SML0836
ML297
≥98% (HPLC)
别名:
1-(3,4-Difluorophenyl)-3-(3-methyl-1-phenyl-1H-pyrazol-5-yl)urea, CID 56642816, VU0456810
产品名称
ML297, ≥98% (HPLC)
SMILES string
Fc1c(ccc(c1)NC(=O)Nc2[n](nc(c2)C)c3ccccc3)F
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
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 15 mg/mL, clear
storage temp.
−20°C
Quality Level
Biochem/physiol Actions
ML297 (VU0456810) is a potent and selective activator of the GIRK potassium channel.
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.
signalword
Warning
hcodes
pcodes
Hazard Classifications
Aquatic Acute 1 - Aquatic Chronic 1
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Jose Carlos Gonzalez et al.
Cell reports, 42(2), 112039-112039 (2023-02-08)
The central circadian regulator within the suprachiasmatic nucleus transmits time of day information by a diurnal spiking rhythm driven by molecular clock genes controlling membrane excitability. Most brain regions, including the hippocampus, harbor similar intrinsic circadian transcriptional machinery, but whether
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
Serap Erdogmus et al.
Nature communications, 10(1), 5784-5784 (2019-12-21)
G-protein coupled receptors (GPCRs) are versatile cellular sensors for chemical stimuli, but also serve as mechanosensors involved in various (patho)physiological settings like vascular regulation, cardiac hypertrophy and preeclampsia. However, the molecular mechanisms underlying mechanically induced GPCR activation have remained elusive.
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