PF-05180999 (Synonyms: PF-999)
目录号: PL09695 纯度: ≥98%
CAS No. :1394033-54-5
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中文名称
PF-05180999
中文别名
化合物 T16484
英文名称
PF-05180999
英文别名
4-(1-Azetidinyl)-7-methyl-5-[1-methyl-5-[5-(trifluoromethyl)-2-pyridinyl]-1H-pyrazol-4-yl]-imidazo[5,1-f][1,2,4]triazine;PF-05180999;PF 5180999;4-(azetidin-1-yl)-7-methyl-5-{1-methyl-5-[5-(trifluoromethyl)pyridin-2-yl]-1H-pyrazol-4-yl}imidazo[5,1-f][1,2,4]triazine;Imidazo[5,1-f][1,2,4]triazine, 4-(1-azetidinyl)-7-methyl-5-[1-methyl-5-[5-(trifluoromethyl)-2-pyridinyl]-1H-pyrazol-4-yl]-;PF-05180999 >=98% (HPLC)
Cas No.
1394033-54-5
分子式
C19H17F3N8
分子量
414.39
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
PF-05180999 (PF-999) 是一种磷酸二酯酶 2A (PDE2A) 抑制剂,IC50 值为 1.6 nM。
生物活性
PF-05180999 (PF-999) is a phosphodiesterase 2A (PDE2A) inhibitor, with an IC 50 of 1.6 nM.
性状
Solid
IC50 & Target[1][2]
PDE2A 1.6 nM (IC50) PDE10A1 2.03 μM (IC
体外研究(In Vitro)
PF-05180999 is a phosphodiesterase 2A (PDE2A) inhibitor, with an IC50 of 1.6 nM. PF-05180999 binds to the rat, dog and monkey PDE2A, with Kis of 4.2, 8.4, and 5.5 nM and IC50s of 2.6, 5.2, and 3.4 nM, respectively. PF-05180999 shows 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. 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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
PF-05180999 (Compound 30; 0.032-0.32 mg/kg mg/kg, s.c.) dramatically reduces the working memory errors produced by ketamine in a working memory radial arm maze (RAM) model in rats. PF-05180999 causes 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. has not independently confirmed the accuracy of these methods. They are for reference only.
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
ClinicalTrial
参考文献
[1]. Helal CJ, et al. Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate. J Med Chem. 2018 Feb 8;61(3):1001-1018.
溶解度数据
In Vitro: DMSO : 50 mg/mL (120.66 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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