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.
CAS Number: 844499-71-4
Molecular Weight: 360.39
Chemical Name: 4-hydroxy-3-(2'-hydroxy-[1,1'-biphenyl]-4-yl)-6-oxo-6,7-dihydrothieno[2,3-b]pyridine-5-carbonitrile
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 50 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
A769662 is typically used at 10-20 µM concentration in vitro.
A769662 could be intraperitoneally (IP) dosed to mice at 30 mg/kg twice per day.
- 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.
- Scott JW, et al. Thienopyridone drugs are selective activators of AMP-activated protein kinase β1-containing complexes. (2008)? Chem. Biol. 15: 1220-1230.
- Huang X, et al. Important role of the LKB1-AMPK pathway in suppressing tumorigenesis in PTEN-deficient mice. (2008) Biochem J. 412:211-221.
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