tcsc6933 ML213

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.

IC50 & Target: EC50: 230 nM (Kv7.2 channel), 510 nM (Kv7.4 channel)^[2][3]

In Vitro: 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].