基本信息 物理化学性质 1426833-08-0价格(试剂级) 常见问题列表 供应商 相关产品
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1426833-08-0

中文名称 1426833-08-0
英文名称 PDE2/PDE10-IN-1
CAS 1426833-08-0
分子式 C15H10ClN5
分子量 295.73
MOL 文件 1426833-08-0.mol
结构式 1426833-08-0 结构式

基本信息

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

物理化学性质

密度 1.49±0.1 g/cm3(Predicted)
储存条件 -20°C储存
溶解度 溶于二甲基亚砜
酸度系数(pKa) 1.72±0.50(Predicted)

常见问题列表

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.

供应商信息 更多

深圳市丽晶生化科技有限公司
联系电话: 0755-0755-85201366 18938635012
产品介绍:
英文名称:PDE2/PDE10-IN-1
CAS:1426833-08-0
纯度:>98.0%
包装信息:10mg;100mg
备注:抑制剂进口标准品
天津普西唐生物医药科技有限公司
联系电话: 010-60605840
产品介绍:
英文名称:PDE2/PDE10-IN-1
CAS:1426833-08-0
包装信息:100mg
备注: 试剂级
TargetMol中国(陶术生物)
联系电话: 4008200310
产品介绍:
中文名称:化合物 T12393
英文名称:PDE2/PDE10-IN-1;PDE2/PDE10 IN 1,PDE-2/PDE10-IN-1,PDE2/PDE10IN1
CAS:1426833-08-0
纯度:98%
包装信息:25 mg
銳迪國際科技有限公司
联系电话: 18024082417
产品介绍:
英文名称:PDE2/PDE10-IN-1
CAS:1426833-08-0
纯度:5mg;10mg;50mg;100mg;250mg;500mg;1g
包装信息:5mg;10mg;50mg;100mg;250mg;500mg;1g