PF-06445974|cas:2055776-17-3|西域试剂

PF-06445974,98.23%

产品编号：Bellancom-119190| CAS NO：2055776-17-3| 分子式：C₂₀H₁₅FN₄O| 分子量：346.36

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货号	价格	库存与货期
Bellancom-119190	￥2500.00	杭州北京（现货）
Bellancom-119190	￥4000.00	杭州北京（现货）
Bellancom-119190	￥8500.00	杭州北京（现货）
Bellancom-119190	￥13500.00	杭州北京（现货）

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PF-06445974

产品介绍

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。

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 (K_i=3850 nM).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.