PF-2545920

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发布时间： 2024-07-15 12:37:28

CAS号：898562-94-2

常用名： Mardepodect

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纯度： 98.0%

备货期： 10天

库存： 现货

其他详情（用途，包装）：
用途： PF-2545920 is a potent and selective PDE10A inhibitor with IC50 of 0.37 nM, with >1000-fold selectivity over the PDE. IC50 value: 0.37 nM [1]Target: PDE10APDE10A subcutaneously administrated at dose of 1 mg/kg elevates striatal cGMP about 3 fold in male CD-1 mice, while PDE10A subcutaneously administrated at dose of 3.2 mg/kg displays a maximal elevation of striatal cGMP approximately a 5-fold increase in male CD-1 mice. PDE10A intravenous injected at a dose of 0.1 mg/kg in Sprague-Dawley rats displays clearance of 36 ml/min/Kg, DE10A intravenous injected at a dose of 0.3 mg/kg in Dog Beagle displays clearance of 7.2 ml/min/Kg in vivo clearance with a moderate volume of distribution, DE10A intravenous injected at a dose of 0.03 mg/kg in Monkey Cynomolgus displays clearance of 13.9 ml/min/Kg in vivo clearance with a moderate volume of distribution. PDE10A is active with an ED50 of 1 mg/kg at a significantly lower total plasma exposure (115 nM) in the conditioned avoidance response assay (CAR) in Sprague-Dawley rats [1]. MP-10 intraperitoneally administrated at dose of 0.3, 3, and 5 mg/kg in male CF-1 mice causes striking increases in GluR1 phosphorylation levels of 3-, 5.4-, and 4.1-fold , respectively. MP-10 at concentration of 1 μM treats Rat striatal slices for 30 min, the level of GluR1S845 phosphorylation at the cell surface is significantly increased 2-fold, without change the level of total GluR1 on the cell surface. MP-10 intraperitoneally administrated at dose of 0.3, 3, and 5 mg/kg in male CF-1 mice results in robust, statistically significant increases in CREBS133 phosphorylation of 3-, 4-, and 2.6-fold, respectively. MP-10 intraperitoneally administrated at dose of 3 mg/kg increases both enkephalin and substance-P mRNA levels in striatum of CF-1 mice. MP-10 intraperitoneally administrated at dose of 0.3-1 mg/kg decreases avoidance responding with a significant treatment effect in the mouse CAR model. Mice treated with MP-10 at dose of 0.03 mg/kg spents more time in the empty than social side in the mice, MP-10 also dose-dependently decreased locomotor activity [2]. 物理化学性质： CAS号：898562-94-2 常用中文名：Mardepodect 常用英文名：PF-2545920 分子式：C25H20N4O 分子量：392.453 密度：1.2±0.1 g/cm3 沸点：568.6±50.0 °C at 760 mmHg 熔点：N/A 闪点：297.7±30.1 °C 储存条件：-20°C，密闭，干燥

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公司名：上海念兴实业有限公司推荐

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地区： 上海市普陀区

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2022-03-04 价格：￥2302.0 PF-2545920

2024-07-15 价格：需询单 PF-2545920

2023-09-22 价格：￥需询单 PF2545920

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Mardepodect价格

PF-2545920

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