A brain-permeable PDE inhibitor selective for PDE9A (IC50 = 12 nM) over other PDEs (IC50s = >940 nM); over 1

PF-04447943 – 1 mg

Brand:
Cayman
CAS:
1082744-20-4
Storage:
-20
UN-No:
De Minimis - 3077 / 9

PF-04447943 is a brain-permeable phosphodiesterase (PDE) inhibitor that is selective for PDE9A (IC50 = 12 nM) over other PDEs (IC50s = >940 nM) in enzymatic assays of second messenger hydrolysis.{41434} It is over 1,000-fold more selective for PDE9A over 79 non-PDE targets, with the exception of the melatonin MT3/ML2 receptor (Ki = 3,800 nM). PF-04447943 also inhibits rat and rhesus monkey PDE9A (Kis = 18.1 and 4.5 nM, respectively).{41435} It increases neurite outgrowth and the density of synapsin puncta in primary rat hippocampal neurons when used at a concentration of 0.03 μM. PF-04447943 increases the cGMP level in the striatum and frontal cortex of mice and in the cerebrospinal fluid (CSF) of rats when administered at 10 and 1 mg/kg, respectively.{41434} It improves deficits in episodic memory induced by scopolamine (Item No. 14108) in rats and increases the time spent exploring the novel object in the novel object recognition (NOR) test when administered at a dose of 1 mg/kg. PF-04447943 (3.2 mg/kg) also improves spatial memory in the Morris water maze (MWM) and decreases the distance traveled to the hidden platform.  

 

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Description

A brain-permeable PDE inhibitor selective for PDE9A (IC50 = 12 nM) over other PDEs (IC50s = >940 nM); over 1,000-fold more selective for PDE9A over 79 non-PDE targets, with the exception of the melatonin MT3/ML2 receptor (Ki = 3,800 nM); inhibits rat and rhesus monkey PDE9A (Kis = 18.1 and 4.5 nM, respectively); increases neurite outgrowth and the density of synapsin puncta in primary rat hippocampal neurons (0.03 μM); improves scopolamine-induced deficits in episodic memory in rats and increases the time spent exploring the novel object in the NOR test (1 mg/kg); improves spatial memory in the MWM and decreases the distance traveled to the hidden platform (3.2 mg/kg)

Formal name: 1,5-dihydro-6-[(3S,4S)-4-methyl-1-(2-pyrimidinylmethyl)-3-pyrrolidinyl]-1-(tetrahydro-2H-pyran-4-yl)-4H-pyrazolo[3,4-d]pyrimidin-4-one

Synonyms: 

Molecular weight: 395.5

CAS: 1082744-20-4

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Small Molecule Inhibitors|Phosphodiesterases||Research Area|Cell Biology|Cell Signaling|cGMP Signaling||Research Area|Neuroscience|Behavioral Neuroscience|Learning & Memory

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