|6-氯-5-(4-(1-羟基环丁基)苯基)-1H-吲哚-3-羧酸|CsnPharm

CAS No.: 1467057-23-3

PF-06409577 Catalog No. CSN22062

Synonyms: PF-6409577

PF-06409577 is a potent and selective allosteric activator of AMPK with EC50 value of 7 nM for AMPKα1β1γ1, but >40000 nM for AMPKα1β2γ1.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述In eukaryotic cells AMP-activated protein kinase (AMPK) plays a major role in regulating cellular energy balance. AMPK responds to changes in intracellular adenine nucleotide levels, being activated by an increase in AMP/ADP relative to ATP. Activation of AMPK increases the rate of catabolic (ATP-generating) pathways and decreases the rate of anabolic (ATP-utilising) pathways^[1]. PF-06409577 is a potent and selective allosteric activator of AMPK α1β1γ1 isoform with an EC₅₀ of 7 nM^[2]. In broad panel screening against other receptors, channels, PDEs and kinases, PF-06409577 exhibits minimal off-target pharmacology. PF-06409577 demonstrates moderate plasma clearance in rats, dogs, and monkeys, and is well distributed with steady state distribution volume. Following oral administration of crystalline PF-06409577 in 0.5% methylcellulose suspension, PF-06409577 is rapidly absorbed in rats, dogs, and monkeys. The corresponding oral bioavailability values in rats, dogs, and monkeys, are 15%, 100%, and 59%, respectively. Oral administration of PF-06409577 (10, 30, and 100 mg/kg QD) results in dose-dependent reductions in proteinuria in the obese ZSF1 animals, with greater than 2-fold reduction in 24-hour urinary albumin loss compared to vehicle control after 60 days of treatment^[2].
参考文献

[1] Carling D. AMPK signalling in health and disease. Curr Opin Cell Biol. 2017 Apr;45:31-37. doi: 10.1016/j.ceb.2017.01.005. Epub 2017 Feb 21. PMID: 28232179.
[2] Cameron KO, Kung DW, Kalgutkar AS, Kurumbail RG, Miller R, Salatto CT, Ward J, Withka JM, Bhattacharya SK, Boehm M, Borzilleri KA, Brown JA, Calabrese M, Caspers NL, Cokorinos E, Conn EL, Dowling MS, Edmonds DJ, Eng H, Fernando DP, Frisbie R, Hepworth D, Landro J, Mao Y, Rajamohan F, Reyes AR, Rose CR, Ryder T, Shavnya A, Smith AC, Tu M, Wolford AC, Xiao J. 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 Diabetic Nephropathy. J Med Chem. 2016 Sep 8;59(17):8068-81. doi: 10.1021/acs.jmedchem.6b00866. Epub 2016 Aug 20. PMID: 27490827.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.9258 mL
- 14.6289 mL
- 29.2579 mL
- 5 mM
- 0.5852 mL
- 2.9258 mL
- 5.8516 mL
- 10 mM
- 0.2926 mL
- 1.4629 mL
- 2.9258 mL

技术信息

CAS号

1467057-23-3

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H16ClNO3

运输

蓝冰

分子量

341.79

别名

PF-6409577

溶解度

DMSO	185.0 mg/mL (541.3 mM)
Water	insoluble

动物实验配方

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PF-06409577 Catalog No. CSN22062

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