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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-ROR-RORγt inverse agonist 1
RORγt inverse agonist 1

Chemical Structure : RORγt inverse agonist 1

CAS No.: 2079892-79-6

RORγt inverse agonist 1

货号: PC-60487Not For Human Use, Lab Use Only.

RORγt inverse agonist 1 is a potent, selective, orally bioavailable RORγt inverse agonist with IC50 of 17 nM in TR-FRET assays.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    RORγt inverse agonist 1 is a potent, selective, orally bioavailable RORγt inverse agonist with IC50 of 17 nM in TR-FRET assays.
    RORγt inverse agonist 1 shows no inhibitory activity against the closely related nuclear hormone receptors RORα or RORβ.
    RORγt inverse agonist 1 attenuates expression of genes such as IL26, IL23R and CCR6 in primary human Th17 cells, attenuate the knee swelling response in an antigen-induced arthritis rat models and inhibits IL-17A cytokine production in ex vivo recall assays.

    物理化学性质&存储条件

    分子量 475.597
    分子式 C26H33N7O2
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20 °C 12 个月; 4°C 6 个月
    配置液
    -80 °C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    (S)-N-(8-((4-(cyclopentanecarbonyl)-3-methylpiperazin-1-yl)methyl)-7-methylimidazo[1,2-a]pyridin-6-yl)-2-methylpyrimidine-5-carboxamide

    参考文献

    1. Guendisch U, et al. PLoS One. 2017 Nov 20;12(11):e0188391.

    2. Hintermann S, et al. ChemMedChem. 2016 Dec 16;11(24):2640-2648.

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