产品
编 号：F254937
分子式：C26H33N7O2
分子量：475.59
分子式：C26H33N7O2
分子量：475.59
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CAS No: 2079892-79-6
产品详情
生物活性：
RORγt Inverse agonist 8 is a potent, selective, orally bioavailable RORγt inverse agonist, with an IC50 of 19 nM for human RORγt-LBD.
体内研究：
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.Animal Model:Female Lewis rats (190–220 g)
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.
体外研究：
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.
RORγt Inverse agonist 8 is a potent, selective, orally bioavailable RORγt inverse agonist, with an IC50 of 19 nM for human RORγt-LBD.
体内研究：
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.Animal Model:Female Lewis rats (190–220 g)
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.
体外研究：
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.
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