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  • PD176252

    货号: abs821472
    CAS号: 204067-01-6
    分子式: C32H36N6O5
    分子量: 584.67
    产品说明书
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    货号-规格 货期 价格 数量
    abs821472-10mg 1-2周 ¥1760.00
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    大包装询价
    产品描述
    描述
    PD176252 is a potent antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptor with Kis of 0.17 nM and 1 nM for human BB1 and BB2 receptors, and 0.66 nM, 16 nM for Rat BB1 and BB2 receptors, respectively; PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC50s of 0.31 and 0.66 μM in HL-60 cells.
    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 : 115 mg/mL (196.69 mM; Need ultrasonic)
    生物活性
    In vitro(体外研究)
    PD176252 is a potent antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptor with Kis of 0.17 nM and 1 nM for human BB1 and BB2 receptors, and 0.66 nM, 16 nM for Rat BB1 and BB2 receptors, respectively. PD176252 inhibits acidification responses to neuromedin-B or neuromedin-C at the human BB1 or BB2 receptors expressed in CHO cells, with the appKBs of 4.0 nM or 13 nM, and blocks bombesin-evoked increases in intracellular calcium levels in CHO cells stably expressing human BB1 or BB2 receptors, with appKBs of 2.3 nM and 36 nM, respectively. PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC50s of 0.31 and 0.66 μM in HL-60 cells. PD176252 activates Ca2+ mobilization in HL-60 cells transfected with human FPRs (EC50, 0.72 ± 0.21 μM). PD176252 inhibits little specific 125I-gastrin releasing peptide binding to NCI-H345 cells at 1 nM and suppresses almost all specific bindings at 1000 nM, with an IC50 of 30 nM. PD176252 (10, 30 μM) significantly inhibits the growth of NCI-H345 or H1299 cells, with IC50s of 7 and 5 μM.
    In vivo(体内研究)
    PD176252 (1, 10 μg, p.o.) potently inhibits the growth of the proliferation of NCI-H1299 xenografts in nude mice.
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