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PF 04449613

Cat. No. 5915 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Potent PDE9 inhibitor; brain penetrant
别名： PF 9613
化学名： 1,5-Dihydro-6-[(1R)-1-(3-phenoxy-1-azetidinyl)ethyl]-1-(tetrahydro-2H-pyran-4-yl)-4H-pyrazolo[3,4-d]pyrimidin-4-one
纯度： ≥98% (HPLC)
说明书
引用文献
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生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for PF 04449613

PF 04449613 is a potent PDE9 inhibitor (IC50 = 22 nM). PF 4449613 shows more than 1000-fold selectivity for PDE9A over most of 79 other non-PDE targets investigated, except for cytochrome P450 2C19 (IC50 = 1600 nM), dopamine transporter (Ki = 110 nM), μ-opioid receptor (Ki =3500 nM), and sodium channel binding site 2 (Ki =470 nM). PF 04449613 reduces body fat in mice with diet-induced obesity, stimulating mitochondrial activity in brown and white fat, and improving cardiometabolic syndrome symptoms. Brain penetrant. PF 04449613 increases synaptic calcium activity and learning-dependent synaptic plasticity in mice.

许可信息

Sold for research purposes under agreement from Pfizer Inc.

化合物库 for PF 04449613

PF 04449613 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。

技术数据 for PF 04449613

分子量 395.45
公式 C21H25N5O3
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 1236858-52-8
PubChem ID 46851937
InChI Key WEDCMPMDOVEMSV-CQSZACIVSA-N
Smiles C[C@H](C1=NC(C2=C(N(C3CCOCC3)N=C2)N1)=O)N4CC(OC5=CC=CC=C5)C4

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for PF 04449613

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 39.55 100

制备储备液 for PF 04449613

以下数据基于产品分子量 395.45。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 2.53 mL 12.64 mL 25.29 mL
5 mM 0.51 mL 2.53 mL 5.06 mL
10 mM 0.25 mL 1.26 mL 2.53 mL
50 mM 0.05 mL 0.25 mL 0.51 mL

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产品说明书 for PF 04449613

分析证书/产品说明书
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化学品安全技术说明书

参考文献 for PF 04449613

参考文献是支持产品生物活性的出版物。

Kleiman et al (2012) Phosphodiesterase 9A regulates central cGMP and modulates responses to cholinergic and monoaminergic perturbation in vivo. J.Pharmacol.Exp.Ther. 341 396 PMID: 22328573

Lee et al (2015) Phosphodiesterase 9A controls nitric-oxide-independent cGMP and hypertrophic heart disease. Nature 519 472 PMID: 25799991

Claffey et al (2012) Application of structure-based drug design and parallel chemistry to identify selective, brain penetrant, in vivo active phosphodiesterase 9A inhibitors. J.Med.Chem. 55 9055 PMID: 23025719

Mishra et al (2021) Inhibition of phosphodiesterase type 9 reduces obesity and cardiometabolic syndrome in mice. J.Clin.Invest. 131 e148798 PMID: 34618683

Lai et al (2018) The phosphodiesterase 9 inhibitor PF-04449613 promotes dendritic spine formation and performance improvement after motor learning. Dev.Neurobiol. 78 859 PMID: 30022611

If you know of a relevant reference for PF 04449613, please let us know.

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关键词: PF 04449613, PF 04449613 supplier, PF04449613, PF9613, phosphodiesterases, PDE, A, inhibitors, inhibits, potent, Schizophrenia, Alzheimer's, disease, brain, penetrant, PF, 9613, Phosphodiesterases, 5915, Tocris Bioscience

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