PF-06445974
Based on 1 Customer Validation
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.
- Purity : 98.59%
- CAS No.: 2055776-17-3
- Formula: C20H15FN4O
- Molecular Weight:346.36
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
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. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Twenty-five drug-naive male 129/B6 PDE4D KO mice (25-35 g)[1]
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Dosage:10 µg/kg
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Administration:Dosed intravenously at 10 µg/kg in a 5 mL/kg dosing volume
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Result:Showed excellent brain uptake and reached peak concentrations at around 20 minutes.
Chemical Information
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CAS No. 2055776-17-3
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Appearance Solid
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Molecular Weight 346.36
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Formula C20H15FN4O
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Color White to off-white
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SMILES
N#CC1=CC=C(C=C1F)C2=C(C3=O)N(CCN3C4CC4)C5=CC=CN=C25
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Shipping
Room temperature in continental US; may vary elsewhere.
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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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Transepithelial/transendothelial electrical resistance assay
TEER measures electrical resistance across epithelial or endothelial monolayers cultured on permeable supports, and the readout reflects ionic conductance through the cell barrier, especially the paracellular pathway regulated by junctional integrity. TEER can be measured without destroying the monolayer and is commonly used before or during transport, permeability, barrier-disruption, and barrier-maturation experiments. TEER values are influenced by biological maturation and technical conditions; reported factors include temperature, medium formulation, passage number, electrode geometry, membrane properties, and junctional length during early monolayer maturation. Therefore, TEER should be interpreted with blank-insert subtraction, area normalization, repeated readings, and, when possible, orthogonal barrier readouts such as FITC-dextran flux or tight-junction staining.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
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 |
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| 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 |
PF-06445974 Related Classifications
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