ML213

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ML213 是 Kv7.2 (KCNQ2) 和 Kv7.4 (KCNQ4) 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。

ML213, also known as CID-3111211, is a selective KV7.2 (KCNQ2) and KV7.4 (KCNQ4) channel opener (EC50 values are 230 and 510 nM for KV7.2 and KV7.4 respectively). ML213 displays > 80-fold selectivity against KV7.1, KV7.3 and KV7.5 in a thallium-based fluorescence assay.

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. ML213 causes a vasorelaxation in different precontracted rat blood vessels. ML213 (10 μM) also hyperpolarizes mesenteric artery smooth muscle cells. 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.

——

ML213 | ML 213 | ML-213 | CID-3111211

Others

Other Targets

Kv7.2 (KCNQ2) channels| Kv7.4 (KCNQ4) channels

Others-Field

——

489402-47-3

257.38

C17H23NO

>98% (HPLC)

DMSO : 30 mg/mL 116.56 mM;

C12C(CC(CC1)C2)C(=O)Nc1c(cc(cc1C)C)C

N-(2,4,6-trimethylphenyl)bicyclo[2.2.1]heptane-6-carboxamide

(-20℃)

With Ice Pack

≥ 2 years