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A769662,AMPKActivator

品牌：Xcessbio

货号：M60020-5s

规格：5 mg solid

货期：

应用：

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A769662,AMPKActivator

商品详情参考文献相关资料

Product Information

Chemical Name:	4-hydroxy-3-(2'-hydroxy-[1,1'-biphenyl]-4-yl)-6-oxo-6,7-dihydrothieno[2,3-b]pyridine-5-carbonitrile
Molecular Weight:	360.39
Formula:	C₂₀H₁₂N₂O₃S
Purity:	≥ 98%
CAS#:	844499-71-4
Solubility:	DMSO up to 50 mM
Storage:	Powder: 4^oC 1 year DMSO: 4^oC 3 month -20^oC 1 year

Biological Activity:

A769662 is a potent and selective small-molecule activator of AMP-activated protein kinase (AMPK). It induces allosteric activation of AMPK and inhibition of dephosphorylation of AMPK on Thr-172, similar to the effects of AMP. The activation of AMPK inhibits mTOR signaling, which is a positive effector of cell growth and survival. A769662 stimulated partially purified rat liver AMPK with an EC₅₀ of 0.8 µM and inhibited fatty acid synthesis in primary rat hepatocytes with an IC₅₀ of 3.2 µM. It can also stimulate Na+,K+-ATPase activity in skeletal muscle cells.

How to Use:

In vitro: A769662 is typically used at 10-20 µM concentration in vitro.

In vivo: A769662 could be intraperitoneally (IP) dosed to mice at 30 mg/kg twice per day.

Reference:

1. Cool B, et al. Identification and characterization of a small molecule AMPK activator that treats key components of type 2 diabetes and the metabolic syndrome. (2006) Cell Metab. 3: 403-416.
2. Scott JW, et al. Thienopyridone drugs are selective activators of AMP-activated protein kinase β1-containing complexes. (2008) Chem. Biol. 15: 1220-1230.
3. Huang X, et al. Important role of the LKB1-AMPK pathway in suppressing tumorigenesis in PTEN-deficient mice. (2008) Biochem J. 412:211-221.
4. Morizane Y, et al. AMP-activated protein kinase suppresses matrix metalloproteinase-9 expression in mouse embryonic fibroblasts. (2011) J Biol Chem. 286(18):16030-8.
5. Benziane B, et al. Activation of AMP-activated protein kinase stimulates Na+,K+-ATPase activity in skeletal muscle cells. (2012) J Biol Chem.287(28):23451-63.

Products are for research use only. Not for human use.

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