PF-05085727

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PF-05085727

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1415637-72-7

PF-05085727 是一种强效的 cGMP 依赖性的PDE2A(IC₅₀=2 nM) 选择性和具有脑通透性的抑制剂。PF-05085727 对 PDE2A 的选择性是 PDE1 和 PDE3-11 的 4000 倍。

生物活性

PF-05085727 is a potent, selective and brain penetrant inhibitor of cGMP-dependentPDE2A(IC₅₀=2 nM). PF-05085727 inhibits PDE2A >4,000-fold selectivity overPDE1and PDE3-11^[1].

IC₅₀& Target^[1]

PDE2A

2 nM (IC₅₀)

体外研究
(In Vitro)

PF-05085727 shows weak activity with IC₅₀ of 162 μM to induce cell death in a cellular toxicity assay using transformed human liver endothelial (THLE) cells^[1].
PF-05085727 (3 μM) shows a minimal inhibition of cytochrome P450 enzymes (CYPs), inhibits 1A2, 2C8, 2C9, 2D6 and 3A4 with percentage% of 16%, 18%, 7%, 4%, and 30%, respectively^[1].
PF-05085727 (10 μM) inhibits PDE1B, PDE4B, PDE7B and PDE10A with IC₅₀values of 12.146 μM, 22,503 μM, 13.157 μM and 6.515 μM, respectively^[1].

体内研究
(In Vivo)

PF-05085727 (subcutaneous injection; 3.2 mg/kg/mice; 3 mg/kg/rat) gives a ratio of unbound brain (C_bu) to unbound plasma (C_pu) of ca. 0.27 and 0.37, respectively^[1].
PF-05085727 in mice leads to an acute and exposure-dependent elevation in the accumulation of bulk levels of cGMP in cortex, striatum, and hippocampus as measured by enzyme-linked immunosorbent assay^[1].

分子量

413.40

性状

Solid

Formula

C₂₀H₁₈F₃N₇

CAS 号

1415637-72-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 62.5 mg/mL(151.19 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.4190 mL	12.0948 mL	24.1896 mL
5 mM	0.4838 mL	2.4190 mL	4.8379 mL
10 mM	0.2419 mL	1.2095 mL	2.4190 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。