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

Voltage-gated potassium channel

Kv

Voltage-gated potassium channel Related Products (43):

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-18063
    ML252
    		Inhibitor 99.9%
    ML252 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 .
  • HY-B1239
    Drofenine hydrochloride
    		98.10%
    Drofenine (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.
  • HY-P3055A
    Dendrotoxin-I TFA
    		Inhibitor 99.85%
    Dendrotoxin-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.
  • HY-186059
    HCN2 modulator-4
    		Inhibitor
    HCN2 modulator-4 is a HCN2 ion channel inhibitor. HCN2 modulator-4 inhibits HCN2 ion channel activity. HCN2 modulator-4 can be used for the research of pain, inflammatory pain, neuropathic pain, tinnitus, central nervous system disorders, psychiatric disorders, mood disorders.
  • HY-186061A
    HCN2 modulator-8
    		Inhibitor
    HCN2 modulator-8 is a pyrazolopyridine derivative and selective HCN2 inhibitor. HCN2 modulator-8 can be used for the research of pain, tinnitus, central nervous system disorders, psychiatric disorders, mood disorders.
  • HY-180464
    Kv7.2/Kv7.3 modulator-3
    		Modulator
    Kv7.2/Kv7.3 modulator-3 (example 40 peak-1) is a selective Kv7.2/Kv7.3 modulator with an EC50 of 0.099 μM.
  • HY-P1427A
    Guangxitoxin 1E TFA
    		Inhibitor
    Guangxitoxin 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.
  • HY-108587
    ICA 110381
    		Modulator 99.80%
    ICA 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).
  • HY-108574
    CP 339818 hydrochloride
    		Inhibitor 99.61%
    CP 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.
  • HY-172374A
    KV1.3-IN-2 hydrochloride
    		Inhibitor
    KV1.3-IN-2 hydrochloride is a kv1.3 potassium channel inhibitor without affecting hERG channel activity. KV1.3-IN-2 hydrochloride can be used in research of immune-related diseases such as psoriasis, rheumatoid arthritis, and systemic lupus erythematosus.
  • 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-172930
    PVTX-405
    		Inhibitor
    PVTX-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.
  • HY-P1073
    ProTx-I
    		Inhibitor
    ProTx-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.
  • HY-P1409A
    ADWX 1 TFA
    		Inhibitor 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.
  • HY-P5917A
    Vm24-toxin TFA
    		Inhibitor
    Vm24-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.
  • HY-P5931
    Spinoxin
    		Inhibitor 98.0%
    Spinoxin 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.
  • HY-18063A
    ML252 hydrochloride
    		Inhibitor 98.5%
    ML252 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.
  • 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.