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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Pregnane X Receptor (PXR)-FKK6
FKK6

Chemical Structure : FKK6

CAS No.: 2238839-34-2

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FKK6 (Felix Kopp Kortagere 6)

货号: PC-38840Not For Human Use, Lab Use Only.

FKK6 (Felix Kopp Kortagere 6) is a specific human pregnane X receptor (hPXR) agonist with IC50 of 1.56 uM in a cell‐free competitive hPXR TR‐FRET‐binding assays.

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

    生物&药学活性

    FKK6 (Felix Kopp Kortagere 6) is a specific human pregnane X receptor (hPXR) agonist with IC50 of 1.56 uM in a cell‐free competitive hPXR TR‐FRET‐binding assays.
    FKK6 did not significantly activate mouse PXR, did not activate AhR and several other related xenobiotic receptors, as well as a broad array of kinase enzymes.
    FKK6 induces robust expression of PXR target genes in intestinal cell lines (LS180, LS174T), also enhances both CYP3A4 and MDR1 promoter occupancy in cells.
    FKK6 inhibited NF‐κB activation in a PXR‐dependent manner in intestinal cell lines (LS180, LS174T), inhibited cytokine and salmonella infection‐induced NF‐κB nuclear translocation in Caco‐2 cells and iPSC‐derived human intestinal organoids.
    FKK6 induced PXR target gene cyp3a11 in mice expressing the human PXR transgene, but not in conventional wild‐type mice or pxr −/− mice, abrogated dextran sulfate sodium‐induced colitis in mice expressing the human PXR gene.

    物理化学性质&存储条件

    分子量 402.468
    分子式 C23H18N2O3S
    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

    1-(1-(phenylsulfonyl)-1H-indol-2-yl)-1-(pyridin-4-yl)but-3-yn-1-ol

    参考文献

    1. Zdeněk Dvořák, et al. EMBO Mol Med. 2020 Apr 7;12(4):e11621.

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