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Merck
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重要文件

SML0836

Sigma-Aldrich

ML297

≥98% (HPLC)

同義詞:

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

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About This Item

經驗公式(希爾表示法):
C17H14F2N4O
CAS號碼:
分子量::
328.32
分類程式碼代碼:
12352200
NACRES:
NA.77

品質等級

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 15 mg/mL, clear

儲存溫度

−20°C

SMILES 字串

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 密鑰

IEKSMUSSYJUQMY-UHFFFAOYSA-N

生化/生理作用

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.

特點和優勢

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.

象形圖

Environment

訊號詞

Warning

危險聲明

防範說明

危險分類

Aquatic Acute 1 - Aquatic Chronic 1

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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分析證明 (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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