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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Constitutive androstane receptor (CAR)-DL7076
DL7076

Chemical Structure : DL7076

CAS No.: 2702273-17-2

DL7076 (CN06)

货号: PC-49714Not For Human Use, Lab Use Only.

DL7076 (CN06) is a small molecule dual activator of the constitutive androstane receptor (CAR, NR1I3) and nuclear factor erythroid 2-related factor 2 (Nrf2) with EC50 of 8.85 and 0.72 uM, respectively.

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

    生物&药学活性

    DL7076 (CN06) is a small molecule dual activator of the constitutive androstane receptor (CAR, NR1I3) and nuclear factor erythroid 2-related factor 2 (Nrf2) with EC50 of 8.85 and 0.72 uM, respectively.
    At concentrations that markedly activate hCAR and Nrf2, and induce their target genes, CN06 is nontoxic to HPH, TNBC cells, H9c2 cells, or human iPSC–derived CM (hiPSC-CM).
    CN06 (1-10 uM) induces hepatic expression of CYP2B6 over CYP3A4 via activation of hCAR, enhances CPA-mediated cytotoxicity in TNBC cells.
    CN06 activates Nrf2 antioxidant signaling in H9c2 cells but not in TNBC cells, attenuates DOX-induced cell death.
    CN06 enhances the anticancer activity while repressing cardiotoxicity of the CPA/DOX combination in a multicellular coculture model, protects DOX-induced cell death and impaired contractility in hiPSC-CMs.

    物理化学性质&存储条件

    分子量 378.47
    分子式 C19H14N4OS2
    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-(2-isothiocyanatoethyl)-6-(naphthalen-2-yl)imidazo[2,1-b]thiazole-5-carboxamide

    参考文献

    1. Sydney Stern, et al. JCI Insight. 2022 Jun 22;7(12):e153868.

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