ML 297

Names

[ Name ]:
ML 297

[Synonym ]:
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

Biological Activity

[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.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
377.8±42.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₇H₁₄F₂N₄O

[ Molecular Weight ]:
328.316

[ Flash Point ]:
182.3±27.9 °C

[ Exact Mass ]:
328.113556

[ PSA ]:
62.44000

[ LogP ]:
4.73

[ Vapour Pressure ]:
0.0±0.9 mmHg at 25°C

[ Index of Refraction ]:
1.617

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS09

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H410

[ Precautionary Statements ]:
P273-P501

[ RIDADR ]:
UN 3077 9 / PGIII