A-769662 An AMPK activator which induces PI3-kinase-dependent glucose uptake

A-769662 (CAS 844499-71-4)

A-769662 | CAS 844499-71-4 is rated 5.0 out of 5 by 2.
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Synonym: 6,7-Dihydro-4-hydroxy-3-(2'-hydroxy[1,1'-biphenyl]-4-yl)-6-oxo-thieno[2,3-b]pyridine-5-carbonitrile
Application: An AMPK activator which induces PI3-kinase-dependent glucose uptake
CAS Number: 844499-71-4
Purity: ≥98%
Molecular Weight: 360.39
Molecular Formula: C20H12N2O3S
* Refer to Certificate of Analysis for lot specific data (including water content).
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A-769662 is an AMP-activated protein kinase (AMPK) activator that mimics the function of AMP on AMPK β-1 by allosteric activation and the inhibition of dephosphorylation of AMPK. In the presence of both LKB1 and A-769662 the phosphorylation of AMPK is suppressed. In addition, A-769662 is not effected by upstream kinases such as calmodulin-dependent protein kinase kinase-β when phosphorylating AMPK β-1. In vitro tests indicate A-769662 suppresses the activity of Sodium-Potassium Adenosine Triphosphatase by inhibiting the α(1)-isoform of the pump and decreasing the cell surface abundance of the protein complex in skeletal muscle cells. A-769662 thereby induces glucose uptake through a PI3-kinase-dependent pathway.


References

1. Göransson, O., et al. 2007. J. Biol. Chem. 282: 32549-32560. PMID: 17855357
2. Treebak, J.T., et al. 2009. Am. J. Physiol. Cell Physiol. 297: 1041-1052. PMID: 19657063
3. Benziane, B., et al. 2009. Am. J. Physiol. Cell Physiol. 297: 1554-1566. PMID: 19828836
4. Rajamohan, F., et al. 2010. Protein Expr. Purif. 73: 189-197. PMID: 20451617

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM), ethanol (10 mM), DMF (~0.5 mg/ml), 1: 1 DMSO:PBS(pH 7.2) (~0.5 mg/ml), and water (<1 mg/ml at 25° C).
Storage :
Store at 4° C
Melting Point :
268.39° C (Predicted)
Boiling Point :
630.08° C at 760 mmHg (Predicted)
Density :
1.56 g/cm3 (Predicted)
Refractive Index :
n20D 1.78 (Predicted)
IC50 :
AMP-activated protein kinase: EC5050 = 0.8 µM; Fatty acid synthesis: IC50 = 3.2 µM (rat); Fatty acid synthesis: IC50 = 3.6 µM (mouse)
pK Values :
pKa: 4.5 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
54708532
MDL Number :
MFCD11977269
SMILES :
C1=CC=C(C(=C1)C2=CC=C(C=C2)C3=CSC4=C3C(=C(C(=O)N4)C#N)O)O

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A-769662  Product Citations

See how others have used A-769662. Click on the entry to view the PubMed entry .

Citations 1 to 9 of 9 total

PMID: # 27128383  Schmitt, DL. et al. 2016. ACS chemical biology.

PMID: # 26297684  Chen, B. et al. 2016. Vascul. Pharmacol. 85: 1-10.

PMID: # 25816318  Kao, YT. et al. 2015. PLoS Pathog. 11: e1004750.

PMID: # 26004183  Sujobert, P. et al. 2015. Cell Rep. 11: 1446-57.

PMID: # 25344585  Beauchamp, EM. et al. 2015. Mol. Cancer Ther. 14: 202-12.

PMID: # 26188187  Xu, Y. et al. 2015. Brain Behav. Immun. 50: 298-313.

PMID: # 24781252  Davidge-Pitts, C. et al. 2014. J. Endocrinol. 222: 87-97.

PMID: # 22553202  Nin, V. et al. 2012. J. Biol. Chem. 287: 23489-501.

PMID: # 22532801  Moser, TS. et al. 2012. PLoS pathogens. 8: e1002661.

Citations 1 to 9 of 9 total

How should I store this compound after dissolving it in DMSO?

Asked by: two2igm05
Thank you for your question. Once dissolved in DMSO, sc-203790 can be stored at -80&ordm;C for up to 6 months. If left in a solid state, the chemical can be stored at -20&ordm;C for up to 3 years. If you have any further question or concerns, please feel free to contact our Technical Service department by calling 800-457-3801 option 2, emailing scbt@scbt.com, or using the Live Chat function on our website.
Answered by: Tech Service 8
Date published: 2017-01-11
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Rated 5 out of 5 by from Gu Q Gu Q, Yang X, Lin L, et al. Genetic ablation of solute carrier family 7a3a leads to hepatic steatosis in zebrafish during fasting[J]. Hepatology, 2014, 60(6): 1929-1941. PMID: 25130427 <br /> The A-769662 works perfect in zebrafish.
Date published: 2015-12-28
Rated 5 out of 5 by from Shen Shen, KZ. et al. (PubMed 24875176) found that bath or intracellular application of the AMPK activator A-769662, augmented tolbutamide-sensitive K-ATP currents evoked by NMDA receptor stimulation. -SCBT Publication Review
Date published: 2015-04-06
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