PF 04449613

Key Product Details

Product Description

PF 04449613 is a potent PDE9 inhibitor (IC₅₀ = 22 nM). PF 4449613 shows more than 1000-fold selectivity for PDE9A over most of 79 other non-PDE targets investigated, except for cytochrome P450 2C19 (IC₅₀ = 1600 nM), dopamine transporter (K_i = 110 nM), μ-opioid receptor (K_i =3500 nM), and sodium channel binding site 2 (K_i =470 nM). PF 04449613 reduces body fat in mice with diet-induced obesity, stimulating mitochondrial activity in brown and white fat, and improving cardiometabolic syndrome symptoms. Brain penetrant. PF 04449613 increases synaptic calcium activity and learning-dependent synaptic plasticity in mice.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Product Specifications for PF 04449613

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for PF 04449613

The following data is based on the product molecular weight 395.45.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.53 mL	12.64 mL	25.29 mL
5 mM	0.51 mL	2.53 mL	5.06 mL
10 mM	0.25 mL	1.26 mL	2.53 mL
50 mM	0.05 mL	0.25 mL	0.51 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Lai The phosphodiesterase 9 inhibitor PF-04449613 promotes dendritic spine formation and performance improvement after motor learning. Dev.Neurobiol. 2018 PMID: 30022611
• Mishra Inhibition of phosphodiesterase type 9 reduces obesity and cardiometabolic syndrome in mice. J.Clin.Invest. 2021 PMID: 34618683
• Lee Phosphodiesterase 9A controls nitric-oxide-independent cGMP and hypertrophic heart disease. Nature 2015 PMID: 25799991
• Claffey Application of structure-based drug design and parallel chemistry to identify selective, brain penetrant, in vivo active phosphodiesterase 9A inhibitors. J.Med.Chem. 2012 PMID: 23025719
• Kleiman Phosphodiesterase 9A regulates central cGMP and modulates responses to cholinergic and monoaminergic perturbation in vivo. J.Pharmacol.Exp.Ther. 2012 PMID: 22328573

Product Documents for PF 04449613