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。
| 生物活性 | RORγt Inverse agonist 8 is a potent, selective, orally bioavailableRORγtinverse agonist, with anIC50of 19 nM for human RORγt-LBD[1]. |
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体外研究
(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 IC50of 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 IC50of 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].
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体内研究
(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].
| Animal Model: | Female Lewis rats (190–220 g)[1] | | Dosage: | 15 mg/kg, 45 mg/kg | | Administration: | Oral gavage; twice daily; for 7 days | | Result: | Ameliorates antigen-induced arthritis (AiA) responses in Lewis rats. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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