1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. PF-06445974

PF-06445974 

Cat. No.: HY-119190
Handling Instructions

PF-06445974, a promising positron emission tomography (PET) lead, has exquisite potency at PDE4B with an IC50 <1 nM. The IC50 values are 36, 4.7 and 17 nM for PDE4D, PDE4A and PDE4C, respectively. PF-06445974 has good selectivity over PDE4D, excellent brain permeability, and a high level of specific binding in the "cold tracer" study.

For research use only. We do not sell to patients.

PF-06445974 Chemical Structure

PF-06445974 Chemical Structure

CAS No. : 2055776-17-3

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Description

PF-06445974, a promising positron emission tomography (PET) lead, has exquisite potency at PDE4B with an IC50 <1 nM. The IC50 values are 36, 4.7 and 17 nM for PDE4D, PDE4A and PDE4C, respectively. PF-06445974 has good selectivity over PDE4D, excellent brain permeability, and a high level of specific binding in the "cold tracer" study[1].

IC50 & Target[1]

PDE4B

<1 nM (IC50)

PDE4D

36 nM (IC50)

PDE4A

4.7 nM (IC50)

PDE4C

17 nM (IC50)

In Vitro

PF-06445974 demonstrates minimal off-target activities in broad-spectrum selectivity panels, with only weak µM activities at PDE10 (IC50=2290 nM), PDE5A (IC50=4640 nM) and GABAA (Ki=3850 nM)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PF-06445974 exhibits high central nervous system (CNS) PET MPO score (4.0). PF-06445974 is a promising radiotracer lead for specific binding assessment. Neuropharmacokinetic study in rats (0.1 mg/kg, IV) confirms high brain permeability with a total brain to plasma ratio of 0.76, corresponding to a free brain to plasma ratio of 0.70[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Twenty-five drug-naive male 129/B6 PDE4D KO mice (25-35 g)[1]
Dosage: 10 µg/kg
Administration: Dosed intravenously at 10 µg/kg in a 5 mL/kg dosing volume
Result: Showed excellent brain uptake and reached peak concentrations at around 20 minutes.
Molecular Weight

346.36

Formula

C20H15FN4O

CAS No.
SMILES

N#CC1=CC=C(C=C1F)C2=C(C3=O)N(CCN3C4CC4)C5=CC=CN=C25

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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PF-06445974
Cat. No.:
HY-119190
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