PF-04447943|cas:1082744-20-4|西域试剂

PF-04447943,98.74%

产品编号：Bellancom-15441| CAS NO：1082744-20-4| 分子式：C₂₀H₂₅N₇O₂| 分子量：395.46

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-15441	￥1950.00	杭州北京（现货）
Bellancom-15441	￥3150.00	杭州北京（现货）
Bellancom-15441	￥6600.00	杭州北京（现货）
Bellancom-15441	￥11000.00	杭州北京（现货）

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PF-04447943

产品介绍

PF-04447943 是一种有效的人重组 PDE9A 抑制剂，IC₅₀ 为 12 nM，比作用于其他PDE家族成员选择性高 78 倍 (IC₅₀>1000 nM)。

生物活性

PF-04447943 is a potent inhibitor of human recombinant PDE9A (IC₅₀=12 nM) with >78-fold selectivity, respectively, over other PDE family members (IC₅₀>1000 nM).

体外研究

Using recombinant human, rhesus, and rat PDE9A2 in a cell free assay PF-04447943 is shown to have a K_i of 2.8±0.26, 4.5±0.13, and 18.1±1.9 nM (n=4, 11 and 9 respectively). PF-04447943 is found to be highly selective over other PDE enzymes (PDE1, K_i=8600±2121 nM, n = 5; PDE2A3, K_i>99,000 nM; PDE3A, K_i>50,000 nM; PDE4A, K_i>29,000 nM; PDE5A, K_i=14,980±5025 nM, n=5; PDE6C, K_i=5324±2612 nM, n=4; PDE7A2, K_i>75,000 nM; PDE8A, K_i>50,000 nM; PDE10, K_i>51,250±20,056 nM, n=4; PDE11, K_i>80,000 nM) and no other significant activity at ~60 other receptors/enzymes. In HEK whole cells expressing rhesus PDE9A2, PF-04447943 inhibits ANP (0.3 μM) stimulated cGMP with an IC₅₀ of 375±36.9 nM (n=16).

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

体内研究

Based on i.v. and p.o. dosing, pharmacokinetic studies with PF-04447943 in the rat indicates a T_max of 0.3 h, T_1/2 of 4.9 h, Cl of 21.7 mL/min/kg and an oral bioavailability of 47%. Thirty minutes following oral administration in rats (1-30 mg/kg), PF-04447943 concentrations dose-dependently increase in blood, brain and cerebrospinal fluid (CSF). The brain:plasma exposure ratios 30 min after dosing range from 0.13 at the 1 mg/kg dose to 0.33 at the 30 mg/kg dose. CSF levels are approximately 50% of brain levels. In mice, PF-04447943 (3, 10, 30 mg/kg p.o.) dose-dependently increases plasma and brain concentrations of PF-04447943 while the brain to plasma ratio ranged from 0.26 to 0.7 although this is not entirely dose dependent. CSF cGMP levels increase in a dose-dependent manner from a basal level of 3 pmol/mL to 13.3 pmol/mL (3.5-fold) at the 30 mg/kg dose. CSF cGMP levels also increase in a dose-dependent manner from a basal level of 3 pmol/mL in vehicle treated animals to 13.3 pmol/mL (3.5-fold) at the 30 mg/kg dose. CSF cGMP levels are elevated at all doses tested with a maximal effect of 3.5 fold increase above controls at 30 mg/kg.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 54.6 mg/mL (138.07 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5287 mL	12.6435 mL	25.2870 mL
5 mM	0.5057 mL	2.5287 mL	5.0574 mL
10 mM	0.2529 mL	1.2644 mL	2.5287 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (6.32 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.32 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.32 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.32 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.32 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.32 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。