RORγt Inverse agonist 8,207989

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RORγt Inverse agonist 8

CAS No. : 2079892-79-6

MCE 国际站：RORγt Inverse agonist 8

产品活性：RORγt Inverse agonist 8 是一种高效、有选择性的,可口服利用的 RORγt 反向激动剂，对人 RORγt-LBD (ligand binding domain) 作用的 IC₅₀ 值为 19 nM。

研究领域：Metabolic Enzyme/Protease  |  Vitamin D Related/Nuclear Receptor

作用靶点：ROR

In Vitro: RORγt Inverse agonist 8 (Cpd 1) is a potent RORγt inhibitor and binds to the ligand binding domain (LBD) of RORγt.
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.
RORγt Inverse agonist 8 selectively suppresses human Th17 and Tc17 cell differentiation.
RORγt Inverse agonist 8 polarizes Th17 cells also blocks IL-17A production in a concentration-dependent manner with an IC₅₀ of 92 nM.
RORγt Inverse agonist 8 reduces Th17 cell-associated mRNA expression including IL17A, IL17F, IL26, IL23R and CCR6 in a concentration-dependent fashion.
RORγt Inverse agonist 8 alters epigenetic regulation at the IL17A and IL23R gene promoters without impairing the DNA binding activity of RORγt.

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.

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