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经验公式(希尔记法):
C25H20N4O · HCl
化学文摘社编号:
分子量:
428.91
UNSPSC Code:
51111800
NACRES:
NA.77
MDL number:
产品名称
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
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.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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
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
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