Voltage-gated potassium channel Activator
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Flupirtine
0 ImagesSynonyms: D 9998Flupirtine (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.
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Opakalim
0 ImagesSynonyms: BHV-7000Opakalim (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.
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QO-83
0 ImagesQO-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.
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IDOR-1104-0086
0 ImagesIDOR-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.
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Kv7.2/Kv7.3 activator-3
0 ImagesCat. No.: HY-175340CAS No.: 1361107-81-4Kv7.2/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.
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Kv7 activator-1
0 ImagesCat. No.: HY-178300CAS No.: 2222822-23-1Kv7 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.
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Kv7.2/Kv7.3 activator-2
0 ImagesCat. No.: HY-172887Kv7.2/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.
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Kv3.1 activator-1
0 ImagesCat. No.: HY-184663Kv3.1 activator-1 is a Kv3.1 voltage-gated potassium channel activator. Kv3.1 activator-1 exhibits distinct activating efficacy in both thallium flux assays and automated patch-clamp electrophysiological assays .
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E0714
0 ImagesCat. No.: HY-181874CAS No.: 1359358-36-3E0714 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.
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Kv7.2/Kv7.3 activator-1
0 ImagesCat. No.: HY-164417CAS No.: 2376398-43-3Kv7.2/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.
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Kv7 activator-2
0 ImagesCat. No.: HY-180468CAS No.: 3067929-64-7Kv7 activator-2 (A14a) is a Kv7 potassium channel activator. Kv7 activator-2 can be used for the research of neurological disease, such as epilepsy.
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