ML335
(Synonyms: CID23723457, CYM 51010) 目录号 : GC45675
An activator of K2P2.1/TREK1 and K2P10.1/TREK2
Cas No.:825658-06-8
Sample solution is provided at 25 µL, 10mM.
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ML335 is an activator of the two-pore domain potassium channels K2P2.1/TREK1 and K2P10.1/TREK2 (EC50s = 14.3 and 5.2 μM, respectively, in Xenopus oocytes).1 It is selective for K2P2.1/TREK1 and K2P10.1/TREK2 channels over K2P4.1/TRAAK channels. ML335 activates K2P2.1/TREK1 by binding to the C-type gate, which is the active site of TREK channels.
|1. Lolicato, M., Arrigoni, C., Mori, T., et al. K2P2.1(TREK-1): Activator complexes reveal a cryptic selectivity filter binding site. Nature 547(7663), 364-368 (2017).
Cell experiment: | Mouse K2P2.1, human K2P4.1, and mutants are expressed from a previously described pIRES2-EGFP vector in HEK293T cells (ATTC). 70% confluent cells are transfected (in 35-mm diameter wells) with LipofectAMINE 2000 for 6?h, and plated onto coverslips coated with Matrigel. Effects of ML335, ML402 and arachidonic acid on K2P2.1 current at 0?mV are measured by whole-cell patch-clamp experiments 24?h after transfection. Acquisition and analysis are performed using pCLAMP9 and an Axopatch 200B amplifier. Pipette resistance ranges from 1 to 1.5?MΩ. Pipette solution contains the following: 145?mM KCl, 3?mM MgCl2, 5?mM EGTA and 20?mM HEPES (pH 7.2 with KOH). Bath solution contains the following: 145?mM NaCl, 5?mM KCl, 1?mM CaCl2, 3?mM MgCl2 and 20?mM HEPES (pH 7.4 with NaOH). K2P2.1 currents are elicited by a 1?s ramp from -100 to +50?mV from a -80?mV holding potential. After stabilization of the basal current, ML335 and ML402 are perfused at 200?mL per hour until potentiation is stably reached[1]. |
References: [1]. Lolicato M, et al. K2P2.1 (TREK-1)-activator complexes reveal a cryptic selectivity filter binding site. Nature. 2017 Jul 20;547(7663):364-368. | |
| Cas No. | 825658-06-8 | SDF | |
| 别名 | CID23723457, CYM 51010 | ||
| Canonical SMILES | CS(NC1=CC=C(C(NCC2=C(Cl)C=C(Cl)C=C2)=O)C=C1)(=O)=O | ||
| 分子式 | C15H14Cl2N2O3S | 分子量 | 373.3 |
| 溶解度 | DMSO: 5 mg/ml | 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 | 2.6788 mL | 13.3941 mL | 26.7881 mL |
| 5 mM | 0.5358 mL | 2.6788 mL | 5.3576 mL |
| 10 mM | 0.2679 mL | 1.3394 mL | 2.6788 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。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet