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BPTU

CAS No. 870544-59-5

BPTU ( BPTU | BMS-646786 | BMS 646786 )

产品货号. M17632 CAS No. 870544-59-5

P2Y1 的变构拮抗剂(EC50 = 0.06-0.3 μM)。非核苷酸配体。结合螺旋束外部的受体。

纯度: >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
2MG ¥365 有现货
5MG ¥535 有现货
10MG ¥956 有现货
25MG ¥2033 有现货
50MG ¥3507 有现货
100MG ¥5200 有现货
200MG 获取报价 有现货
500MG 获取报价 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    BPTU
  • 注意事项
    本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
  • 产品简述
    P2Y1 的变构拮抗剂(EC50 = 0.06-0.3 μM)。非核苷酸配体。结合螺旋束外部的受体。
  • 产品描述
    Allosteric antagonist of P2Y1 (EC50 = 0.06-0.3 μM). Non-nucleotide ligand. Binds receptor outside of the helical bundle. Blocks inhibition of spontaneous contraction of rat and mouse colon induced by electrical field stimulation, nicotine and P2Y agonists. Antithrombotic; reduces platelet aggregation.
  • 体外实验
    BPTU blocks the supramaximal fast inhibitory junction potentials (fIJP) in a concentration-dependent manner both in the rat and mouse colon. The EC50 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<0.0001) and its effect is reversed with BPTU at 3 μM (82.7±3.6%). Addition of MRS2365, a selective P2Y1 agonist, at a concentration of 5 μM significantly reduces spontaneous contractions to a 21.2±4.8% (N=5) (P=0.0002) in the murine colon, and this reduction is blocked by 15 min incubation with BPTU at a concentration of 3 μM (93.1±3.8%). The blockage of the MRS2365-induced response by BPTU at 3 μM also occurs in control conditions (N=5) (10.2±5.5% vs. 86.7±5.0%).
  • 体内实验
    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.
  • 同义词
    BPTU | BMS-646786 | BMS 646786
  • 通路
    Others
  • 靶点
    Other Targets
  • 受体
    P2Y1
  • 研究领域
    Cardiovascular Disease
  • 适应症
    ——

化学信息

  • CAS Number
    870544-59-5
  • 分子量
    445.42
  • 分子式
    C23H22F3N3O3
  • 纯度
    >98% (HPLC)
  • 溶解度
    DMSO : ≥ 33.3 mg/mL. 74.76 mM; H2O : < 0.1 mg/mL
  • SMILES
    CC(C)(C)C1=CC=CC=C1OC2=C(C=CC=N2)NC(=O)NC3=CC=C(C=C3)OC(F)(F)F
  • 化学全称
    1-[2-(2-tert-Butylphenoxy)pyridin-3-yl]-3-[4-(trifluoromethoxy)phenyl]urea

运输与储存

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 稳定性
    ≥ 2 years

参考文献

1.Abrahamsen B, et al. J Neurosci. 2013 Jan 16;33(3):1068-87.
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