ML297 | GIRK inhibitor
NMR (Conforms)
Available Options
| Size : | Price | Quantity | |
|---|---|---|---|
| 10 mg | $70.00 | ||
| 50 mg | $280.00 |
ML297 (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
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
ML297 (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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Focus Biomolecules • Plymouth Meeting, PA USA • 1-855-FOCUS21
Focus Biomolecules
Plymouth Meeting, PA USA
1-855-FOCUS21
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