产品
编 号：F252516
分子式：C20H15FN4O
分子量：346.36
分子式：C20H15FN4O
分子量：346.36
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
结构图
CAS No: 2055776-17-3
产品详情
生物活性：
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.
体内研究：
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.Animal Model:Twenty-five drug-naive male 129/B6 PDE4D KO mice (25-35 g)
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.
体外研究：
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).
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.
体内研究：
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.Animal Model:Twenty-five drug-naive male 129/B6 PDE4D KO mice (25-35 g)
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.
体外研究：
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).
产品资料
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