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当前位置: 首页 > 信号通路研究 > PDE > PF2545920
PF2545920
PF2545920
PF2545920
商品货号:MB7418
CAS 号:1292799-56-4
英文名字:PF-2545920
质量标准:>98%,选择性PDE10A抑制剂
分子式:C25H20N4O
  • 包装规格:
    规格 库存 发货时间
    10MG [¥1800.00]15 现货,一周内发货
    50MG [¥6800.00]15 现货,一周内发货
    200MG [¥12000.00]15 现货,一周内发货
  • 购买数量:
  • 会员尊享价:

    商品信息

    质检证书(coa)

    说明书下载

     PF2545920

    分子式:C25H20N4O   分子量392.45

     

    产品描述

    PF-2545920是有效的,选择性PDE10A抑制剂,IC500.37 nM,比作用于PDE选择性高1000倍以上。

    靶点

    PDE10A

             

    IC50

    0.37 nM

             

    体外研究

    MP-10 shows excellent potency and selectivity of PDE10A with IC50 of 1.26 nM.

    体内研究

    MP-10 intraperitoneally administrated at dose of 0.3, 3, and 5 mg/kg in male CF-1 mice causes striking increases in GluR1 phosphorylation levels of 3-, 5.4-, and 4.1-fold , respectively. MP-10 at concentration of 1 μM treats Rat striatal slices for 30 min, the level of GluR1S845 phosphorylation at the cell surface is significantly increased 2-fold, without change the level of total GluR1 on the cell surface. MP-10 intraperitoneally administrated at dose of 0.3, 3, and 5 mg/kg in male CF-1 mice results in robust, statistically significant increases in CREBS133 phosphorylation of 3-, 4-, and 2.6-fold, respectively. MP-10 intraperitoneally administrated at dose of 3 mg/kg increases both enkephalin and substance-P mRNA levels in striatum of CF-1 mice. MP-10 intraperitoneally administrated at dose of 0.3-1 mg/kg decreases avoidance responding with a significant treatment effect in the mouse CAR model. Mice treated with MP-10 at dose of 0.03 mg/kg spents more time in the empty than social side in the mice, MP-10 also dose-dependently decreased locomotor activity.PDE10A subcutaneously administrated at dose of 1 mg/kg elevates striatal cGMP about 3 fold in male CD-1 mice, while PDE10A subcutaneously administrated at dose of 3.2 mg/kg displays a maximal elevation of striatal cGMP approximately a 5-fold increase in male CD-1 mice. PDE10A intravenous injected at a dose of 0.1 mg/kg in Sprague-Dawley rats displays clearance of 36 ml/min/Kg, DE10A intravenous injected at a dose of 0.3 mg/kg in Dog Beagle displays clearance of 7.2 ml/min/Kg in vivo clearance with a moderate volume of distribution, DE10A intravenous injected at a dose of 0.03 mg/kg in Monkey Cynomolgus displays clearance of 13.9 ml/min/Kg in vivo clearance with a moderate volume of distribution. PDE10A is active with an ED50 of 1 mg/kg at a significantly lower total plasma exposure (115 nM) in the conditioned avoidance response assay (CAR) in Sprague-Dawley rats.

    溶解性

    DMSO 79 mg/mL,水 <1 mg/mL,乙醇 79 mg/mL

    稳定性

    2 -20°C粉状,6-80°C溶于DMSO

    特征

           

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    http://www.meilune.com/article.php?id=374

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    http://www.meilune.com/article.php?id=374

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