WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H533245
CAS#: 1443246-62-5
Description: 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.
Hodoodo Cat#: H533245
Name: ML297
CAS#: 1443246-62-5
Chemical Formula: C17H14F2N4O
Exact Mass: 328.11
Molecular Weight: 328.323
Elemental Analysis: C, 62.19; H, 4.30; F, 11.57; N, 17.06; O, 4.87
Synonym: ML297; ML 297; ML-297.
IUPAC/Chemical Name: 1-(3,4-difluorophenyl)-3-(5-methyl-2-phenylpyrazol-3-yl)urea
InChi Key: IEKSMUSSYJUQMY-UHFFFAOYSA-N
InChi Code: 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)
SMILES Code: O=C(NC1=CC(C)=NN1C2=CC=CC=C2)NC3=CC=C(F)C(F)=C3InChI=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)
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 328.32 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Nimitvilai S, Lopez MF, Mulholland PJ, Woodward JJ. Ethanol Dependence Abolishes Monoamine and GIRK (Kir3) Channel Inhibition of Orbitofrontal Cortex Excitability. Neuropsychopharmacology. 2017 Mar 15. doi: 10.1038/npp.2017.22. [Epub ahead of print] PubMed PMID: 28139680.
2: 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. doi: 10.1111/bph.13407. PubMed PMID: 26661062; PubMed Central PMCID: PMC4761093.
3: 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. 2014 Nov 1;24(21):5102-6. doi: 10.1016/j.bmcl.2014.08.061. PubMed PMID: 25264075.
4: 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. doi: 10.1073/pnas.1405190111. PubMed PMID: 25002517; PubMed Central PMCID: PMC4115558.
5: Days E, Kaufmann K, Romaine I, Niswender C, Lewis M, Utley T, Du Y, Sliwoski G, Morrison R, Dawson ES, Engers JL, Denton J, Daniels JS, Sulikowski GA, Lindsley CW, Weaver CD. Discovery and Characterization of a Selective Activator of the G-Protein Activated Inward-Rectifying Potassium (GIRK) Channel. 2012 Apr 6 [updated 2013 Mar 14]. Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-. Available from http://www.ncbi.nlm.nih.gov/books/NBK143539/ PubMed PMID: 23762945.
6: 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. doi: 10.1021/cn400062a. PubMed PMID: 23730969; PubMed Central PMCID: PMC3778424.
7: Uchihata Y, Ando N, Ikeda Y, Kondo S, Hamada M, Umezawa K. Isolation of a novel cyclic hexadepsipeptide pipalamycin from Streptomyces as an apoptosis-inducing agent. J Antibiot (Tokyo). 2002 Jan;55(1):1-5. PubMed PMID: 11918058.
