RORγt Inverse agonist 8 

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: 19 nM (RORγt)^[1]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

475.59

C₂₆H₃₃N₇O₂

2079892-79-6

O=C(C1=CN=C(C)N=C1)NC2=CN3C(C(CN4C[C@H](C)N(C(C5CCCC5)=O)CC4)=C2C)=NC=C3

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Guendisch U, et al. Pharmacological inhibition of RORγt suppresses the Th17 pathway and alleviates arthritis in vivo. PLoS One. 2017 Nov 20;12(11):e0188391.  [Content Brief]