PF 04449613

Name: PF 04449613
Brand: Tocris Bioscience
SKU: 5915

Tocris Bioscience, part of Bio-Techne | Catalog # 5915

COA / SDS

Potent PDE9 inhibitor; brain penetrant

Key Product Details

Description:	Potent PDE9 inhibitor; brain penetrant
Alternative Names:	PF 9613
Chemical Name:	1,5-Dihydro-6-[(1R)-1-(3-phenoxy-1-azetidinyl)ethyl]-1-(tetrahydro-2H-pyran-4-yl)-4H-pyrazolo[3,4-d]pyrimidin-4-one
Purity:	≥98% (HPLC)
Molecular Weight:	395.45

View Full Technical Details for PF 04449613

Technical Data
Citations

Biological Activity for PF 04449613

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.

Compound Libraries for PF 04449613

PF 04449613 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for PF 04449613

M. Wt	395.45
Formula	C₂₁H₂₅N₅O₃
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1236858-52-8
PubChem ID	46851937
InChi Key	WEDCMPMDOVEMSV-CQSZACIVSA-N
Smiles	C[C@H](C1=NC(C2=C(N(C3CCOCC3)N=C2)N1)=O)N4CC(OC5=CC=CC=C5)C4

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

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for PF 04449613

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	39.55	100

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 will affect the solvent volumes required to prepare stock solutions.

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

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References for PF 04449613

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