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  • GPR39-C3

    • TC-G 1008
    货号: abs812279
    CAS号: 1621175-65-2
    分子式: C18H19ClN6O2S
    分子量: 418.9
    产品说明书
    分享:
    货号-规格 货期 价格 数量
    abs812279-5mg 1-2周 ¥1147.00
    - +
    abs812279-10mg 1-2周 ¥1764.00
    - +
    大包装询价
    产品描述
    描述
    TC-G-1008 is a GPR39 (zinc receptor) agonist (EC50 values are 0.4 and 0.8 nM for rat and human receptors respectively). 
    纯度
    98%
    储存/保存方法
    Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
    基本信息
    别名
    TC-G 1008
    外观
    Solid powder
    可溶性/溶解性
    DMSO : ≥100 mg/mL
    生物活性
    靶点
    GHSR
    In vitro(体外研究)
    TC-G-1008 shows selectivity over a panel of kinases (IC50s>10 μM) and does not exhibit relevant binding affinity for the related ghrelin and neurotensin-1 receptors (IC50s>30 μM). In HEK293-GPR39 cells, GPR39-C3, which is a positive allosteric modulator, activates cAMP production (downstream of Gs), IP1 accumulation (downstream of Gq), SRF-RE-dependent transcription (downstream of G12/13), and β-arrestin recruitment. GPR39-C3 induces dose- and time-dependent loss of response in cAMP production by second challenge of the compound.
    In vivo(体内研究)
    Rat and mouse plasma protein binding for TC-G-1008 is measured as 99.3% and 99.1%, respectively. TC-G-1008 is orally bioavailable in mice and robustly induces acute GLP-1 levels. Upon single oral doses of 10, 30, and 100 mg/kg of aqueous suspensions in 0.5% methylcellulose/0.1% Tween 80, TC-G-1008 achieves, between 1 and 1.5 h, maximal exposures of 1.4, 6.1, and 25.3 μM, respectively.
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    • 实验方法 实验条件
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