| Bioactivity | ML 297 (VU 0456810) is a potent and selective GIRK1/2 activator, with an EC50 of 0.16 μM. ML 297 is potential for the treatment of epilepsy[1][2]. | |||||||||
| Target | EC50: 0.16 μM (GIRK1/2), 18 μM (GIRK1/4) | |||||||||
| Invitro | ML 297 is completely inactive for GIRK2/3[1].ML297 shows concentration-dependent efficacy in expressing GIRK1/2 cells and with an EC50 of 162 nM[2]. ML297 shows a complete inability to modulate the activity of HEK-293 cells expressing GIRK2 alone and GIRKGIRK2/3[2]. | |||||||||
| In Vivo | ML297 (60 mg/kg; i.p.) shows a highly significant ability to both prevent convulsions and prevent fatality of the PTZ treatment[2]. Animal Model: | |||||||||
| Name | ML 297 | |||||||||
| CAS | 1443246-62-5 | |||||||||
| Formula | C17H14F2N4O | |||||||||
| Molar Mass | 328.32 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Wen W, et al. Discovery of 'molecular switches' within a GIRK activator scaffold that afford selective GIRK inhibitors. Bioorg Med Chem Lett. 2013 Aug 15;23(16):4562-6. [2]. Kaufmann K, et al. 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. |