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Merck
CN

PZ0351

Sigma-Aldrich

PF-2545920 hydrochloride

≥97% (HPLC)

别名:

2-[4-(1-Methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline hydrochloride, MP-10 hydrochloride, PF-02545920 hydrochloride, PF-920 hydrochloride

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About This Item

经验公式(希尔记法):
C25H20N4O · HCl
分子量:
428.91
MDL编号:
UNSPSC代码:
51111800
NACRES:
NA.77

质量水平

方案

≥97% (HPLC)

表单

powder

储存条件

desiccated

颜色

white to brown

溶解性

DMSO: 20 mg/mL, clear

储存温度

room temp

SMILES字符串

CN1C=C(C2=CC=NC=C2)C(C(C=C3)=CC=C3OCC4=NC5=CC=CC=C5C=C4)=N1.[H]Cl

InChI

1S/C25H20N4O/c1-29-16-23(18-12-14-26-15-13-18)25(28-29)20-7-10-22(11-8-20)30-17-21-9-6-19-4-2-3-5-24(19)27-21/h2-16H,17H2,1H3

InChI key

AZEXWHKOMMASPA-UHFFFAOYSA-N

生化/生理作用

PF-2545920 hydrochloride (MP-10) is a potent and selective cyclic nucleotide phosphodiesterase (PDE) 10A competitive inhibitor with a reported IC50 value of 1.26 nM. PDE10A hydrolyzes both cAMP and cGMP, and is highly expressed in medium spiny neurons of the mammalian striatum and in basal ganglia areas where D1 and D2 dopamine receptors are expressed. PF-2545920 has been studied for treatment of schizophrenia and Huntington′s disease.

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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Patrick R Verhoest et al.
Journal of medicinal chemistry, 52(16), 5188-5196 (2009-07-28)
By utilizing structure-based drug design (SBDD) knowledge, a novel class of phosphodiesterase (PDE) 10A inhibitors was identified. The structure-based drug design efforts identified a unique "selectivity pocket" for PDE10A inhibitors, and interactions within this pocket allowed the design of highly
Vahri Beaumont et al.
Neuron, 92(6), 1220-1237 (2016-12-06)
Huntington's disease (HD) symptoms are driven to a large extent by dysfunction of the basal ganglia circuitry. HD patients exhibit reduced striatal phoshodiesterase 10 (PDE10) levels. Using HD mouse models that exhibit reduced PDE10, we demonstrate the benefit of pharmacologic PDE10 inhibition
Jonathan M Wilson et al.
Neuropharmacology, 99, 379-386 (2015-08-11)
Studies described here tested the hypothesis that phosphodiesterase 10A inhibition by a selective antagonist, MP-10, activates the dopamine D2 receptor expressing medium spiny neurons to a greater extent than the D1 receptor expressing neurons. We used regional pattern of c-Fos

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