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  • BPTU

    • BMS-646786
    货号: abs822883
    CAS号: 870544-59-5
    分子式: C23H22F3N3O3
    分子量: 445.43
    产品说明书
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    货号-规格 货期 价格 数量
    abs822883-10mg 1-2周 ¥1250.00
    - +
    abs822883-50mg 1-2周 ¥3750.00
    - +
    大包装询价
    产品描述
    描述
    BPTU is a novel P2Y1 allosteric antagonist.
    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
    BMS-646786
    可溶性/溶解性
    DMSO : ≥ 33.3 mg/mL (74.76 mM)
    生物活性
    靶点
    P2Y1
    In vitro(体外研究)
    BPTU blocks the supramaximal fast inhibitory junction potentials (fIJP) in a concentration-dependent manner both in the rat and mouse colon (P50 of BPTU is approximately 0.3 μM and 0.06 μM for the rat and mouse colon, respectively. In the rat colon, addition of the P2Y agonist ADPβS at 10 μM significantly reduces spontaneous contractions to a 43.2±13.4% (N=5) (P=0.0002), and this reduction is blocked by 15 min incubation with BPTU at a concentration of 3 μM (93.3±5.1%). Similar results are obtained in the murine colon where ADPβS at 10 μM reduces the area under the curve (AUC) of contractions to a 15.8±5.1% (N=4) (P.
    In vivo(体内研究)
    Uptake of BPTU from the peritoneal cavity is relatively rapid. Blood boron levels are maximal within 1 h after administration. After only 1 h, a boron tumor-to-blood ratio above 1 is found for BPTU in pigmented tumors, which is indicative of drug retention. This is not seen in the non-pigmented tumor variant, in which tumor boron levels closely follow blood levels. Up to 24 h, Borocaptate sodium (BSH) exhibits no selective retention in either tumor, but achieves higher maximum tumor boron concentrations than BPTU as a result of the administration of higher amounts of boron. During the tissue distribution phase, liver-to-kidney boron concentration ratios range from 2 to 4 for BSH and from 0.5 to 1 for BPTU.
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