A selective GIRK1/2 activator (EC50s = 0.16 and 1.8 μM for GIRK1/2 and GIRK1/4

ML-297 – 1 mg

Brand:
Cayman
CAS:
1443246-62-5
Storage:
-20
UN-No:
De Minimis - 3077 / 9

G protein-regulated inwardly rectifying potassium (GIRK1-4) channels are a family of Kir3.1-Kir3.4 ion channels that modulate cell excitability. The four different GIRK subunits are composed in different homo- and heterotetrameric combinations, which are expressed with regional specificity throughout the central nervous system and in the periphery.{23990} ML-297 is a selective GIRK1/2 activator (EC50s = 0.16 and 1.8 μM for GIRK1/2 and GIRK1/4, respectively, and is completely inactive at GIRK2/3).{23990,23989} In two different mouse models of epilepsy, ML-297 at 60 mg/kg was shown to delay seizure onset and to prevent convulsions.{23990}  

 

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Description

A selective GIRK1/2 activator (EC50s = 0.16 and 1.8 μM for GIRK1/2 and GIRK1/4, respectively; 60 mg/kg can delay seizure onset and prevent convulsions in two different mouse models of epilepsy

Formal name: N-(3,4-difluorophenyl)-N’-(3-methyl-1-phenyl-1H-pyrazol-5-yl)-urea

Synonyms:  CID-56642816|VU0456810

Molecular weight: 328.3

CAS: 1443246-62-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Activators||Research Area|Neuroscience|Seizure Disorders

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