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Documentos clave

SML0836

Sigma-Aldrich

ML297

≥98% (HPLC)

Sinónimos:

1-(3,4-Difluorophenyl)-3-(3-methyl-1-phenyl-1H-pyrazol-5-yl)urea, CID 56642816, VU0456810

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About This Item

Fórmula empírica (notación de Hill):
C17H14F2N4O
Número de CAS:
Peso molecular:
328.32
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 15 mg/mL, clear

storage temp.

−20°C

InChI

1S/C17H14F2N4O/c1-11-9-16(23(22-11)13-5-3-2-4-6-13)21-17(24)20-12-7-8-14(18)15(19)10-12/h2-10H,1H3,(H2,20,21,24)

InChI key

IEKSMUSSYJUQMY-UHFFFAOYSA-N

Biochem/physiol Actions

ML297 (VU0456810) is the first potent and selective activator of the GIRK potassium channel. The G protein-coupled inwardly-rectifying potassium channels (GIRKs 1-4) are widely distributed broadly in the central nervous system (GIRKs 1-3) and also found in the heart (GIRK-4). ML297 activates GIRK channels containing a GIRK1 subunit, and does not activate channels without a GIRK1 subunit or the closely related potassium channel Kir2.1 or voltage-gated potassium channels. ML297 has been shown to activate GIRK1/2 with a potency of ~160 nM and also to activate GIRK channels comprising of GIRK1/3 and GIRK1/4 subunit combinations. ML297 was active in two in vivo models of epilepsy, and showed equal or greater efficacy than the anti-seizure medication, sodium valproate.

Features and Benefits

This compound is featured on the Potassium Channels page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

pictograms

Environment

signalword

Warning

hcodes

Hazard Classifications

Aquatic Acute 1 - Aquatic Chronic 1

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


Certificados de análisis (COA)

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Yulin Zhao et al.
Cell reports, 31(11), 107770-107770 (2020-06-20)
G-protein-gated inwardly rectifying K+ (GIRK) channels are essential effectors of inhibitory neurotransmission in the brain. GIRK channels have been implicated in diseases with abnormal neuronal excitability, including epilepsy and addiction. GIRK channels are tetramers composed of either the same subunit

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