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ML-297
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
ML-297图片
CAS NO:1443246-62-5
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
ML-297 (VU 0456810) 是一种有效的选择性 GIRK1/2 激活剂，EC50 为 0.16 μM。
Cas No.1443246-62-5
别名CID-56642816,VU0456810
化学名N-(3,4-difluorophenyl)-N'-(3-methyl-1-phenyl-1H-pyrazol-5-yl)-urea
Canonical SMILESO=C(NC1=CC(F)=C(F)C=C1)NC2=CC(C)=NN2C3=CC=CC=C3
分子式C17H14F2N4O
分子量328.3
溶解度≤20mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

EC50: 0.16 and 1.8 μM for GIRK1/2 and GIRK1/4, respectively.

ML-297 is a selective Kir3.1/3.2 (GIRK1/2) channel activator.

G protein-regulated inwardly rectifying potassium (GIRK1-4) channels are a family of Kir3.1-Kir3.4 ion channels modulating cell excitability. The four different GIRK subunits are composed in different combinations expressed with regional specificity throughout the central nervous system and in the periphery.

In vitro: In thallium flux assays, ML297 showed concentration-dependent efficacy when tested on cells expressing GIRK1/2. ML297 could also activate GIRK channels comprised of GIRK1/3 and GIRK1/4 subunit combinations. However, ML297 diaplayed a complete inability to modulate the activity of HEK-293 cells expressing GIRK2 alone. A similar complete lack of efficacy was seen when ML297 was tested on HEK-293 cells expressing GIRK2/3. Therefore, it appeared that ML297 is only capable of activating GIRK channels containing a GIRK1 subunit [1].

In vivo: Previous study performed an ascending dose study in mice and it was found that the animals appeared normal and not under obvious distress at all doses tested. ML297’s effects on locomotor activity as well as effects on motor function and coordination were further evaluated. Results showed that ML297 at 60 mg/kg could immediate decrease in locomotor activity compared to the control group [1].

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Kaufmann, K. ,Romaine, I.M.,Days, E., et al. ML297 (VU0456810), the first potent and selective activator of the GIRK potassium channel, displays antiepileptic properties in mice. ACS Chem.Neurosci. 4(9), 1278-1286 (2013).