ML297

• CAT Number: I008093
• CAS Number: 1443246-62-5
• Molecular Formula: C17H14F2N4O
• Molecular Weight: 328.323
• Purity: ≥95%
• Synonyms: ML297; ML 297; ML-297.;1-(3,4-difluorophenyl)-3-(5-methyl-2-phenylpyrazol-3-yl)urea
• Target: Potassium Channel
• Solubility: Soluble in DMSO
• Storage: Store at -20°C
• IUPAC Name: 1-(3,4-difluorophenyl)-3-(5-methyl-2-phenylpyrazol-3-yl)urea
• InChI: InChI=1S/C17H14F2N4O/c1-11-9-16(23(22-11)13-5-3-2-4-6-13)21-17(24)20-12-7-8-14(18)15(19)10-12/h2-10H,1H3,(H2,20,21,24)
• InChIKey: IEKSMUSSYJUQMY-UHFFFAOYSA-N
• SMILES: CC1=NN(C(=C1)NC(=O)NC2=CC(=C(C=C2)F)F)C3=CC=CC=C3

ML297 (CAT: I008093) is a selective activator of Kir3.1/3.2 channels, also known as GIRK1/2 channels. It displays potent activation of GIRK1/2 channels with an IC50 value of 160 nM. ML297 shows minimal activity on other channel subtypes, including GIRK1/4 and GIRK1/3, as well as Kir2.1 and Kv7.4 channels. It has also been found to have little effect on a panel of other ion channels, receptors, and transporters, making it a valuable tool for studying the specific function and modulation of GIRK1/2 channels in cellular and physiological processes.

Reference

1:Mechanisms underlying the activation of G-protein-gated inwardly rectifying K+ (GIRK) channels by the novel anxiolytic drug, ML297. Wydeven N, Marron Fernandez de Velasco E, Du Y, Benneyworth MA, Hearing MC, Fischer RA, Thomas MJ, Weaver CD, Wickman K.Proc Natl Acad Sci U S A. 2014 Jul 22;111(29):10755-60. doi: 10.1073/pnas.1405190111. Epub 2014 Jul 7. PMID: 25002517 Free PMC Article2:ML297 (VU0456810), the first potent and selective activator of the GIRK potassium channel, displays antiepileptic properties in mice. 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.ACS Chem Neurosci. 2013 Sep 18;4(9):1278-86. doi: 10.1021/cn400062a. Epub 2013 Jun 13. PMID: 23730969 Free PMC Article