PF-06445974
目录号 : GC69692PF-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。
Cas No.:2055776-17-3
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
PF-06445974, a promising positron emission tomograp (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].
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].
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. |
[1]. Lei Zhang,et al. The Discovery of a Novel Phosphodiesterase (PDE) 4B-Preferring Radioligand for Positron Emission Tomograp (PET) Imaging. J Med Chem.2017 Oct 26;60(20):8538-8551.
Cas No. | 2055776-17-3 | SDF | Download SDF |
分子式 | C20H15FN4O | 分子量 | 346.36 |
溶解度 | DMSO : 33.33 mg/mL (96.23 mM; ultrasonic and warming and heat to 60°C) | 储存条件 | Store at -20°C |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
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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 |
10 mM | 0.2887 mL | 1.4436 mL | 2.8872 mL |
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2.
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