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A-769662 | AMPK activator

CAS:
844499-71-4
Catalog Number:
10-1171
Activity:
AMPK activator
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
Molecular Formula:
C20H12N2O3S
Solubility:
Soluble in DMSO (up to 30 mg/ml) or in Ethanol (up to 5 mg/ml),
Physical Properties:
Beige solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT

A-769662 (844499-71-4) is a potent and reversible AMP-activated protein kinase (AMPK) allosteric activator.  Activates AMPK by binding to the β and γ subunits and not the AMP binding site.1 EC50=0.8 µM for purified rat liver AMPK and inhibits fatty acid biosynthesis in rat hepatocytes IC50=3.2 µM.2 A-769662 inhibits the rate of whole-body fatty acid oxidation, decreases body weight gain, reduces plasma and liver triglycerides and lowers plasma glucose in ob/ob mice.2 Inhibits adipocyte differentiation.3  Prevents transcriptional activation of Oct4 and establishes a metabolic barrier to induced pluripotent stem cell reprogramming.4 A-769662 synergizes with AICAR.5 Cell permeable.

References/Citations

1) Scott et al. (2008), Thienopyridone drugs are selective activators of AMP-activated protein kinase beta1-containing complexes; Cell Biol., 15 1220
2) Cool et al. (2006), Identification and characterization of a small molecule AMPK activator that treats key components of type 2 diabetes and the metabolic syndrome; Cell Metab., 3 403
3) Zhou et al. (2009), Inhibitory effects of A-769662, a novel activator of AMP-activated protein kinase on 3T3-L1 adipogenesis; Biol. Pharm. Bull., 32 993
4) Vazquez-Martin et al. (2012) Activation of AMP-activated protein kinase (AMPK) provides a metabolic barrier to reprogramming somatic cells into stem cells; Cell Cycle, 11 974
5) Ducommun et al. (2014) Enhanced activation of cellular AMPK by dual-small molecule treatment: AICAR and A769662; Am. J. Physiol. Endocrinol. Metab., 306 E688

A-769662 | AMPK activator is also available in the Cellular Metabolism Library.
CAS:
844499-71-4
Catalog Number:
10-1171
Activity:
AMPK activator
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
Molecular Formula:
C20H12N2O3S
Solubility:
Soluble in DMSO (up to 30 mg/ml) or in Ethanol (up to 5 mg/ml),
Physical Properties:
Beige solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

Product Data Sheet:

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