2. Academic Validation
  3. Identification and characterization of a small molecule AMPK activator that treats key components of type 2 diabetes and the metabolic syndrome

Identification and characterization of a small molecule AMPK activator that treats key components of type 2 diabetes and the metabolic syndrome

  • Cell Metab. 2006 Jun;3(6):403-16. doi: 10.1016/j.cmet.2006.05.005.
Barbara Cool 1,  Bradley Zinker,  William Chiou,  Lemma Kifle,  Ning Cao,  Matthew Perham,  Robert Dickinson,  Andrew Adler,  Gerard Gagne,  Rajesh Iyengar,  Gang Zhao,  Kennan Marsh,  Philip Kym,  Paul Jung,  Heidi S Camp,  Ernst Frevert
Affiliations

Affiliation

  • 1 Department of Metabolic Disease Research, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064, USA. barbara.l.cool@abbott.com
PMID: 16753576 DOI: 10.1016/j.cmet.2006.05.005
Abstract

AMP-activated protein kinase (AMPK) is a key sensor and regulator of intracellular and whole-body energy metabolism. We have identified a thienopyridone family of AMPK activators. A-769662 directly stimulated partially purified rat liver AMPK (EC50 = 0.8 microM) and inhibited fatty acid synthesis in primary rat hepatocytes (IC50 = 3.2 microM). Short-term treatment of normal Sprague Dawley rats with A-769662 decreased liver malonyl CoA levels and the respiratory exchange ratio, VCO2/VO2, indicating an increased rate of whole-body fatty acid oxidation. Treatment of ob/ob mice with 30 mg/kg b.i.d. A-769662 decreased hepatic expression of PEPCK, G6Pase, and FAS, lowered plasma glucose by 40%, reduced body weight gain and significantly decreased both plasma and liver triglyceride levels. These results demonstrate that small molecule-mediated activation of AMPK in vivo is feasible and represents a promising approach for the treatment of type 2 diabetes and the metabolic syndrome.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-50662
    99.20%, AMPK激动剂
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z