PF 06409577

Cat. No. 6114 1 次引用提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Potent and selective allosteric activator of AMPK

化学名： 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic acid

纯度： ≥98% (HPLC)

引用文献 (1)

通路 (1)

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 06409577

PF 06409577 is a potent and selective allosteric activator of AMPK (EC₅₀ values are 7 and >40000 nM for AMPKα1β1γ1 and AMPKα1β2γ1, respectively). Exhibits minimal off-target effects on a panel of receptors, ion channels, PDEs and kinases. Improves kidney function and reduces proteinuria in a preclinical model of diabetic nephropathy. Orally bioavailable.

许可信息

Sold for research purposes under agreement from Pfizer Inc.

化合物库 for PF 06409577

PF 06409577 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。

技术数据 for PF 06409577

分子量	341.79
公式	C₁₉H₁₆ClNO₃
储存	Store at RT
纯度	≥98% (HPLC)
CAS Number	1467057-23-3
PubChem ID	71748255
InChI Key	FHQXLWCFSUSXBF-UHFFFAOYSA-N
Smiles	O=C(O)C1=CNC2=CC(Cl)=C(C3=CC=C(C4(CCC4)O)C=C3)C=C21

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 06409577

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
	DMSO	34.18	100
	ethanol	6.84	20

制备储备液 for PF 06409577

以下数据基于产品分子量 341.79。 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.

浓度/溶剂体积/质量	1 mg	5 mg	10 mg
1 mM	2.93 mL	14.63 mL	29.26 mL
5 mM	0.59 mL	2.93 mL	5.85 mL
10 mM	0.29 mL	1.46 mL	2.93 mL
50 mM	0.06 mL	0.29 mL	0.59 mL

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产品说明书 for PF 06409577

分析证书/产品说明书

化学品安全技术说明书

参考文献 for PF 06409577

参考文献是支持产品生物活性的出版物。

Cameron et al (2016) Discovery and preclinical characterization of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic Acid (PF-06409577), a direct activator of adenosine monophosphate-activated protein kinase (AMPK), for the potential treatment of diab J.Med.Chem. 59 8068 PMID: 27490827

Salatto et al (2017) Selective activation of AMPK β1-containing isoforms improves kidney function in a rat model of diabetic nephropathy. J.Pharmacol.Exp.Ther. 361 303 PMID: 28289077

If you know of a relevant reference for PF 06409577, please let us know.

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关键词: PF 06409577, PF 06409577 supplier, PF06409577, AMP-activated, protein, kinase, AMPK, activators, activates, diabetic, nephropathy, potent, selective, allosteric, orally, bioavailable, α1β1γ1, Enzyme, Substrates, /, Activators, 6114, Tocris Bioscience

1 篇 PF 06409577 的引用文献

引用文献是使用了 Tocris 产品的出版物。 PF 06409577 的部分引用包括：

Smith et al (2019) An ErbB2/c-Src axis links bioenergetics with PRC2 translation to drive epigenetic reprogramming and mammary tumorigenesis. Nat Commun 10 2901 PMID: 31263101

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Pathways for PF 06409577

AMPK Signaling Pathway

AMPK signaling pathway plays an important role in the cellular reponse to low levels of available ATP, often caused by stresses such as heat shock, ischemia or hypoxia.