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ML 213
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 213图片
CAS NO:489402-47-3
包装与价格：
包装价格(元)
10mg电议
50mg电议

产品介绍
ML 213 是 Kv7.2 和 Kv7.4 通道的选择性激活剂，增强 Kv7.2 和 Kv7.4 通道，EC50 分别为 230 和 510 nM。
Cas No.489402-47-3
别名N-(2,4,6-三甲基苯基)-双环[2.2.1]庚烷-2-甲酰胺
化学名(1R,2R,4S)-N-mesitylbicyclo[2.2.1]heptane-2-carboxamide
Canonical SMILESO=C([C@H]1[C@H](CC2)C[C@H]2C1)NC3=C(C)C=C(C)C=C3C
分子式C17H23NO
分子量257.37
溶解度DMSO: 5 mg/ml,Ethanol: 5 mg/ml
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

ML213 is a selective activator of Kv7.2 and Kv7.4 channels, enhances Kv7.2 and Kv7.4 channels with EC50s of 230 and 510 nM, respectively.

ML213 (100 nM-30 μM) increases maximal conductance to a peak at 212% ± 27% of control, with an EC50 of 0.8 ± 0.3 μM. ML213 (10 μM) reduces the deactivation rates of Kv7.4 currents by 4.6-fold in the voltage range from –130 mV to –90 mV. ML213 is a potent and effective activator of homomeric Kv7.5 channels overexpressed in A7r5 cells. ML213 increases maximal conductance of Kv7.5 channels with an EC50 of 0.7 ± 0.2 μM. ML213 (10 μM) also reduces deactivation rates of Kv7.5 currents by 5.9-fold on average. ML213 produces similar effects on heteromeric Kv7.4/7.5 channels: 204% ± 11% maximal increase in conductance with an EC50 of 1.1 ± 0.6 μM and a 34.2 ± 3.3 mV maximal negative shift of the activation curve, with an EC50 of 3.8 ± 1.2 μM[1]. ML213 causes a vasorelaxation in different precontracted rat blood vessels. ML213 (10 μM) also hyperpolarizes mesenteric artery smooth muscle cells[2]. ML213 causes a concentration-dependent shift in the V1/2 for KCNQ2 activation with an EC50 340 ± 70 nM and a maximal shift of 37.4 mV[3].

References:
[1]. Brueggemann LI, et al. Differential activation of vascular smooth muscle Kv7.4, Kv7.5, and Kv7.4/7.5 channels by ML213 and ICA-069673. Mol Pharmacol. 2014 Sep;86(3):330-41.
[2]. Jepps TA, et al. Vasorelaxant effects of novel Kv 7.4 channel enhancers ML213 and NS15370. Br J Pharmacol. 2014 Oct;171(19):4413-24.
[3]. Yu H, et al. Discovery, Synthesis, and Structure Activity Relationship of a Series of N-Aryl- bicyclo[2.2.1]heptane-2-carboxamides: Characterization of ML213 as a Novel KCNQ2 and KCNQ4 Potassium Channel Opener. ACS Chem Neurosci. 2011 Oct 19;2(10):572-577.