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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-ROR-BMS-336
BMS-336

Chemical Structure : BMS-336

CAS No.: 2204226-97-9

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BMS-336 (BMS336)

货号: PC-49023Not For Human Use, Lab Use Only.

BMS-336 is a potent, selective, orally active RORγt (RORC2) inverse agonist with EC50 of 39 nM in RORγt reporter assays.

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

    生物&药学活性

    BMS-336 is a potent, selective, orally active RORγt (RORC2) inverse agonist with EC50 of 39 nM in RORγt reporter assays.
    BMS-336 displays weak to no activity against PXR, LXRα an d LXRβ.
    BMS-336 (p.o.) significantly blocked the IL-17 response in a dose-dependent manner and achieved 74% inhibition at 25 mg/kg and 98% inhibition at 100 mg/kg doses, respectively.
    BMS-336 inhibited expression of RORC2-regulated genes in peripheral Th17 cells (CD4+CD25-CD127+CXCR3-CCR4+CCR6+) in a dose-dependent manner, with similar inhibitory effects on laminar propria mononuclear cells from IBD and non-IBD subjects.
    BMS-336 inhibited IL-17A production and prevented inflammatory cytokine-induced destabilization in peripheral Th17-Tregs (CD4+CD25hiCD127loCXCR3-CCR4+CCR6+).

    物理化学性质&存储条件

    分子量 618.539
    分子式 C25H26F8N2O5S
    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

    N-((R)-2-fluoro-3-hydroxy-3-methylbutyl)-2-((S)-1-((4-fluorophenyl)sulfonyl)-6-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-1,2,3,4-tetrahydroquinolin-2-yl)acetamide

    参考文献

    1. Hua Gong, et al. Bioorg Med Chem Lett. 2018 Jan 15;28(2):85-93.

    2. Dominic A Boardman, et al. Eur J Immunol. 2020 Sep;50(9):1400-1411.

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