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首页-小分子抑制剂&激动剂-GPCR-5-HT Receptor-DSP-1053
DSP-1053

Chemical Structure : DSP-1053

CAS No.: 1176326-78-5

DSP-1053 (DSP1053)

货号: PC-63256Not For Human Use, Lab Use Only.

DSP-1053 is a novel potent serotonin reuptake (SERT) inhibitor with 5-HT1A partial agonistic activity that binds to human serotonin transporter and 5-HT1A receptor with Ki of 1.02 and 5.05 nM, respectively.

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

    生物&药学活性

    DSP-1053 is a novel potent serotonin reuptake (SERT) inhibitor with 5-HT1A partial agonistic activity that binds to human serotonin transporter and 5-HT1A receptor with Ki of 1.02 and 5.05 nM, respectively.
    DSP-1053 inhibits serotonin transporter with IC50 of 2.74 nM and shows an intrinsic activity for 5-HT1A receptors of 70.0%.
    DSP-1053 dose-dependently increases extracellular 5-HT levels in rat microdialysis at 3-10 mg/kg, demonstrates antidepressant-like effect in vivo.

    物理化学性质&存储条件

    分子量 660.62
    分子式 C32H38BrNO7S
    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

    6-(2-{4-[4-Bromo-3-(2-methoxyethoxy)benzyl]piperidin-1-yl}ethyl)-2,3-dihydro-4H-chromen-4-one benzenesulfonate

    参考文献

    1. Yoshinaga H, et al. Bioorg Med Chem. 2018 May 1;26(8):1614-1627.

    2. Kato T, et al. Pharmacol Res Perspect. 2015 Jun;3(3):e00142.

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