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1426833-08-0

中文名稱 1426833-08-0
英文名稱 PDE2/PDE10-IN-1
CAS 1426833-08-0
分子式 C15H10ClN5
分子量 295.73
MOL 文件 1426833-08-0.mol
1426833-08-0 結構式 1426833-08-0 結構式

基本信息

中文別名
化合物 T12393
英文別名
PDE2/PDE10-IN-1
Pyrido[4,3-e][1,2,4]triazolo[4,3-a]pyrazine, 1-(2-chlorophenyl)-4-methyl-

物理化學性質

密度1.49±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度溶于二甲基亞砜
酸度系數(pKa)1.72±0.50(Predicted)
形態(tài)Solid
顏色Off-white to brown

常見問題列表

生物活性
PDE2/PDE10-IN-1 是一種磷酸二酯酶 PDE2 和 PDE10 抑制劑,IC50 分別為 29 和 480 nM。
靶點

hPDE2A

29 nM (IC 50 )

rPDE10A

480 nM (IC 50 )

hPDE4D

5890 nM (IC 50 )

hPDE11A

6920 nM (IC 50 )

體外研究

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.

體內研究

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.

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