產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 10mg 25mg 50mg
CAS	844499-71-4
別名	A-769662;A769662
化學(xué)名	4-hydroxy-3-[4-(2-hydroxyphenyl)phenyl]-6-oxo-7H-thieno[2,3-b]pyridine-5-carbonitrile
分子式	C20H12N2O3S
分子量	360.39
溶解度	≥ 18.0195 mg/mL in DMSO
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

A-769662 is a potent activator of AMPK with EC50 value of 0.8 μM in vitro[1].

AMPK(AMP-activated protein kinase) is a serine/threonine protein kinase which is formed by three proteins: α,β and γ subunits. They play important roles in both the activity and stabilities of AMPK. AMPK functions as sensors of cellular energy by detecting and reacting to the change of AMP: ATP ratio. AMPK plays an important role in regulating intracellular energy metabolism. AMPK inhibits ATP-consuming pathways containing cholesterol synthesis, fatty acid synthesisand gluconeogenesis. AMPK stimulates fatty acid oxidation and glycolysis which are ATP-generating processes. AMPK inhibits gluconeogenesis by suppressing the expression of glucose-6-phosphatase and PEPCK wich are two key gluconeogenic enzymes.[1]

A-769662 belongs to the thienopyridone family. It activates the activity of purified AMPK from diffrent tissues with a dose-dependent manner. A-769662 activated the activity of AMPK extracted from human embryonic kidney cells (HEKs), rat muscle, or rat heart with EC50 values of 1.1 mM, 1.9 mM, or 2.2mM, respectively. A-769662 inhibited the synthesis of fatty acid with IC50 value of 3.2mM in primary rat hepatocytes.[1] A769662 also has inhibition effect on the 26S proteasome with an AMPK-independent mechanism. A769662 does not inhibit the proteolytic activities of the 20S core subunit which is a novel mechanism. A769662 can cause the arrest of cell cycle by inhibiting the 26S proteasome[2]. A-769662 activates AMPK in an allosterically manner. It also inhibits Thr-172 dephosphorylation of AMPK.[3]

In mice treated with dose of 30mg/kg, A-769662 decreased the expression of FAS, G6Pase, and PEPCK in liver of. It also lowered plasma glucose by 40% and reduced body weight gain.[1]

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1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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