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TAK-828F

Names

[ CAS No. ]:
1854901-94-2

[ Name ]:
TAK-828F

Biological Activity

[Description]:

TAK-828F is a potent, selective, and orally available retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist (binding IC50=1.9 nM, reporter gene IC50=6.1 nM). TAK-828F shows excellent ROR isoforms selectivity (>5000-fold selectivity against human RORα and RORβ)[1].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> ROR
Research Areas >> Inflammation/Immunology

[Target]

IC50: 1.9 nM (RORγt, binding IC50), 6.1 nM (RORγt, reporter gene IC50)[1]


[References]

[1]. Kono M, et al. Discovery of [ cis-3-({(5 R)-5-[(7-Fluoro-1,1-dimethyl-2,3-dihydro-1 H-inden-5-yl)carbamoyl]-2-methoxy-7,8-dihydro-1,6-naphthyridin-6(5 H)-yl}carbonyl)cyclobutyl]acetic Acid (TAK-828F) as a Potent, Selective, and Orally Available Novel Retinoic Acid Receptor-Related Orphan Receptor γt Inverse Agonist. J Med Chem. 2018 Apr 12;61(7):2973-2988.

Chemical & Physical Properties

[ Molecular Formula ]:
C28H32FN3O5

[ Molecular Weight ]:
509.57

Related Compounds