kcnq

KCNQ2/3 activator-1 is a Kv7.2/Kv7.3 (KCNQ2/3) potassium channel activator, details of which are from Compound A of Patent WO2021113757A1.

Linopirdine (DuP 996) is a TRPV1 agonist. Linopirdine is an orally active and selective M-type K+ current (IM; Kv7; KCNQ Channels) inhibitor (IC50: 2.4 μM). Linopirdine is a cognitive enhancer. It acts by stimulating release of acetylcholine and other neurotransmitters.Linopirdine is a putative cognition-enhancing drug that increases acetylcholine release in rat brain tissue.

2-Piperidinecarboxamide, N-[4-(4-methoxyphenyl)-2-thiazolyl]-1-(phenylsulfonyl)- is a potent KCNQ1 channel activator that can be used in long QT syndrome (LQTS) studies.

ZTZ240 is a KCNQ2 channel activator used in the study of epilepsy.

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.

XE 991 dihydrochloride is a Kv7 (KCNQ) channel blocker. XE 991 dihydrochloride potently inhibits Kv7.1 (KCNQ1), Kv7.2 (KCNQ2), Kv7.2 + Kv7.3 (KCNQ3) channel, and M-current (IC50s: 0.75 μM, 0.71 μM, 0.6 μM, and 0.98 μM, respectively).

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.

Kv7.2/Kv7.3 activator-2 is a blood-brain barrier-penetrating activator of Kv7.2/Kv7.3 channels with an EC50 of 0.25 μM. This compound exhibits excellent photostability and demonstrates potent anticonvulsant effects in acute epilepsy mouse models induced by maximal electroshock (MES) and sc-pentylenetetrazol (sc-PTZ).

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.

ML277 (CID-53347902) was identified as a potent activator of KCNQ1 channels (EC(50)=260 nM).

ML213 (CID-3111211) is a selective activator of Kv7.2 (KCNQ2) and Kv7.4 (KCNQ4) channels, enhances Kv7.2 and Kv7.4 channels with EC50s of 230 and 510 nM, respectively.

Hexachlorophene is an agonist of the KCNQ1/KCNE1 potassium ion channel with an EC50 value of 4.61 μM. Hexachlorophene is also an inhibitor of the Wnt/β-catenin signaling pathway.

Linoleoyl glycine, a modified polyunsaturated fatty acid, is an endogenous homologue of linoleoyl glycine. Linoleoyl glycine activates human KCNQ1/KCNE1 (hKCNQ1/hKCNE1) channels expressed in xenopus oocytes from mammalian skin, spinal cord and brain, and has shown analgesic activity in animal studies.

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.

XE991 is a novel and selective Kv7 (KCNQ) channel blocker.XE 991 dihydrochloride inhibits Kv7.1 (KCNQ1), Kv7.2 (KCNQ2), Kv7.2 + Kv7.3 (KCNQ3) channels, and M-current, and can be used for the study of neurological diseases.

UCL 2077 is a subtype-selective blocker of the epilepsy-associated KCNQ channels and it also is a selective slow-afterhyperpolarization channel blocker,with IC50 of 500 nM in hippocampal neurons in culture, having minimal effects on Ca2+ channels, action potentials, input resistance, and the medium afterhyperpolarization.

KV7 (KCNQ) voltage-gated potassium channels blocker

QO-58 is a novel Kv7 activator (opener) that activates neuronal Kv7/KCNQ/M channels, dose-dependently activating Kv7 currents, enhancing native neuronal M currents, and causing a decrease in evoked action potentials. It has anti-nociceptive effects on inflammatory pain and can be used for neuronal excitability disorders.

Ssm Spooky Toxin, derived from Scolopendra mutilans, exhibits potent lethality affecting both hematological and respiratory systems primarily through the inhibition of KCNQ (voltage-gated potassium channel family 7) channels. It demonstrates IC50 values of 2.8 μM for Kv7.4, 5.26 μM for Kv1.3, and 0.1-0.3 M for the Shal channel, respectively. Additionally, this toxin impedes cytokine production by selectively targeting the KV1.3 channel in T cells and is crucial for the centipede's circulatory system functions [1] [2] [3].

Ssm Spooky Toxin TFA, found in Scolopendra mutilans, effectively inhibits the KCNQ (voltage-gated potassium channel family 7) channels. Its IC50 values for Kv7.4, Kv1.3, and Shal channels are 2.8 μM, 5.26 μM, and 0.1-0.3 M, respectively. This toxin suppresses cytokine production by specifically targeting KV1.3 channels in T cells and plays a crucial role in the centipede's circulatory system.