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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Keap1-Nrf2-S217879
S217879

Chemical Structure : S217879

CAS No.: 2700303-28-0

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S217879 (S 217879, CAS 2700303-28-0)

货号: PC-20065Not For Human Use, Lab Use Only.

S217879 (S 217879) is a highly potent and selective NRF2 activator, binds to KEAP1 Kelch domain (SPR Kd=4.15 nM), disrupts the KEAP1-NRF2 interaction leading to robust NRF2 pathway activation.

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

    生物&药学活性

    S217879 (S 217879) is a highly potent and selective NRF2 activator, binds to KEAP1 Kelch domain (SPR Kd=4.15 nM), disrupts the KEAP1-NRF2 interaction leading to robust NRF2 pathway activation.
    S217879 displays high selectivity for KEAP1 binding in a broad selectivity panel comprising 110 targets at 10 uM.
    S217879 significantly activated a reporter gene driven by an ARE in HepG2 cells in a concentration-dependent manner with an EC50 of 18 nM, reduced H2O2-stimulated ROS production in HepG2 cells.|
    In hPBMCs, S217879 treatment for 6 h resulted in a concentration-dependent increase in Nqo1 gene expression with an EC50 of 16 nM.
    Pretreatment for 4 h with S217879 led to a significant and concentration-dependent inhibition of LPS-induced cytokine release as measured by IL1β, MCP-1 and IL6 MagPix multiplex assays.
    S217879 (30 mg/kg, PO, QD) reduced NASH progression in MCDD mice in a dose-dependent manner, reduced NASH progression and liver fibrosis in DIO NASH mice model.

    物理化学性质&存储条件

    分子量 578.64
    分子式 C29H30N4O7S
    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

    2-((2R,4S)-54,2-dimethyl-12,12-dioxido-13,14-dihydro-51H-8,11-dioxa-1(3,6)-benzo[e][1,2,3]oxathiazina-5(6,1)-benzo[d][1,2,3]triazola-3(1,3)-benzenacycloundecaphane-4-yl)acetic acid

    参考文献

    1. Klaus Seedorf, et al. JHEP Rep. 2022 Dec 16;5(4):100651.

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