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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Cathepsin-RO5459072
RO5459072

Chemical Structure : RO5459072

CAS No.: 1252637-35-6

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RO5459072 (RG7625, Petesicatib)

货号: PC-60528Not For Human Use, Lab Use Only.

RO5459072 (Petesicatib, RG7625) is a potent, selective cathepsin S (Cat-S) inhibitor, inhibits human Cat-S with apparent IC50 of 0.1 nM and murine Cat-S of 0.3 nM.

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

    生物&药学活性

    RO5459072 (Petesicatib, RG7625) is a potent, selective cathepsin S (Cat-S) inhibitor, inhibits human Cat-S with apparent IC50 of 0.1 nM and murine Cat-S of 0.3 nM.
    RO5459072 displats no sub-micro molar inhibition on any other of the tested cathepsins (Cat L, B, K, and F) with the exception of Cat V with apparent IC50 of 700 nM.
    RO5459072 also shows ≤30% inhibition on a diversity panel consisting of nearly 100 receptor binding and enzymatic assays at 10 µM。
    RO5459072 inhibits Cat-S in cells in the lip10 accumulation assays in human purified B-cells from whole blood and a potent induction of lip10 with EC50 of 15.8 nM.
    RO5459072 attenuates systemic autoimmunity in MRL-(Fas)lpr mice, RO5459072 is more potent than MMF in suppressing kidney pathology.
    RO5459072 effectively suppresses hypergammaglobulinemia and anti-dsDNA production, albuminuria, and lupus nephritis disease activity.

    物理化学性质&存储条件

    分子量 603.54
    分子式 C25H23F6N5O4S
    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

    (2S,4R)-N-(1-cyanocyclopropyl)-4-((4-(1-methyl-1H-pyrazol-4-yl)-2-(trifluoromethyl)phenyl)sulfonyl)-1-(1-(trifluoromethyl)cyclopropane-1-carbonyl)pyrrolidine-2-carboxamide

    参考文献

    1. Tato M, et al. Sci Rep. 2017 Jun 5;7(1):2775.
    2. Theron M, et al. Front Immunol. 2017 Jul 17;8:806.
    3. Kratochwil NA, et al. Br J Clin Pharmacol. 2021 Sep;87(9):3550-3560.

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