Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PF-05180999 is an inhibitor of phosphodiesterase 2A (IC50: 1.6 nM).
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 484 | 5日内发货 | ||
5 mg | ¥ 792 | 8-10周 | ||
100 mg | ¥ 7,320 | 8-10周 |
产品描述 | PF-05180999 is an inhibitor of phosphodiesterase 2A (IC50: 1.6 nM). |
靶点活性 | PDE11A4:26.969 μM, PDE7B:50.09 μM, PDE2A:1.6 nM, PDE10A1:2.03 μM |
体外活性 | PF-05180999 is also a weak inducer of CYP3A4, and with no direct inhibition of human recombinant cytochrome P450 (CYP) enzymes (1A2, 2B6, 2C8, 2C9, 2C19, 2D6, and 3A) and no induction of CYP1A2. PF-05180999 binds to the rat, dog and monkey PDE2A (Kis: 4.2, 8.4, and 5.5 nM and IC50s: 2.6, 5.2, and 3.4 nM, respectively). PF-05180999 displays weak activity against PDE, with IC50s of 2.03 μM (PDE10A1), 26.969 μM (PDE7B), 50.09 μM (PDE11A4), and >56.25 μM (PDE1B1, PDE3A1, PDE4D3, PDE5A1, PDE6 (bovine), PDE8B, PDE9A1), respectively [1]. |
体内活性 | PF-05180999 induces acute and exposure-dependent elevation in the accumulation of cGMP bulk levels in the cortex, striatum, and hippocampus, but with no changes in cAMP and the associated downstream phospho-cAMP response element-binding protein (p-CREB) in mice. PF-05180999 (0.032-0.32 mg/kg mg/kg, s.c.) dramatically decreases the working memory errors produced by ketamine in a working memory radial arm maze (RAM) model in rats [1]. |
分子量 | 414.39 |
分子式 | C19H17F3N8 |
CAS No. | 1394033-54-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (120.66 mM), sonification is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.4132 mL | 12.0659 mL | 24.1319 mL | 60.3296 mL |
5 mM | 0.4826 mL | 2.4132 mL | 4.8264 mL | 12.0659 mL | |
10 mM | 0.2413 mL | 1.2066 mL | 2.4132 mL | 6.033 mL | |
20 mM | 0.1207 mL | 0.6033 mL | 1.2066 mL | 3.0165 mL | |
50 mM | 0.0483 mL | 0.2413 mL | 0.4826 mL | 1.2066 mL | |
100 mM | 0.0241 mL | 0.1207 mL | 0.2413 mL | 0.6033 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
PF-05180999 1394033-54-5 Metabolism PDE PF05180999 PF 05180999 Inhibitor inhibitor inhibit