Voltage-gated potassium channel
Voltage-gated potassium channels (Kv channels) are transmembrane ion channels that regulate membrane excitability by mediating K+ efflux and contributing to the repolarization of neuronal and cardiac action potentials, while also influencing calcium signaling, cell volume regulation, proliferation, and migration[1]. Kv channels are broadly expressed across multiple tissues, and genetic alterations in Kv channel genes are associated with neurological disorders, cardiac diseases, and deafness, highlighting their central role in excitable and non-excitable cells[2]. Mechanistically, Kv channel activity shapes cellular signaling networks by controlling membrane potential and thereby modulating downstream calcium-dependent biological processes[1]. In disease models, dysregulation of specific Kv isoforms has been linked to autoimmune, neuroinflammatory, metabolic, neurological, cardiovascular, and cancer-related pathologies, supporting their value as therapeutic targets[1][3]. Compared with related Kv isoforms, Kv1.3 exhibits a distinctive role in immune and inflammatory regulation because its expression is upregulated during lymphocyte, microglial, and macrophage activation, and its activity contributes to cellular proliferation and apoptosis control[3][4]. This isoform-specific biology has positioned Kv1.3 as an important target for autoimmune and neuroinflammatory disease research[4]. For experimental applications, pharmacological inhibition of Kv1.3 suppresses proliferation-related signaling and can promote apoptosis through mitochondrial mechanisms, providing a useful strategy for mechanistic studies and therapeutic development[3]. More broadly, recent advances in Kv channel pharmacology have expanded interest in channel-selective modulators and structure-guided drug discovery approaches for neurological and cardiovascular disorders[5].
References:
- [1]. Wulff H, et al. Voltage-gated potassium channels as therapeutic targets. Nat Rev Drug Discov. 2009 Dec;8(12):982-1001. [Content Brief]
- [2]. Database: Guide to pharmacology.
- [3]. A. Teisseyre, et al. Chmielarz, ‘Voltage-Gated Potassium Channels Kv1.3 in Health and Disease’, Physiology. IntechOpen, Dec. 11, 2023
- [4]. Chandy KG, et al. Structure of the voltage-gated potassium channel KV1.3: Insights into the inactivated conformation and binding to therapeutic leads. Channels (Austin). 2023 Dec;17(1):2253104. [Content Brief]
- [5]. Lopez-Mateos D, et al. Recent advances in the pharmacology of voltage-gated ion channels. Pharmacol Rev. 2025 Nov;77(6):100090. [Content Brief]
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Voltage-gated potassium channel Related Products (55)
Related Products (55)
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Mepyramine maleate
0 ImagesMepyramine maleate (Pyrilamine maleate) is a selective histamine H1 receptor antagonist and KCNQ channel inhibitor, with an IC50 of 12.5 μM against KCNQ2/Q3. Mepyramine maleate shows no activity against allergic asthma in mice when used alone, but modulates the effect of JNJ 7777120 (HY-13508) on allergic asthma in mice; it inhibits the development of morphine physical dependence and increases histamine levels in mouse brains. Mepyramine maleate can be used in studies related to seizures, convulsions, allergic asthma and morphine physical dependence.
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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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ML252
0 ImagesML252 is a selective inhibitor of KCNQ2 (Kv7.2) channel with an IC50s of 69 nM, 2.92 μM, 0.12 μM and 0.20 μM for KCNQ2, KCNQ1 (Kv7.1), KCNQ2/Q3 and KCNQ4, respectively. ML252 also inhibits Cytochrome P450 with IC50s of 6.1 nM (CYP1A2), 18.9 nM (CYP2C9), 3.9 nM (CYP3A4), 19.9 nM (CYP2D6), respectively. ML252 shows highly brain penetrant .
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Guangxitoxin 1E TFA
0 ImagesCat. No.: HY-P1427AGuangxitoxin 1E TFA is the TFA salt form of Guangxitoxin 1E (HY-P1427). Guangxitoxin 1E TFA is a peptide toxin and a selective inhibitor for voltage-gated potassium channel KV2.1 and KV2.2 with IC50 of 1-3 nM. Guangxitoxin 1E TFA enhances glucose-stimulated intracellular calcium ion oscillations and increases insulin secretion in a glucose-dependent manner.
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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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LY3972406
0 ImagesCat. No.: HY-184003CAS No.: 3071928-57-6LY3972406 is an orally active, selective Kv1.3 antagonist. LY3972406 acts on chronically stimulated effector memory T cells without affecting naive central memory T cells. LY3972406 induces mild, non-adverse skin irritation in Rattus norvegicus. LY3972406 is applicable for the research of autoimmune diseases.
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Drofenine hydrochloride
0 ImagesDrofenine (Cycloadiphene; Hexahydroadiphenine) hydrochloride is an brain-penetrant antispasmodic agent. Drofenine hydrochloride is a Kv2.1 channel inhibitor with human IC50 of 9.53 μM. Drofenine hydrochloride is a butyrylcholinesterase (BChE) inhibitor with Ki of 0.003 mM, and is a TRPV3 activator. Drofenine hydrochloride blocks Kv2.1-dependent potassium efflux, inhibits Kv2.1/JNK/NF-κB and IkBa/NF-kB signaling, suppresses Kv2.1 mRNA/protein expression. Drofenine suppresses oligomeric Aβ-induced microglial NLRP3 inflammasome activation and neuronal Tau hyperphosphorylation, improves cognitive impairment, promotes neurite outgrowth. Drofenine hydrochloride induces calcium influx in keratinocytes and exert cytotoxicity against keratinocytes. Drofenine hydrochloride ameliorates diabetic peripheral neuropathy -like pathology. Drofenine hydrochloride can be used for the researches of Alzheimer's disease, diabetic peripheral neuropathy and smooth muscle spasm.
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Dendrotoxin-I TFA
0 ImagesCat. No.: HY-P3055APurity: 99.85%Synonyms: DTX-I TFADendrotoxin-I (DTX-I) TFA is a potent K+ channel blocker with IC50s of 0.13-50 nM for voltage-gated potassium channel subunits KV1.1, KV1.2 and KV1.6. Dendrotoxin-I TFA, a neurotoxin, has the potential for cancer research.
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ICA 110381
0 ImagesICA 110381 is an orally active Kv7.2/Kv7.3 (KCNQ2/3) potassium channel activator with anticonvulsive properties. ICA 110381 is a KCNQ2/Q3 activator (EC50=0.38 μM) as well as KCNQ1 antagonist (IC50=15 μM).
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CP 339818 hydrochloride
0 ImagesCP 339818 hydrochloride is a non-peptide Kv1.3 channel (IC50 = 200 nM) and Kv1.4 channel blocker. CP 339818 hydrochloride inhibits HCN channel with IC50s of 18.9 μM and 43.4 μM against HCN1 and HCN4 (high Cl-). CP 339818 hydrochloride has significantly weaker blocking effects on Kv1.1, Kv1.2, Kv1.5, Kv1.6, Kv3.1-4, and Kv4.2 channels. CP 339818 hydrochloride selectively blocked Kv1.3, thereby inhibiting the activation process of human T cells. CP 339818 hydrochloride can be used to study the physiological functions of HCN and Kv channels.
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LY3972406 hydrochloride
0 ImagesLY3972406 hydrochloride is a kv1.3 potassium channel inhibitor without affecting hERG channel activity. LY3972406 hydrochloride hydrochloride can be used in research of immune-related diseases such as psoriasis, rheumatoid arthritis, and systemic lupus erythematosus.
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PVTX-405
0 ImagesCat. No.: HY-172930CAS No.: 2991021-08-8PVTX-405 is a selective and oral active IKZF2 molecular glue degrader with a DC50 of 0.7 nM and a Dmax of 91%. PVTX-405 enhances degradation efficiency, significantly reduces off-target degradation, and alleviates hERG inhibition with IC50 of 48 µM. PVTX-405 significantly inhibits the growth of MC38 tumors, with greater synergistic anti-cancer efficacy in combination with immune checkpoint therapies (ICTs) (anti-PD1 or anti-LAG3) in the MC38 mouse tumor xenograft model using Crbn391V C57BL/6 mice.
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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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ProTx-I
0 ImagesCat. No.: HY-P1073CAS No.: 484598-35-8ProTx-I is a toxin derived from Thrixopelma pruriens and a peptide inhibitor targeting TTX-resistant sodium channels. ProTx-I interacts with voltage sensors of multiple domains such as NaV1.7, reduces neuronal excitability through allosteric modulation of channel gating and alteration of voltage dependence. The IC50 values of ProTx-I against human NaV1.7, NaV1.2, NaV1.6, and NaV1.5 are 95 nM, 104 nM, 21 nM, and 358 nM, respectively; ProTx-I also potently inhibits Ba2+ currents of hCav3.1, while its inhibitory potency against hCav3.2 is approximately 160-fold lower. ProTx-I is applicable to the research of chronic pain.
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Vm24-toxin TFA
0 ImagesCat. No.: HY-P5917ASynonyms: Vaejovis mexicanus peptide 24 TFAVm24-toxin (Vaejovis mexicanus peptide 24) TFA, a 36-residue peptide, is a potent and selective Kv1.3 blocker with a Kd of ~3 pM in lymphocytes. Vm24-toxin TFA shows >1500-fold affinity for Kv1.3 over other assayed potassium channels. Vm24-toxin TFA folds into a distorted cystine-stabilized α/β motif consisting of a single-turn α-helix and a three-stranded antiparallel β-sheet, stabilized by four disulfide bridges. Vm24-toxin TFA attenuates the CD4+ effector memory T cell response to T cell receptor (TCR) stimulation.
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ADWX 1 TFA
0 ImagesCat. No.: HY-P1409APurity: 98.37%ADWX 1 TFA is a new peptide inhibitor that is potent and selective for Kv1.3 with an IC50 value of 1.89 pM. ADWX 1 inhibits Kv1.3 channel activity specifically to inhibit both the initial calcium signaling and NF-κB activation. ADWX 1 TFA ameliorates the disease in rats of experimental autoimmune encephalomyelitis (EAE) models. ADWX 1 TFA can be used to study T cell-mediated autoimmune diseases.
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4',7-Di-O-methylnaringenin
0 ImagesSynonyms: (-)-Naringenin 4',7-dimethyl Ether; (-)-NRG-DM4',7-Di-O-methylnaringenin ((−)-NRG-DM) is a flavonoid found in Renealmia alpinia. (−)-NRG-DM inhibits Nav1.7, Nav1.8 and Kv2.1 channels and has analgesic activity. Intraperitoneal administration of (−)-NRG-DM dose-dependently attenuated pain in a formalin-induced mouse inflammatory pain model and mustard oil-induced mouse colorectal pain model[2].
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Spinoxin
0 ImagesSynonyms: Potassium channel toxin alpha-KTx 6.13; SPX; α-KTx6.13Spinoxin isolated from the venom of scorpion Heterometrus spinifer, is a 34-residue peptide neurotoxin cross-linked by four disulfide bridges. Spinoxin is a potent inhibitor of Kv1.3 potassium channel (IC50 = 63 nM), considering to be valid molecular targets in the diagnostics and therapy of various autoimmune disorders and cancers.
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ML252 hydrochloride
0 ImagesCat. No.: HY-18063ACAS No.: 2309887-61-2ML252 hydrochloride is a selective inhibitor of KCNQ2 (Kv7.2) channel with IC50s of 69 nM, 2.92 μM, 0.12 μM and 0.20 μM for KCNQ2, KCNQ1 (Kv7.1), KCNQ2/Q3 and KCNQ4, respectively. ML252 hydrochloride also inhibits Cytochrome P450 with IC50s of 6.1 nM (CYP1A2), 18.9 nM (CYP2C9), 3.9 nM (CYP3A4), 19.9 nM (CYP2D6), respectively. ML252 hydrochloride shows highly brain penetrant.
