RORγt inverse agonist 30

Names

[ CAS No. ]:
1445901-41-6

[ Name ]:
RORγt inverse agonist 30

Biological Activity

[Description]:

RORγt inverse agonist 30 (Compound 1) is a potent RORγt inverse agonist with the IC50 of 46 nM. Targeting the nuclear receptor RORγt is effective in autoimmune disorders[1].

[Related Catalog]:

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

[Target]

RORγt:46 nM (IC50)


[In Vitro]

RORγt inverse agonist 30 (compound 1) inhibits mouse Th17 cell differentiation with an IC50 of 0.67 μM[1].

[In Vivo]

RORγt inverse agonist 30 exhibits favorable pharmacokinetics profiles with T1/2 of 2.3 min, CLint of 612 μL/min/mg and CLint(liver) of 2423.5 mL/min/kg[1].

[References]

[1]. Nannan Sun, et al. Discovery of novel N-sulfonamide-tetrahydroquinolines as potent retinoic acid receptor-related orphan receptor γt inverse agonists for the treatment of autoimmune diseases. Eur J Med Chem. 2020 Feb 1;187:111984.

Chemical & Physical Properties

[ Molecular Formula ]:
C24H31N3O3S

[ Molecular Weight ]:
441.59

Related Compounds