TargetMol

ML 297

Product Code:
 
TAR-T4664
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1
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CodeSizePrice
TAR-T4664-1mg1mg£96.00
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TAR-T4664-5mg5mg£128.00
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TAR-T4664-1mL1 mL * 10 mM (in DMSO)£132.00
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TAR-T4664-10mg10mg£168.00
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TAR-T4664-25mg25mg£254.00
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TAR-T4664-50mg50mg£345.00
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TAR-T4664-100mg100mg£497.00
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  • Further Information
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Further Information

Bioactivity:
ML297 is a selective Kir3.1/3.2 (GIRK1/2) channel activator (IC50 values are 160, 887 and 914 nM for GIRK1/2, GIRK1/4 and GIRK1/3 respectively). ML297 exhibits no effect on GIRK2, GIRK2/3, Kir2.1 and Kv7.4 channels, and has minimal effect on a panel of other ion channels, receptors and transporters.
CAS:
1443246-62-5
Formula:
C17H14F2N4O
Molecular Weight:
328.323
Pathway:
Membrane transporter/Ion channel
Purity:
0.9777
SMILES:
Cc1cc(NC(=O)Nc2ccc(F)c(F)c2)n(n1)-c1ccccc1
Target:
Potassium Channel

References

Wydeven N, Marron Fernandez de Velasco E, Du Y, Benneyworth MA, Hearing MC, Fischer RA, Thomas MJ, Weaver CD, Wickman K. Mechanisms underlying the activation of G-protein-gated inwardly rectifying K+ (GIRK) channels by the novel anxiolytic drug, ML297. Proc Natl Acad Sci U S A. 2014 Jul 22;111(29):10755-60. Psichas A, Glass LL, Sharp SJ, Reimann F, Gribble FM. Galanin inhibits GLP-1 and GIP secretion via the GAL1 receptor in enteroendocrine L and K cells. Br J Pharmacol. 2016 Mar;173(5):888-98. Kaufmann K, Romaine I, Days E, Pascual C, Malik A, Yang L, Zou B, Du Y, Sliwoski G, Morrison RD, Denton J, Niswender CM, Daniels JS, Sulikowski GA, Xie XS, Lindsley CW, Weaver CD. ML297 (VU0456810), the first potent and selective activator of the GIRK potassium channel, displays antiepileptic properties in mice. ACS Chem Neurosci. 2013 Sep 18;4(9):1278-86. Nimitvilai S, Lopez MF, Mulholland PJ, Woodward JJ. Ethanol Dependence Abolishes Monoamine and GIRK (Kir3) Channel Inhibition of Orbitofrontal Cortex Excitability. Neuropsychopharmacology. 2017 Aug;42(9):1800-1812. Wen W, Wu W, Weaver CD, Lindsley CW. Discovery of potent and selective GIRK1/2 modulators via 'molecular switches' within a series of 1-(3-cyclopropyl-1-phenyl-1H-pyrazol-5-yl)ureas. Bioorg Med Chem Lett.Br J Pharmacol. 2016 Mar;173(5):888-98.