1426833-08-0
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- CAS号:
- 1426833-08-0
- 英文名:
- PDE2/PDE10-IN-1
- 英文别名:
- PDE2/PDE10-IN-1;PDE2/PDE10 IN 1,PDE-2/PDE10-IN-1,PDE2/PDE10IN1;Pyrido[4,3-e][1,2,4]triazolo[4,3-a]pyrazine, 1-(2-chlorophenyl)-4-methyl-
- 中文名:
- 1426833-08-0
- 中文别名:
- 化合物 T12393
- CBNumber:
- CB24796677
- 分子式:
- C15H10ClN5
- 分子量:
- 295.73
- MOL File:
- 1426833-08-0.mol
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1426833-08-0化学性质
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密度:
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1.49±0.1 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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酸度系数(pKa):
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1.72±0.50(Predicted)
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1426833-08-0性质、用途与生产工艺
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。
hPDE2A
29 nM (IC
50
)
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rPDE10A
480 nM (IC
50
)
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hPDE4D
5890 nM (IC
50
)
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hPDE11A
6920 nM (IC
50
)
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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.
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
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
---|
2024/04/30 | HY-U00427 | PDE2/PDE10-IN-1 | | 1 mg | 1909元 |
2024/04/30 | HY-U00427 | 1426833-08-0 PDE2/PDE10-IN-1 | 1426833-08-0 | 5 mg | 4200元 |
1426833-08-0, 1426833-08-0 相关搜索:
- 化合物 T12393
- 1426833-08-0
- PDE2/PDE10 IN 1,PDE-2/PDE10-IN-1,PDE2/PDE10IN1
- Pyrido[4,3-e][1,2,4]triazolo[4,3-a]pyrazine, 1-(2-chlorophenyl)-4-methyl-
- PDE2/PDE10-IN-1