A 769662

A 769662
  • CAS No.:844499-71-4
Other grades of this product :
A 769662 Basic information
Product Name:A 769662
Synonyms:A 769662;4-Hydroxy-3-(2'-hydroxy-1,1'-biphenyl-4-yl)-6-oxo-6,7-dihydrothieno[2,3-b]pyridine-5-carbonitrile;4-hydroxy-3-[4-(2-hydroxyphenyl)phenyl]-6-oxo-7H-thieno[2,3-b]pyridine-5-carbonitrile;CS-18;6,7-Dihydro-4-hydroxy-3-(2'-hydroxy[1,1'-biphenyl]-4-yl)-6-oxo-thieno[2,3-b]pyridine-5-carbonitrile;Thieno[2,3-b]pyridine-5-carbonitrile, 6,7-dihydro-4-hydroxy-3-(2'-hydroxy[1,1'-biphenyl]-4-yl)-6-oxo-;A-769662/A769662;4-Hydroxy-3-(2'-hydroxy-[1,1'-biphenyl]-4-yl)-6-oxo-6,7-dihydrothieno[2,3-b]pyridine-5-carbonitri
CAS:844499-71-4
MF:C20H12N2O3S
MW:360.39
EINECS:
Product Categories:Inhibitors;Akt;Signalling;APIs;mTOR;PI3K
Mol File:844499-71-4.mol
A 769662 Chemical Properties
Melting point 263 - 266oC
Boiling point 630.1±55.0 °C(Predicted)
density 1.56
Fp 334.9℃
storage temp. Keep in dark place,Sealed in dry,Room Temperature
solubility Soluble in DMSO (up to 30 mg/ml) or in Ethanol (up to 5 mg/ml),
form solid
pka4.50±1.00(Predicted)
color Beige
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.
Safety Information
Safety Statements 24/25
HS Code 29333990
MSDS Information
A 769662 Usage And Synthesis
DescriptionA-769662 is a small molecule thienopyridone that activates AMPK directly in cell-free assays (EC50 = 116 nM) and intact cells by allosterically activating AMPK and inhibiting its dephosphorylation on Thr172. A-769662 specifically activates β1 subunit-containing AMPK heterotrimers, and its effects are independent of kinases upstream of AMPK. A-769662 has been used to stimulate CYP450-mediated fatty acid oxidation, inhibit adipocyte differentiation, explore glucose uptake in skeletal muscle, and promote endothelial cell survival during metabolic stress.
UsesA 769662 is an AMP-activated protein kinase (AMPK) activiator. A 769662 selectively activates cardiac AMPK heterotrimeric complexes contg. α2/β1-subunits.
Biological ActivityPotent, reversible AMP-activated protein kinase (AMPK) activator (EC 50 = 0.8 μ M) that displays selectivity towards β 1 subunit-containing heterotrimers. Inhibits fatty acid synthesis (IC 50 = 3.2 μ M) and decreases plasma glucose and triglyceride levels in vivo .
References1) 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 Preparation Products And Raw materials

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