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ST2 inhibitor XY52

Chemical Structure : ST2 inhibitor XY52

CAS No.:

ST2 inhibitor XY52

货号: PC-21150Not For Human Use, Lab Use Only.

ST2 inhibitor XY52 is a specific small molecule inhibitor of soluble suppression of tumorigenesis-2 factor (ST2) with IC5 of 5.68 and 4.59 uM in ST2/IL-33 AlphaLISA and HEK-Blue reporter assays, repsectively.

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

    生物&药学活性

    ST2 inhibitor XY52 is a specific small molecule inhibitor of soluble suppression of tumorigenesis-2 factor (ST2) with IC5 of 5.68 and 4.59 uM in ST2/IL-33 AlphaLISA and HEK-Blue reporter assays, repsectively.
    ST2 inhibitor XY52 shows 11-fold selectivity over ST2/IL1RAcP(IC50=64.3 uM) in AlphaLISA assay, inhibits more effectively the binding of IL-33 with sST2 than membrane ST2 bound with IL1RAcP.
    ST2 inhibitor XY52 shows improved inhibitory activity and metabolic stability in vitro and in vivo than iST2-1 (Cat# PC-35645).
    ST2 inhibitor XY52 (5-10 uM) induces dose-dependent reduction in CD4+ and CD8+ T-cell proliferation, with no significant toxicity to human peripheral blood mononuclear cells (PBMCs).
    ST2 inhibitor XY52 (40 mg/kg BID, i.p. 21 days) reduces plasma sST2 and IFN-γ levels and GVHD score and extends survival in mice graft versus host disease (GVHD) model.

    物理化学性质&存储条件

    分子量 499.66
    分子式 C30H37N5O2
    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

    3-(3-(1-((1-Ethyl-5-(2-methyl-4-nitrophenyl)-1H-pyrrol-2-yl)methyl)pyrrolidin-2-yl)phenyl)-3,8-diazabicyclo[3.2.1]octane

    参考文献

    1. Xinrui Yuan , et al. ACS Pharmacol Transl Sci. 2023 Aug 16;6(9):1275-1287.

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