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Merck
CN

PZ0351

PF-2545920 hydrochloride

≥97% (HPLC)

Synonym(s):

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

Empirical Formula (Hill Notation):
C25H20N4O · HCl
CAS Number:
898562-94-2
Molecular Weight:
428.91
UNSPSC Code:
51111800
NACRES:
NA.77
MDL number:
MFCD30489759

Key Documents

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Product Name

PF-2545920 hydrochloride, ≥97% (HPLC)

form

powder

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

SMILES string

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

InChI key

AZEXWHKOMMASPA-UHFFFAOYSA-N

assay

≥97% (HPLC)

storage condition

desiccated

color

white to brown

solubility

DMSO: 20 mg/mL, clear

storage temp.

room temp

Quality Level

100

Biochem/physiol Actions

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.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000267865
0000263274
0000263274
0000267865
0000107240

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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
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
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

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