PF-06445974,2055776-17-3

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PF-06445974

CAS No. : 2055776-17-3

MCE 国际站：PF-06445974

产品活性：PF-06445974 是一种正电子发射断层扫描 (PET) 化合物，有效作用于 PDE4B，IC₅₀ <1 nM。对 PDE4D、PDE4A 和 PDE4C 的 IC₅₀ 值分别为 36、4.7 和 17 nM。PF-06445974 对 PDE4D 具有良好的选择性，出色的脑通透性，在 “冷示踪剂” 研究中能够高水平特异性结合。

研究领域：Metabolic Enzyme/Protease

作用靶点：Phosphodiesterase (PDE)

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 (K_i=3850 nM).

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.

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