A-769662

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A-769662 Chemical information IUPAC Nomenclature 4-hydroxy-3-(2'-hydroxybiphenyl-4-yl)-6-oxo-6,7-dihydrothieno[2,3-b]pyridine-5-carbonitrile Chemical Formula C20H12N2O3S Molecular Weight 360.39 g/mol Clinical information Clinical Usage Exercise mimetic[1] Mechanism of Action AMPK activator[2] Route of Administration Oral[1]
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A-769662 is a small-molecule chemical activator of 5' adenosine monophosphate-activated protein kinase (AMPK)^[2]. It was discovered by Cool et. al at Abbott Laboratories at Illinois, USA in 2006.

In 2008, Narkar et. al at the Salk Institute and the Howard Hughes Medical Institute at La Jolla, California would demonstrate that oral administration of 250mg/kg of a structurally-unrelated and less potent AMPK activator, AICAR, to eight-week-old male C57B/6J mice mediates a 44% increase in endurance without exercise in untrained mice.^[1]

[edit] References

1. ↑ ^{1.0 1.1 1.2} Narkar et. al (2008). AMPK and PPARδ Agonists Are Exercise Mimetics. Cell (134), 405–415.
2. ↑ ^{2.0 2.1} 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 Metabolism (3): 403–416.

Chemical Biology: Small-Molecule Control of Biological Systems (RelentlessRecusant)
Biological Targets		Compound Names
Receptor Tyrosine Kinases		A-83-01 (TGFβ/Activin) · BPIQ-II (EGFR) · Dorsomorphin/LDN-193189 (TGFβ/BMP) · SU5402 (FGFR)
Signaling Kinases		A-769662 (AMPK) · BMS-354825 (BCR-ABL, Src)· BIO-Acetoxime (GSK3) · CHIR99021 (GSK3) · GO 6976 (PKC) · IMD-0354 (IκBa) · PD184352 (MAPK) · SB203580 (MAPK) · Y-27632 (ROCK)
G Protein-Coupled Receptor		(+)-WIN-55212 (CB1/CB2) · ±-Sulpride (D2) · A 841720 (mGluR1) · BP-554 (5-HT1A) · Hh-Ag1.5 (Smo) · Cyclopamine/KAAD-Cyclopamine (Smo) · SANT1 (Smo) · SB-277011 (D3)
Ion Channels		BAY K8644 (Cav1.2) · Bicuculline (GABAAR) · Cymarin (Na+/H+) · G-strophanthin (Na+/H+) · L-AP4 (Na+/H+) · Oxcarbazepine (Na+) · Resiniferatoxin (TRPV1) · Sarmentogenin (Na+/H+) · Theanine (AMPAR, NMDAR)
Transporters		O-1783 (DAT) · WF-23 (DAT, SERT)
Nuclear Receptor		All-trans retinoic acid (RAR/RXR) · GW501516 (PPARδ) · RU-486 (Nr3c1, Nr3c3)
Protein Phosphatases		Endothall (PP2A)
Polypharmacological		Phosphoserine (mGluR4) · PK115-584 (Tcf4/β-catenin, PKC) · Pluripotin · Reversine
Other		2C-E (DAT) · 4-methoxyphenyl-HTI-286 (α/β-tubulin) · Compound E/DAPT (presenilin-1) · D-cysteine · D-phenylalanine · Flurbiprofen (COX) · JZL184 (MAGL) · QS11 (RAFGAP1) · RO-28-1675 (glucokinase) · Robotnikinin (Shh) · Selegiline (MAOB)
Uncharacterized		Neuropathiazol
Libraries		Kinase Inhibitor Library
Publications
Small molecule-mediated manipulation of the adult human induces selective and reversible control of physiological and psychological phenotype (Rubin et. al, 2590. Nature Medicine)
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