2055776-17-3
2055776-17-3 structure
- Name: PF-06445974
- Chemical Name: PF-06445974
- CAS Number: 2055776-17-3
- Molecular Formula: C20H15FN4O
- Molecular Weight: 346.36
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Phosphodiesterase (PDE)
- Create Date: 2022-03-10 18:15:34
- Modify Date: 2024-04-03 18:17:07
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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].
| Name | PF-06445974 |
|---|
| 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]. |
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| Related Catalog | |
| Target |
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]. |
| 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]. 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. |
| References |
| Molecular Formula | C20H15FN4O |
|---|---|
| Molecular Weight | 346.36 |