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Mardepodect HCl(PF-2545920 HCl)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Mardepodect HCl(PF-2545920 HCl)图片
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)428.91
FormulaC25H20N4O. HCl
CAS No.N/A
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 10 mM
Water: N/A
Ethanol: N/A
Solubility (In vivo) CN1N=C(C2=CC=C(OCC3=NC4=CC=CC=C4C=C3)C=C2)C(C5=CC=NC=C5)=C1
Synonyms MP-10 HCl; MP10; MP 10, Mardepodect HCl; PF-2545920; PF 2545920; PF2545920 HCl
实验参考方法
In Vitro

In vitro activity: PF-2545920 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.


Kinase Assay: PF-2545920 (Also known as Mardepodect, MP-10) is a potent and selective PDE10A (phosphodiesterase) inhibitor with IC50 of 0.37 nM, and with>1000-fold selectivity over the PDE.

In VivoPF-2545920 is shown to be efficacious both in vitro and in vivo with improved penetration in CNS. It has excellent in vivo efficacy in neurochemical elevation of cyclic nucleotides and in models predictive of antipsychotic activity. Administration of PF-2545920 to mice can cause increase in striatal cGMP with the minimal effective dose at about 1mg/kg.
Animal modelJugular vein-cannulated male Sprague-Dawley rats
Formulation & DosageDissolved in 5:5:90 DMSO:1N HCl:saline; 0.1 mg/kg; i.v. injection
References

J Pharmacol Exp Ther. 2009 Nov;331(2):574-90; J Med Chem. 2009 Aug 27;52(16):5188-96.