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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-RAR/RXR-Ro41-5253
Ro41-5253

Chemical Structure : Ro41-5253

CAS No.: 144092-31-9

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Ro41-5253 (Ro 41-5253)

货号: PC-49025Not For Human Use, Lab Use Only.

Ro 41-5253 is a potent and selective retinoic acid receptor-α (RARα) antagonist with IC50 of 16 nM.

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

    生物&药学活性

    Ro 41-5253 is a potent and selective retinoic acid receptor-α (RARα) antagonist with IC50 of 16 nM.
    Ro41-5253 treatment ameliorated the depressive-like behaviors in CUMS rats, as evidenced by increased sucrose preference in SPT, raised numbers of crossing and rearing in OFT, reduced immobility time and prolonged swimming time in FST.
    Ro41-5253 (1 mg/kg) attenuated HPA axis hyperactivity by reduced serum corticosterone level, decreased adrenal gland index, reduced corticotrophin-releasing hormone protein level in hypothalamus, and recovered hypothalamic glucocorticoid receptor protein level.
    Ro41-5253 (1 mg/kg) treatment downregulated RARα protein expression in hypothalamic PVN and hypothalamus, and increased the protein levels of BDNF, PSD95, SYP and MAP2 in the hippocampus.
    Ro41-5253 completely abolished atRA-induced increase in fms transcript levels in breast carcinoma cells.

    物理化学性质&存储条件

    分子量 484.65
    分子式 C28H36O5S
    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

    4-[(1E)-2-[7-(Heptyloxy)-3,4-dihydro-4,4-dimethyl-1,1-dioxido-2H-1-benzothiopyran-6-yl]-1-propen-1-yl]benzoic acid

    参考文献

    1. Zhang LX, et al. J Biol Chem. 1995 Mar 17;270(11):6022-9.

    2. Shibakura M, et al. Blood. 1997 Aug 15;90(4):1545-51.

    3. Qi Ke, et al. Brain Res Bull. 2019 Mar;146:302-309.

    4. Sapi E, et al. Cancer Res. 1999 Nov 1;59(21):5578-85.

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