1. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  2. ROR
  3. RORγt Inverse agonist 8

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。

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RORγt Inverse agonist 8 Chemical Structure

RORγt Inverse agonist 8 Chemical Structure

CAS No. : 2079892-79-6

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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[1].

IC50 & Target

IC50: 19 nM (RORγt)[1]

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 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].

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

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].

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

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.
分子量

475.59

Formula

C26H33N7O2

CAS 号
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.

纯度 & 产品资料
参考文献

RORγt Inverse agonist 8 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
RORγt Inverse agonist 8
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HY-122737
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