生物活性 靶点 体外研究 体内研究 1426833-08-0 试剂级价格
ChemicalBook  CAS数据库列表  1426833-08-0

1426833-08-0

1426833-08-0,1426833-08-0,结构式
1426833-08-0
  • CAS号:1426833-08-0
  • 英文名:PDE2/PDE10-IN-1
  • 中文名:1426833-08-0
  • CBNumber:CB24796677
  • 分子式:C15H10ClN5
  • 分子量:295.73
  • MOL File:1426833-08-0.mol
1426833-08-0化学性质
  • 密度 :1.49±0.1 g/cm3(Predicted)
  • 储存条件 :Store at -20°C
  • 溶解度 :Soluble in DMSO
  • 酸度系数(pKa) :1.72±0.50(Predicted)

1426833-08-0性质、用途与生产工艺

  • 生物活性 PDE2/PDE10-IN-1 是一种磷酸二酯酶 PDE2 和 PDE10 抑制剂,IC50 分别为 29 和 480 nM。
  • 靶点

    hPDE2A

    29 nM (IC 50 )

    rPDE10A

    480 nM (IC 50 )

    hPDE4D

    5890 nM (IC 50 )

    hPDE11A

    6920 nM (IC 50 )

  • 体外研究

    PDE2/PDE10-IN-1 (Compound 6) inhibits PDE2 and PDE10, respectively, with an IC 50 value of 29 and 480 nM. PDE2/PDE10-IN-1 also inhibits PDE11A and PDE4D with IC 50 s of 6920 nM and 5890 nM, respectively. In addition PDE2/PDE10-IN-1 does not show significant inhibition of a panel of CYP450 enzymes (CYP1A2, 2C9, 2D6, 2C19, and 3A4). PDE2/PDE10-IN-1 is also inactive up to a concentration of 125 μg/mL in a bacterial mutagenicity assay.

  • 体内研究

    The PK properties of PDE2/PDE10-IN-1 are studied in rats after 2.5 mg/kg i.v. and 10 mg/kg p.o. administration. After i.v. administration, a rapid clearance is observed (t 1/2 =0.47 h), which is not expected based on the in vitro metabolic stability in rat liver microsomes (rLMs). Interestingly, PDE2/PDE10-IN-1 shows much slower clearance after p.o. administration (t 1/2 =2.36 h), resulting in good bioavailability and a maximum plasma concentration (C max ) of 997 ng/mL. PDE2/PDE10-IN-1 is assessed for its potential to cross the blood–brain barrier in rats after 10 mg/kg s.c. administration. PDE2/PDE10-IN-1 shows good formulatability with 10 to 20% HPβCD at pH>3.5. The brain concentration for PDE2/PDE10-IN-1 after 1 h administration is in the range of 370-895 ng/g with high brain free fractions and brain/plasma ratios. More specifically, PDE2/PDE10-IN-1, which is orally bioavailable, occupies PDE2 with an ED 50 of 21 mg/kg.

1426833-08-0上下游产品信息
上游原料
下游产品
1426833-08-0 试剂级价格
  • 更新日期:2024/04/30
  • 产品编号:HY-U00427
  • 产品名称:PDE2/PDE10-IN-1
  • CAS编号:
  • 包装:1 mg
  • 价格:1909元
  • 更新日期:2024/04/30
  • 产品编号:HY-U00427
  • 产品名称:1426833-08-0 PDE2/PDE10-IN-1
  • CAS编号:1426833-08-0
  • 包装:5 mg
  • 价格:4200元
1426833-08-0生产厂家
  • 公司名称:TargetMol Chemicals Inc.
  • 联系电话:+1-781-999-5354 +1-00000000000
  • 电子邮件:marketing@targetmol.com
  • 国家:美国
  • 产品数:19892
  • 优势度:58
  • 公司名称:TargetMol中国(陶术生物)
  • 联系电话: 4008200310
  • 电子邮件:marketing@tsbiochem.com
  • 国家:中国
  • 产品数:24017
  • 优势度:58
  • 公司名称:銳迪國際科技有限公司
  • 联系电话: 18024082417
  • 电子邮件:market@ubiochem.com
  • 国家:中国
  • 产品数:9180
  • 优势度:58