1. Signaling Pathways
  2. Membrane Transporter/Ion Channel
  3. Potassium Channel
  4. Voltage-gated potassium channel Isoform
  5. Voltage-gated potassium channel Activator

Voltage-gated potassium channel Activator

Voltage-gated potassium channel Activators (10):

Cat. No. Product Name Effect Purity
  • HY-17001A
    Flupirtine
    Activator 99.98%
    Flupirtine (D 9998) is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis.
  • HY-172431
    Opakalim
    Activator 99.88%
    Opakalim (BHV-7000) is a selective Kv7.2/7.3 potassium channels activator with an EC50 of 0.6 μM. Opakalim shows minimal GABAA receptor activation and exhibits potent anti-seizure efficacy in the maximal electroshock seizure (MES) model. Opakalim can be used for the study of seizures.
  • HY-175668
    IDOR-1104-0086
    Activator 98.98%
    IDOR-1104-0086 is an orally active Kv7 potassium channel opener with an EC50 of 210 nM that can cross blood-brain barrier. IDOR-1104-0086 displays strong selectivity against the hERG channel with an IC20 of 25 μM. IDOR-1104-0086 exhibits efficacy in two rodent models of epilepsy and a favorable tolerability profile. IDOR-1104-0086 can used for the study of epilepsy.
  • HY-175340
    Kv7.2/Kv7.3 activator-3
    Activator
    Kv7.2/Kv7.3 activator-3 (GRT-X) is an orally active Kv7.2/Kv7.3 and TSPO activator. Kv7.2/Kv7.3 activator-3 activates Kv7.2/Kv7.3, Kv7.4, and Kv7.5 with EC50 values of 0.37, 2.06, and 0.75 μM, respectively, and binds to TSPO with Ki values of 0.07 μM (rat membrane) and 4.60 μM (human U-118 MG cells). Kv7.2/Kv7.3 activator-3 prevents motor neuron degeneration in mice and humans conditioned by ALS/FTD astrocytes. Kv7.2/Kv7.3 activator-3 stimulates dorsal root ganglion axonal growth through TSPO and Kv7.2/3 activation. Kv7.2/Kv7.3 activator-3 has anti-epileptic effects in epileptic seizure models. Kv7.2/Kv7.3 activator-3 reduces pain hypersensitivity in patients with diabetic neuropathy, promotes neuronal survival and regeneration after cervical neuropathy in rats, and accelerates the recovery of normal function of sensory and motor neurons.
  • HY-178300
    Kv7 activator-1
    Activator
    Kv7 activator-1 (Page 66) is a Kv7 channel activator. Kv7 activator-1 can be used for the studies of depression disorders, neurodegenerative diseases or pain disorders.
  • HY-172887
    Kv7.2/Kv7.3 activator-2
    Activator
    Kv7.2/Kv7.3 activator-2 is a BBB-penetrable Kv7.2/7.3 activator (EC50: 0.25 μM). Kv7.2/Kv7.3 activator-2 has good photostability. Kv7.2/Kv7.3 activator-2 has potently antiepileptic effects in maximal electroshock (MES) and sc-pentylenetetrazol (sc-PTZ)-induced acute mice seizure models.
  • HY-181874
    E0714
    Activator
    E0714 is a blood-brain barrier-permeable, selective Kv7.2 potassium channel activator, with EC50 values of 1.90 μM and 0.021 μM for homotetrameric Kv7.2 channels and heterotetrameric Kv7.2/7.3 channels, respectively. E0714 exhibits anticonvulsant activity. E0714 can be used in research related to epilepsy.
  • HY-164417
    Kv7.2/Kv7.3 activator-1
    Activator
    Kv7.2/Kv7.3 activator-1 (compound 517) is a potent Kv7.2/Kv7.3 channel activator with an EC50 value of <1 µM. Kv7.2/Kv7.3 activator-1 has the potential for the research of neurological diseases.
  • HY-180468
    Kv7 activator-2
    Activator
    Kv7 activator-2 (A14a) is a Kv7 potassium channel activator. Kv7 activator-2 can be used for the research of neurological disease, such as epilepsy.
  • HY-181128
    QO-83
    Activator
    QO-83, Retigabine analogue, is a voltage-gated potassium channel KCNQ2 (Kv7.2) activator with an EC50 of 0.56 μM. QO-83 binds to a single hydrophobic pocket of KCNQ2-CaM complex in closed conformation. QO-83 induces a negative shift in the voltage-dependent activation curve of KCNQ2 channels, increasing the channel's voltage sensitivity. QO-83 can be used for the research of epilepsies.