RORγt Inverse agonist 8
CAS No. : 2079892-79-6
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| Cat. No. : | HY-122737 |
| M.Wt: | 475.59 |
| Formula: | C26H33N7O2 |
| Purity: | >98 % |
| Solubility: | 10 mM in DMSO |
RORγt Inverse agonist 8 is a potent, selective, orally bioavailable RORγt inverse agonist, with an IC50 of 19 nM for human RORγt-LBD[1].
IC50 & Target: IC50: 19 nM (RORγt)[1]
In Vitro: RORγt Inverse agonist 8 (Cpd 1) is a potent RORγt inhibitor and binds to the ligand binding domain (LBD) of RORγt[1].
RORγt Inverse agonist 8 (0-10μM ;24 hours) results in complete attenuation of IL-17A secretion in a concentration-dependent manner with an IC50 of 60 nM in HUT78 cells[1].
RORγt Inverse agonist 8 selectively suppresses human Th17 and Tc17 cell differentiation[1].
RORγt Inverse agonist 8 polarizes Th17 cells also blocks IL-17A production in a concentration-dependent manner with an IC50 of 92 nM[1].
RORγt Inverse agonist 8 reduces Th17 cell-associated mRNA expression including IL17A, IL17F, IL26, IL23R and CCR6 in a concentration-dependent fashion[1].
RORγt Inverse agonist 8 alters epigenetic regulation at the IL17A and IL23R gene promoters without impairing the DNA binding activity of RORγt[1].
In Vivo: RORγt Inverse agonist 8 (15 mg/kg, 45 mg/kg ; i.g.; twice daily; for 7 days) ameliorates antigen-induced arthritis (AiA) responses in Lewis rats[1].
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