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  • CCR2-RA-[R]
    货号: abs822239
    CAS号: 512177-83-2
    分子式: C18H19ClFNO3
    分子量: 351.80
    产品说明书
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    货号-规格 货期 价格 数量
    abs822239-5mg 4周 ¥1164.00
    - +
    abs822239-25mg 4周 ¥3704.00
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    大包装询价
    产品描述
    描述
    CCR2-RA-[R] is an allosteric antagonist of the C-C chemokine receptor type 2 (CCR2) with an IC50 of 103 nM.
    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
    可溶性/溶解性
    DMSO : ≥ 125 mg/mL (355.32 mM)
    生物活性
    In vitro(体外研究)
    The chemokine receptor CCR2 is a G protein-coupled receptor that is involved in many diseases characterized by chronic inflammation, and therefore a large variety of CCR2 small molecule antagonists has been developed. CCR2-RA-[R] displaces [125I]CCL2 from CCR2 with an pIC50 value of 6.1. The pKD of CCR2-RA-[R] for CCR2 and CCR5 is 8.8±0.1 and 7.0±0.1, respectively. CCR2-RA-[R] inhibits CCR2 non-competitively by blocking activation-associated conformational changes and formation of the G protein-binding interface. The binding pocket of CCR2-RA-[R] is highly enclosed and possesses a balanced combination of hydrophobic and polar features, all of which favors pocket “druggability”.
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    • 实验方法 实验条件
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