TAK-828F

• 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 RORγt isoforms selectivity (>5000-fold selectivity against human RORα and RORβ) [1].

• UNSPSC :

  12352005

• Target :

  ROR

• Type :

  Reference compound

• Related Pathways :

  Metabolic Enzyme/Protease; Vitamin D Related/Nuclear Receptor

• Applications :

  COVID-19-immunoregulation

• Field of Research :

  Inflammation/Immunology

• Assay Protocol :

  https://www.medchemexpress.com/TAK-828F.html

• Solubility :

  10 mM in DMSO

• Smiles :

  CC1(C)C2=C(F)C=C(NC([C@@H]3N(C([C@@H]4C[C@H](CC(O)=O)C4)=O)CCC5=C3C=CC(OC)=N5)=O)C=C2CC1

• Molecular Formula :

  C28H32FN3O5

• Molecular Weight :

  509.57

• References & Citations :

  [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.

• Shipping Conditions :

  Room temperature

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• CAS Number :

  [1854901-94-2]