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
- 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.
- 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
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