1443246-62-5

1443246-62-5 structure

Name: ML 297
Chemical Name: 1-(3,4-Difluorophenyl)-3-(3-methyl-1-phenyl-1H-pyrazol-5-yl)ure
CAS Number: 1443246-62-5
Molecular Formula: C₁₇H₁₄F₂N₄O
Molecular Weight: 328.316
Catalog: Signaling Pathways Membrane Transporter/Ion Channel Potassium Channel
Create Date: 2016-05-13 11:13:35
Modify Date: 2024-02-01 10:33:02
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].

Name	1-(3,4-Difluorophenyl)-3-(3-methyl-1-phenyl-1H-pyrazol-5-yl)ure
Synonyms	Urea, N-(3,4-difluorophenyl)-N'-(3-methyl-1-phenyl-1H-pyrazol-5-yl)- 1-(3,4-Difluorophenyl)-3-(3-methyl-1-phenyl-1H-pyrazol-5-yl)urea

Description	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].
Related Catalog	Research Areas >> Neurological Disease Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel
Target	EC50: 0.16 μM (GIRK1/2), 18 μM (GIRK1/4)[1]
In Vitro	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: 8-10 months old C57/BL6 male mice (approximately 30 g)[2] Dosage: 60 mg/kg Administration: Intraperitoneal injection Result: Most of the animals neither convulsions nor death.
References	[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.