ML-297
(Synonyms: CID-56642816,VU0456810) 目录号 : GC15117
A selective GIRK1/2 activator
Cas No.:1443246-62-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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).
| Cas No. | 1443246-62-5 | SDF | |
| 别名 | CID-56642816,VU0456810 | ||
| 化学名 | N-(3,4-difluorophenyl)-N'-(3-methyl-1-phenyl-1H-pyrazol-5-yl)-urea | ||
| Canonical SMILES | O=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°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.046 mL | 15.23 mL | 30.4599 mL |
| 5 mM | 0.6092 mL | 3.046 mL | 6.092 mL |
| 10 mM | 0.3046 mL | 1.523 mL | 3.046 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。