For research use only. Not for therapeutic Use.
A-769662（Cat No.:I005049）is a small molecule activator of AMP-activated protein kinase (AMPK), a key regulator of cellular energy balance. By activating AMPK, A-769662 helps to promote glucose uptake, enhance mitochondrial function, and improve fat metabolism, making it a potential candidate for treating metabolic disorders such as type 2 diabetes, obesity, and cardiovascular diseases. The compound works by directly binding to and activating the AMPK enzyme, stimulating energy production pathways. Although it shows promise in preclinical studies, further research and clinical trials are necessary to evaluate its safety and effectiveness in humans.
| Catalog Number | I005049 |
| CAS Number | 844499-71-4 |
| Synonyms | 6,7-dihydro-4-hydroxy-3-(2/’-hydroxy[1,1/’-biphenyl]-4-yl)-6-oxo-thieno[2,3-b]pyridine-5-carbonitrile |
| Molecular Formula | C20H12N2O3S |
| Purity | ≥95% |
| Target | PI3K/Akt/mTOR |
| Solubility | DMSO: ≤ 24 mg/mL |
| Storage | 3 years -20C powder |
| IC50 | 8 uM (EC50) |
| IUPAC Name | 4-hydroxy-3-[4-(2-hydroxyphenyl)phenyl]-6-oxo-7H-thieno[2,3-b]pyridine-5-carbonitrile |
| InChI | InChI=1S/C20H12N2O3S/c21-9-14-18(24)17-15(10-26-20(17)22-19(14)25)12-7-5-11(6-8-12)13-3-1-2-4-16(13)23/h1-8,10,23H,(H2,22,24,25) |
| InChIKey | CTESJDQKVOEUOY-UHFFFAOYSA-N |
| SMILES | C1=CC=C(C(=C1)C2=CC=C(C=C2)C3=CSC4=C3C(=C(C(=O)N4)C#N)O)O |
| Reference | </br>1:AMP-activated protein kinase (AMPK) activator A-769662 increases intracellular calcium and ATP release from astrocytes in an AMPK-independent manner. Vlachaki Walker JM, Robb JL, Cruz AM, Malhi A, Weightman Potter PG, Ashford MLJ, McCrimmon RJ, Ellacott KLJ, Beall C.Diabetes Obes Metab. 2017 Feb 17. doi: 10.1111/dom.12912. [Epub ahead of print] PMID: 28211632 </br>2:Effect of A-769662, a direct AMPK activator, on <i>Tlr-4</i> expression and activity in mice heart tissue. Rameshrad M, Maleki-Dizaji N, Soraya H, Toutounchi NS, Barzegari A, Garjani A.Iran J Basic Med Sci. 2016 Dec;19(12):1308-1317. doi: 10.22038/ijbms.2016.7917. PMID: 28096963 Free PMC Article</br>3:A-769662, a direct AMPK activator, attenuates lipopolysaccharide-induced acute heart and lung inflammation in rats. Rameshrad M, Soraya H, Maleki-Dizaji N, Vaez H, Garjani A.Mol Med Rep. 2016 Mar;13(3):2843-9. doi: 10.3892/mmr.2016.4821. Epub 2016 Jan 28. PMID: 26820069 </br>4:AMPK Activation by A-769662 Controls IL-6 Expression in Inflammatory Arthritis. Guma M, Wang Y, Viollet B, Liu-Bryan R.PLoS One. 2015 Oct 16;10(10):e0140452. doi: 10.1371/journal.pone.0140452. eCollection 2015. PMID: 26474486 Free PMC Article</br>5:A-769662 protects osteoblasts from hydrogen dioxide-induced apoptosis through activating of AMP-activated protein kinase (AMPK). Zhu Y, Zhou J, Ao R, Yu B.Int J Mol Sci. 2014 Jun 23;15(6):11190-203. doi: 10.3390/ijms150611190. PMID: 24960362 Free PMC Article</br>6:A-769662 potentiates the effect of other AMP-activated protein kinase activators on cardiac glucose uptake. Timmermans AD, Balteau M, Gélinas R, Renguet E, Ginion A, de Meester C, Sakamoto K, Balligand JL, Bontemps F, Vanoverschelde JL, Horman S, Beauloye C, Bertrand L.Am J Physiol Heart Circ Physiol. 2014 Jun 15;306(12):H1619-30. doi: 10.1152/ajpheart.00965.2013. Epub 2014 Apr 18. PMID: 24748590 Free Article</br>7:Small molecule drug A-769662 and AMP synergistically activate naive AMPK independent of upstream kinase signaling. Scott JW, Ling N, Issa SM, Dite TA, O/’Brien MT, Chen ZP, Galic S, Langendorf CG, Steinberg GR, Kemp BE, Oakhill JS.Chem Biol. 2014 May 22;21(5):619-27. doi: 10.1016/j.chembiol.2014.03.006. Epub 2014 Apr 17. PMID: 24746562 Free Article</br>8:AMP-activated protein kinase activator A-769662 is an inhibitor of the Na(+)-K(+)-ATPase. Benziane B, Björnholm M, Lantier L, Viollet B, Zierath JR, Chibalin AV.Am J Physiol Cell Physiol. 2009 Dec;297(6):C1554-66. doi: 10.1152/ajpcell.00010.2009. Epub 2009 Oct 14. PMID: 19828836 Free Article</br>9:A-769662 activates AMPK beta1-containing complexes but induces glucose uptake through a PI3-kinase-dependent pathway in mouse skeletal muscle. Treebak JT, Birk JB, Hansen BF, Olsen GS, Wojtaszewski JF.Am J Physiol Cell Physiol. 2009 Oct;297(4):C1041-52. doi: 10.1152/ajpcell.00051.2009. Epub 2009 Aug 5. PMID: 19657063 Free Article</br>10:Inhibitory effects of A-769662, a novel activator of AMP-activated protein kinase, on 3T3-L1 adipogenesis. Zhou Y, Wang D, Zhu Q, Gao X, Yang S, Xu A, Wu D.Biol Pharm Bull. 2009 Jun;32(6):993-8. PMID: 19483304 Free Article |
