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PF-04447943

Catalog No. T16478 CAS 1082744-20-4

Synonyms: PF 04447943, Edelinontrine, PF04447943

PF-04447943 (Edelinontrine) is a potent and selective phosphodiesterase 9A inhibitor with an IC50 of 12 nM, which is 78-fold more selective than that used for other PDE family members (IC50<1000 nM).PF-04447943 exhibits anti-inflammatory activity, attenuates inflammatory responses by inhibiting oxidative stress, inflammation, and modulating T-cell polarization, and may be useful for research on sickle cell anemia.

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PF-04447943, CAS 1082744-20-4

Pack Size	Availability	Price/USD
5 mg	In stock	$ 83.00
10 mg	In stock	$ 133.00
25 mg	In stock	$ 283.00
50 mg	In stock	$ 453.00
100 mg	In stock	$ 728.00
1 mL * 10 mM (in DMSO)	In stock	$ 91.00

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Purity: 99.11%

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Description	PF-04447943 (Edelinontrine) is a potent and selective phosphodiesterase 9A inhibitor with an IC50 of 12 nM, which is 78-fold more selective than that used for other PDE family members (IC50>1000 nM).PF-04447943 exhibits anti-inflammatory activity, attenuates inflammatory responses by inhibiting oxidative stress, inflammation, and modulating T-cell polarization, and may be useful for research on sickle cell anemia.
Targets&IC50	PDE9A:12 nM
In vitro	PF-04447943 inhibits ANP (0.3 μM) stimulated cGMP (IC50: 375±36.9 nM (n=16)), in HEK whole cells expressing rhesus PDE9A2. PF-04447943 is found to be highly selective over other PDE enzymes (PDE1, Ki=8600±2121 nM, n = 5; PDE2A3, Ki>99,000 nM; PDE3A, Ki>50,000 nM; PDE4A, Ki>29,000 nM; PDE5A, Ki=14,980±5025 nM, n=5; PDE6C, Ki=5324±2612 nM, n=4; PDE7A2, Ki>75,000 nM; PDE8A, Ki>50,000 nM; PDE10, Ki>51,250±20,056 nM, n=4; PDE11, Ki>80,000 nM) and no other significant activity at ~60 other receptors/enzymes. Using recombinant human, rhesus, and rat PDE9A2 in a cell-free assay PF-04447943 is shown to have a Ki of 2.8±0.26, 4.5±0.13, and 18.1±1.9 nM (n=4, 11 and 9 respectively).[2]
In vivo	PF-04447943 concentrations dose-dependently increase in blood, brain, and cerebrospinal fluid (CSF), thirty minutes following oral administration in rats (1-30 mg/kg). In mice, PF-04447943 (3, 10, 30 mg/kg p.o.) dose-dependently enhances plasma and brain concentrations of PF-04447943 while the brain-to-plasma ratio ranged from 0.26 to 0.7 although this is not entirely dosed-dependent. Based on i.v. and p.o. dosing, pharmacokinetic studies with PF-04447943 in the rat indicate a Tmax of 0.3 h, T1/2 of 4.9 h, Cl of 21.7 mL/min/kg, and oral bioavailability of 47%. The brain: plasma exposure ratios 30 min after dosing range from 0.13 at the 1 mg/kg dose to 0.33 at the 30 mg/kg dose. CSF levels are approximately 50% of brain levels. CSF cGMP levels increase in a dose-dependent manner from a basal level of 3 pmol/mL to 13.3 pmol/mL (3.5-fold) at the 30 mg/kg dose. CSF cGMP levels also increased in a dose-dependent manner from a basal level of 3 pmol/mL in vehicle-treated animals to 13.3 pmol/mL (3.5-fold) at the 30 mg/kg dose. CSF cGMP levels are elevated at all doses tested with a maximal effect of 3.5 fold increase above controls at 30 mg/kg.[2]

Synonyms	PF 04447943, Edelinontrine, PF04447943
Molecular Weight	395.46
Formula	C20H25N7O2
CAS No.	1082744-20-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 39.55 mg/mL (100 mM), Sonication is recommended.

References and Literature

1. Kleiman RJ, et al. Phosphodiesterase 9A regulates central cGMP and modulates responses to cholinergic and monoaminergic perturbation in vivo. J Pharmacol Exp Ther. 2012 May;341(2):396-409. 2. Hutson PH, et al. The selective phosphodiesterase 9 (PDE9) inhibitor PF-04447943 (6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one) enhances synaptic plasticity and cognitive function in rodents. Neuropharmacology. 2011 Sep;61(4):665-76.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Drug Repurposing Compound Library Bioactive Compounds Library Max Bioactive Compound Library Immunology/Inflammation Compound Library Covalent Inhibitor Library

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Keywords

PF-04447943 1082744-20-4 Metabolism PDE PF 04447943 Edelinontrine PF04447943 inhibitor inhibit

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