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

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.

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PF-06445974 Chemical Structure

PF-06445974 Chemical Structure

CAS No. : 2055776-17-3

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Based on 1 publication(s) in Google Scholar

PF-06445974 Related Antibodies

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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].

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

PF-06445974 Related Antibodies
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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (96.23 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8872 mL 14.4358 mL 28.8717 mL
5 mM 0.5774 mL 2.8872 mL 5.7743 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8872 mL 14.4358 mL 28.8717 mL 72.1792 mL
5 mM 0.5774 mL 2.8872 mL 5.7743 mL 14.4358 mL
10 mM 0.2887 mL 1.4436 mL 2.8872 mL 7.2179 mL
15 mM 0.1925 mL 0.9624 mL 1.9248 mL 4.8119 mL
20 mM 0.1444 mL 0.7218 mL 1.4436 mL 3.6090 mL
25 mM 0.1155 mL 0.5774 mL 1.1549 mL 2.8872 mL
30 mM 0.0962 mL 0.4812 mL 0.9624 mL 2.4060 mL
40 mM 0.0722 mL 0.3609 mL 0.7218 mL 1.8045 mL
50 mM 0.0577 mL 0.2887 mL 0.5774 mL 1.4436 mL
60 mM 0.0481 mL 0.2406 mL 0.4812 mL 1.2030 mL
80 mM 0.0361 mL 0.1804 mL 0.3609 mL 0.9022 mL
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PF-06445974 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PF-064459742055776-17-3PF06445974PF 06445974Phosphodiesterase (PDE)positronemissiontomographyPETPDE4BInhibitorinhibitorinhibit

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