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PF2545920

更新时间:2024-01-10 19:16:49

常用名 Mardepodect CAS号 898562-94-2
价格 ¥需询单/1kg ¥需询单/1g ¥需询单/1mg 纯度 98.0%
备货期 需询单 库存 询单
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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

供应商信息

上海楼岚生物科技有限公司

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电话:52996696
地址:沪南路2729弄1310号
地区: 上海市 上海市 浦东新区
联系人:孙先生
联系人电话:021-52996696
邮件:sales@lollanechem.com
网址:http://www.bioll.com
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参考价格:$168/5mg
其他供应商价格:
2022-11-29 PF-2545920(MP-10)
价格:¥需询单
2022-03-04 PF-2545920
价格:¥2302.0

查看所有价格,请点击Mardepodect价格