbeta). TAK-828F showed potent RORgammat inverse agonistic activity, excellent selectivity against other ROR isoforms and nuclear receptors, and a good pharmacokinetic profile. In animal studies, oral administration of compound 10 exhibited robust and dose-dependent inhibition of IL-17A cytokine expression in a mouse IL23-induced gene expression assay. Furthermore, development of clinical symptoms in a mouse experimental autoimmune encephalomyelitis model was significantly reduced. Compound 10 was selected as a clinical compound for the treatment of Th17-driven autoimmune diseases.

References: J Med Chem. 2018 Apr 12; 61(7):2973-2988.

Related CAS : 1854901-94-2 (free base); 1854902-31-0 (sulfate); 1854902-23-0 (TAK-828F : sulfate : hydrate 2 : 2 : 1); 1854902-24-1 (TAK-828F : sulfate : hydrate 1:1:1)