kcnq2/q3

ICA-069673 is an activator of KCNQ2 Q3 potassium channel (IC50: 0.69 μM).

ICA 110381 is a KCNQ2 Q3 potassium channel opener for the treatment of epilepsy

QO-40 is a KCNQ2 3 potassium channels activator.

ICA-27243 is less effective at activating KCNQ4 and KCNQ3 Q5. ICA-27243 is a potent and orally active KCNQ2 Q3 potassium channel opener (EC50: 0.38 μM). ICA-27243 also has antiepileptic and anticonvulsant effects.

Kv7.2 Kv7.3 agonist 1 (Compound 16) is an orally effective agonist for the KV7.2 7.3 channels (KV7.2 7.3 channel KCNQ2 3) with an EC50 of 1.03 μM. This compound demonstrates analgesic effects in mouse models of chronic constriction injury (CCI) and Streptozotocin-induced diabetic peripheral neuropathy (DPNP), with ED50 values of 12.02 mg kg and 9.63 mg kg, respectively.

RL648_81 is a selective activator of KCNQ2 3 channels (EC50 = 190 nM). RL648_81 can be used in studies about neuronal hyperexcitability neurologic disorders.

ML252 is a selective potassium channel inhibitor, specifically targeting the KCNQ2 channel (Kv7.2) with an IC50 value of 69 nM. Additionally, ML252 demonstrates inhibitory activity against Cytochrome P450 isoforms, including IC50 values of 6.1 nM (CYP1A2), 18.9 nM (CYP2C9), 3.9 nM (CYP3A4), and 19.9 nM (CYP2D6).

ML-252 is a potent, selective inhibitor of the Kv7.2 voltage-gated potassium channel, demonstrating an IC50 value of 69 nM in patch clamp assays. It exists as the (S)-enantiomer, which is significantly more effective than both its (R)-enantiomer counterpart and the racemic mixture, with respective IC50 values of 944 nM and 160 nM. ML-252 exhibits high selectivity for Kv7.2 over other potassium channel subtypes and shows minimal activity against more than 68 G protein-coupled receptors, various transporters, L- and N-type calcium channels, K_ATP, and hERG potassium channels. However, it does inhibit the melatonin MT1 receptor by 61% at a 10 µM concentration.