1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. ML402

ML402 

目录号: HY-104027 纯度: 99.77%
产品使用指南

ML402,一种噻吩甲酰胺,是一种选择性的 K2P2.1 (TREK-1)K2P10.1 (TREK-2) 活化剂,对 K2P4.1 (TRAAK) 无明显作用。

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ML402 Chemical Structure

ML402 Chemical Structure

CAS No. : 298684-44-3

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3579
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1 mg ¥1100
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5 mg ¥3300
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10 mg ¥5000
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50 mg ¥15000
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200 mg   询价  

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Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

ML402, a thiophene-carboxamide, is a selective K2P2.1(TREK-1) and K2P10.1(TREK-2) activator. ML402 is inactive against K2P4.1(TRAAK)[1].

IC50 & Target

TREK-1/2[1]

体外研究
(In Vitro)

Xenopus oocyte two-electrode voltage-clamp measurements show that ML335 and ML402 activate K2P2.1 and K2P10.1 but not K2P4.1(14.3±2.7 μM, K2P2.1-ML335; 13.7±7.0 μM, K2P2.1-ML402; 5.2±0.5 μM, K2P10.1-ML335; and 5.9±1.6 μM, K2P10.1-ML402). The K2P modulator pocket has a single difference among TREK subfamily members at the cation-π interaction position, K2P2.1 Lys271, which is also a lysine in K2P10.1 but a glutamine in K2P4.1. Swapping the Lys271 equivalent between K2P2.1 and K2P4.1 results in a clear phenotype reversal for ML335 and M402 activation. K2P2.1 (K271Q) is insensitive to ML335 and ML402, whereas K2P4.1 (Q258K) responds to both with a similar EC50 to K2P2.1 (14.3±2.7 μM, K2P2.1-ML335; 16.2±3.0 μM, K2P4.1(Q258K)-ML335; 13.7±7.0 μM, K2P2.1-ML402; 13.6±1.5 μM, K2P4.1 (Q258K)-ML402) but with a lower magnitude response than K2P2.1[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

295.78

Formula

C14H14ClNO2S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (338.09 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.3809 mL 16.9045 mL 33.8089 mL
5 mM 0.6762 mL 3.3809 mL 6.7618 mL
10 mM 0.3381 mL 1.6904 mL 3.3809 mL
*

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (8.45 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.45 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.45 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.45 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
Kinase Assay
[1]

K2P2.1cryst ML335 and ML402 complex crystals grow in the same conditions as K2P2.1cryst, but the protein is incubated for at least 1 h with 2.5 mM of activator (including ML 402) before setting the crystal plates. ML335 and ML402 are insoluble in aqueous solutions, so they are dissolved in 100% DMSO at a concentration of 500 mM. Then each compound is diluted 1:100 in SEC buffer to 5 mM concentration, giving a milky solution. This solution is mixed 1:1 to K2P2.1cryst previously concentrating to 12 mg/mL. The K2P2.1cryst ML402 mixture results in a clear solution, while the mixture with ML335 is slightly milky. The samples are briefly centrifuged in a table-top centrifuge (10,000×g) to remove any insoluble material before setting the crystal plates. Dose-response experiments are carried by first preparing a DMSO stock solution of each activator (including ML402) at a concentration of 100 mM. Owing to the low solubility of the compounds the highest test concentrations in recording solution are 100 μM and 80 μM for ML335 and ML402, respectively. Other concentrations are prepared by serial dilutions of the 100 μM solution in recording buffer supplementing with 0.1% DMSO[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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