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Product Details

ML-297 | GIRK inhibitor

ML-297 (1443246-62-5) is a selective GIRK 1/2 (Kir3.1/3.2) channel activator, IC50 = 160, 887 and 914 nM for GIRK1/2, GIRK1/4 and GIRK1/3 respectively. Has no effect on GIRK2, GIRK2/3, Kir2.1 and Kv7.4 channels.1,2  Displays antiseizure activity2 and decreases anxiety-related behavior without sedative or addictive effects3. Reduces glucose- and IBMX-stimulated GLP-1 secretion with no effect on GIP in murine L and K cells.4 Brain penetrant.

References/Citations

1) Wen et al. (2014), 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., 24 5102
2) Kaufmann et al. (2013), ML-297 (VU0456810), the first potent and selective activator of the GIRK potassium channel, displays antiepileptic properties in mice; ACS Chem. Neurosci., 4 1278
3) Wydeven et al. (2014), Mechanisms underlying the activation of G-protein-gated inwardly rectifying K+ (GIRK) channels by the novel anxiolytic drug, ML297; Proc. Natl. Acad. Sci. USA, 111 10755
4) Psichas et al. (2016), Galanin inhibits GLP-1 and GIP secretion via the GAL1 receptor in enteroendocrine L and K cells; Br. J. Pharmacol., 173 888

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ML-297 | 1443246-62-5 | Structure | Supplier

Catalog#  10-1469-0010

$70.00
Quantity
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CAS:
1443246-62-5
Catalog Number:
10-1469
Activity:
GIRK inhibitor
Chemical Name:
N-(3.4-Difluorophenyl)-n’-(3-methyl-1-phenyl-1H-pyrazol-5-yl)urea
Alternate Names:
VU0456810
Molecular Weight:
328.32
Molecular Formula:
C17H14F2N4O
Solubility:
Soluble in DMSO (up to 45 mg/ml) or in Ethanol (up to 20 mg/ml)
Physical Properties:
White solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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