Mardepodect (Synonyms: PF-2545920)
目录号: PL09701 纯度: ≥99%
CAS No. :898562-94-2
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中文名称
Mardepodect
中文别名
2-[[4-[1-甲基-4-(4-吡啶基)-1H-吡唑-3-基]苯氧基]甲基]-喹啉;2-[(4-(1-甲基-4-(吡啶-4-基)-1H-吡唑-3-基)苯氧基)甲基]喹啉
英文名称
Mardepodect
英文别名
2-((4-(1-Methyl-4-(pyridin-4-yl)-1H-pyrazol-3-yl)phenoxy)methyl)quinoline;2-[(4-(1-Methyl-4-(pyridin-4-yl)-1H-pyrazol-3-yl)phenoxy)methyl]quinoline;2-[(4-(1-Methyl-4-(pyridin-4-yl)-1H-pyrazol-3-yl)phexy)methyl]quiline;PF-2545920;Quinoline, 2-[[4-[1-methyl-4-(4-pyridinyl)-1H-pyrazol-3-yl]phenoxy]methyl]-;MP 10;Mardepodect;2-[[4-[1-Methyl-4-(4-pyridinyl)-1H-pyrazol-3-yl]phenoxy]methyl]quinoline (ACI);PF 02545920;PF 2545920
Cas No.
898562-94-2
分子式
C25H20N4O
分子量
392.45
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Mardepodect (PF-2545920) 是一种有效的,口服活性的,选择性的 PDE10A 抑制剂,IC50 为 0.37 nM,比作用于其他 PDE 选择性高 1000 多倍。Mardepodect 可穿过血脑屏障。
生物活性
Mardepodect (PF-2545920) is a potent, orally active and selective PDE10A inhibitor with an IC 50 of 0.37 nM, with >1000-fold selectivity over other PDEs. Mardepodect can cross the blood-brain barrier.
性状
Solid
体内研究(In Vivo)
In the conditioned avoidance response assay (CAR), Mardepodect (PF-2545920) is active with an ED 50 of 1 mg/kg. Administration of Mardepodect (PF-2545920) to mice causes a dose dependent increase in striatal cGMP. 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]. Verhoest PR, et al. Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. J Med Chem
[2]. Grauer SM, et al. Phosphodiesterase 10A inhibitor activity in preclinical models of the positive, cognitive, and negative symptoms of schizophrenia. J Pharmacol Exp Ther, 2009, 331(2), 574-590.
溶解度数据
In Vitro: DMSO : ≥ 45 mg/mL (114.66 mM)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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