ML213 (CID-3111211) is a selective KV7.2 (KCNQ2) and KV7.4 (KCNQ4) channel opener, with EC50 values of 230 and 510 nM for KV7.2 and KV7.4, respectively. 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 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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO ≥ 25 mg/mL (May need warming)|
Differential activation of vascular smooth muscle Kv7.4, Kv7.5, and Kv7.4/7.5 channels by ML213 and ICA-069673
Lyubov I Brueggemann, et al. Mol Pharmacol. 2014 Sep;86(3):330-41. PMID: 24944189.
Vasorelaxant effects of novel Kv 7.4 channel enhancers ML213 and NS15370
T A Jepps, et al. Br J Pharmacol. 2014 Oct;171(19):4413-24. PMID: 24909207.
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
Haibo Yu, et al. ACS Chem Neurosci. 2011 Oct 19;2(10):572-577. PMID: 22125664.
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