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Hyperpolarization

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34

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3

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-100945

    mAChR Neurological Disease
    Nitrocaramiphen hydrochloride is a selective M1 receptor antagonist (Ki: 5.5 nM). Nitrocaramiphen Hydrochloride inhibits the hyperpolarizing effect of muscarine in the muscle fibers .
    Nitrocaramiphen hydrochloride
  • HY-16689
    VU 0240551
    1 Publications Verification

    Potassium Channel Others
    VU 0240551 is a potent neuronal K-Cl cotransporter KCC2 inhibitor (IC50=560 nM) and is selective versus NKCC1. VU 0240551 also inhibits hERG and L-type Ca 2+ channels. VU 0240551 attenuates GABA-induced hyperpolarization of P cells, produces a positive shift in the P cell GABA reversal potential and enhances P cell synaptic transmission .
    VU 0240551
  • HY-124424

    Potassium Channel Others Neurological Disease
    VU0071063 is a potent and specific Kir6.2/SUR1 opener (EC50=7.44 μM) and can be used for investigating Kir6.2/SUR1 expressed in the pancreas and brain. VU0071063 inhibits insulin secretion by inducing hyperpolarization of β-cell membrane potential. VU0071063 chemotype has a very steep structure-activity relationships .
    VU0071063
  • HY-123264

    Potassium Channel Neurological Disease
    RL648_81 is a specific KQT-like subfamily 2/3 (KCNQ2/3) activator with an EC50 of 190 nM. RL648_81 robustly shifts the V1/2 of KCNQ2/3 channels towards hyperpolarized potentials.RL648_81 does not shift the V1/2 of either KCNQ4 or KCNQ5.RL648_81 has the potential for neurologic disorders associated with neuronal hyperexcitability research .
    RL648_81
  • HY-101346
    ZD7288
    5+ Cited Publications

    ICI D7288

    HCN Channel Neurological Disease
    ZD7288 (ICI D7288) is a selective hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker .
    ZD7288
  • HY-N12528

    Epoxide Hydrolase Cardiovascular Disease
    10,11-EDT, a soluble epoxide hydrolase (sEH) substrate, is a metabolic product of adrenic acid. 10,11-EDT is an endothelium-derived hyperpolarizing factor with strong vasorelaxant effects .
    10,11-EDT
  • HY-131281

    Drug Metabolite Others
    Ivabradine impurity 1 is an Ivabradine impurity. Ivabradine is an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker .
    Ivabradine impurity 1
  • HY-131282

    Drug Metabolite Others
    Ivabradine impurity 2 is an Ivabradine impurity. Ivabradine is an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker .
    Ivabradine impurity 2
  • HY-131283

    Drug Metabolite Endocrinology
    8-Demethyl Ivabradine is a metabolite of Ivabradine. Ivabradine is an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker .
    8-Demethyl Ivabradine
  • HY-P3384

    Antibiotic Others Inflammation/Immunology
    Pezadeftide is a potent antifungal peptide. Pezadeftide can enter fungal cells and cause a rapid mitochondrial response that results in hyperpolarization of the mitochondrial membrane .
    Pezadeftide
  • HY-100799

    GABA Receptor Neurological Disease
    ZAPA sulfate is an agonist at low affinity GABAA-receptors. ZAPA sulfate induces membrane hyperpolarization of the Ascaris muscle cell with an EC50 of 10.3 μM .
    ZAPA sulfate
  • HY-133614

    Potassium Channel Others
    Dihydroisopimaric acid activates large conductance Ca 2+ activated K + (BK) channels alphabeta1 in the direct measurement of BKalphabeta1 opening under whole-cell voltage clamp .
    Dihydroisopimaric acid
  • HY-119102

    HCN Channel Inflammation/Immunology
    BPU-11 is a hyperpolarization-activated cyclic nucleotide-gated (HCN) C-linker pocket (CLP) HCN4 CLP ligand. BPU-11 can be used for the research of congenital immune disease .
    BPU-11
  • HY-161092A

    HCN Channel Potassium Channel Others
    KIO-301 chloride hydrochloride is an azobenzene photoswitchable compound that blocks voltage-gated ion channels, including hyperpolarization-activated cyclic nucleotide gating (HCN, during exposure to visible light) ) and voltage-gated potassium channels (voltage-gated potassium channels) .
    KIO-301 chloride (hydrochloride)
  • HY-122114
    ICA-27243
    1 Publications Verification

    Potassium Channel Neurological Disease
    ICA-27243 is a selective, potent and orally active KCNQ2/Q3 potassium channel opener with an EC50 of 0.38 μM. ICA-27243 is less effective at activating KCNQ4 and KCNQ3/Q5. ICA-27243 has antiepileptic and anticonvulsant effects .
    ICA-27243
  • HY-B0162A
    Ivabradine hydrochloride
    2 Publications Verification

    HCN Channel Cardiovascular Disease Endocrinology Cancer
    Ivabradine hydrochloride is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine hydrochloride reduces dose-dependently heart rate without modification of blood pressure. Ivabradine hydrochloride shows anticonvulsant, anti-ischaemic and anti-anginal activity .
    Ivabradine hydrochloride
  • HY-108592

    Potassium Channel Neurological Disease
    UCL 2077 is a selective slow-afterhyperpolarization (sAHP) channel blocker (IC50 = 500 nM in hippocampal neurons in culture), having minimal effects on Ca2+ channels, action potentials, input resistance and the medium after hyperpolarization . UCL 2077 is also a subtype-selective blocker of the epilepsy associated KCNQ channels .
    UCL 2077
  • HY-B0162

    HCN Channel Cardiovascular Disease
    Ivabradine is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine reduces dose-dependently heart rate without modification of blood pressure. Ivabradine shows anticonvulsant, anti-ischaemic and anti-anginal activity .
    Ivabradine
  • HY-N0219
    Bicuculline
    Maximum Cited Publications
    21 Publications Verification

    (+)-Bicuculline; d-Bicuculline

    GABA Receptor Neurological Disease
    Bicuculline ((+)-Bicuculline) is A competing neurotransmitter GABAA receptor antagonist (IC50=2 μM). Bicuculline also blocks Ca 2+ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice .
    Bicuculline
  • HY-100418

    Potassium Channel Cardiovascular Disease
    SKA-111 is a selective activator of potassium phannel KCa 3.1 , evokes KCa 3.1 membrane hyperpolarization in porcine endothelial cell. SKA-111 is capable of improving Bradykinin (HY-P0206)-induced coronary dilations in the isolated rat heart and can be used for cardiovascular disease research .
    SKA-111
  • HY-163455

    HCN Channel Neurological Disease
    pan-HCN-IN-1 (Compound J&J12e) is an inhibitor for hyperpolarization-activated and cyclic-nucleotide-gated 1 (HCN1) ion channel, with IC50 of 58 nM. pan-HCN-IN-1 reduces the voltage sag response and enhances EPSP summation in ex vivo rats brain slices .
    pan-HCN-IN-1
  • HY-111655
    SKA-31
    3 Publications Verification

    Potassium Channel Cardiovascular Disease
    SKA-31 is a potent potassium channel activator with EC50s of 260 nM, 1.9 μM, 2.9 μM, and 2.9 μM for KCa3.1, KCa2.2, KCa2.1 and KCa2.3, respectively. SKA-31 potentiates endothelium-derived hyperpolarizing factor response and lowers blood pressure .
    SKA-31
  • HY-B0162S

    HCN Channel Cardiovascular Disease
    Ivabradine-d6 is the deuterium labeled Ivabradine[1]. Ivabradine is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine reduces dose-dependently heart rate without modification of blood pressure. Ivabradine shows anticonvulsant, anti-ischaemic and anti-anginal activity[2][3][4][5].
    Ivabradine-d6
  • HY-N12788

    Parasite Infection
    T-Cadinol is a sesquiterpene isolated from C. sylvestris that exhibits anti-Trypanosoma cruzi activity, with IC50 values of 18.2 μM and 15.8 μM against trypomastigote and amastigote forms, respectively. T-Cadinol can induce mitochondrial damage in parasites, leading to membrane hyperpolarization and decreased levels of reactive oxygen species. T-Cadinol can be used for the research of Chagas disease .
    T-Cadinol
  • HY-B0162AR

    HCN Channel Cardiovascular Disease Endocrinology Cancer
    Ivabradine (hydrochloride) (Standard) is the analytical standard of Ivabradine (hydrochloride). This product is intended for research and analytical applications. Ivabradine hydrochloride is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine hydrochloride reduces dose-dependently heart rate without modification of blood pressure. Ivabradine hydrochloride shows anticonvulsant, anti-ischaemic and anti-anginal activity .
    Ivabradine hydrochloride (Standard)
  • HY-163880

    EGFR Ras p38 MAPK Reactive Oxygen Species Cancer
    EGFR-IN-119 (Compound 5l) is an inhibitor for EGFR with an IC50 of 84.3 nM. EGFR-IN-119 inhibits the cytotoxicity in lung cancer cell A549 with an IC50 of 1.34 μM. EGFR-IN-119 downregulates the expressions of EGFR, KRAS, and MAP2K genes, exhibits antioxidant activity through reduction of reactive oxygen species (ROS), and hyperpolarizes the mitochondrial membrane potential .
    EGFR-IN-119
  • HY-118689

    Potassium Channel Cardiovascular Disease Neurological Disease Inflammation/Immunology
    RA-2 is a negative-gating modulator of KCa2/3 channels with an IC50 of 17 nM. RA-2 inhibits bradykinin-induced endothelium-derived hyperpolarization (EDH)-type relaxation in U46619-precontracted rings. RA-2 can help to define the physiologic and pathomechanistic roles of KCa2/3 in the vasculature, central nervous system, and during inflammation .
    RA-2
  • HY-N0219R

    GABA Receptor Neurological Disease
    Bicuculline (Standard) is the analytical standard of Bicuculline. This product is intended for research and analytical applications. Bicuculline ((+)-Bicuculline) is A competing neurotransmitter GABAA receptor antagonist (IC50=2 μM). Bicuculline also blocks Ca2+ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice .
    Bicuculline (Standard)
  • HY-13422
    Zatebradine hydrochloride
    1 Publications Verification

    UL-FS-49; UL-FS-49CL

    HCN Channel Cardiovascular Disease
    Zatebradine (UL-FS-49 (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 values 1.96 μM. Zatebradine blocks the slow inward current through human HCN1, HCN2, HCN3 and HCN4 channels, with IC50 values of 1.83 μM, 2.21 μM, 1.90 μM and 1.88 μM, respectively .
    Zatebradine hydrochloride
  • HY-118317

    Others Cardiovascular Disease
    Zacopride is a selective agonist with the activity of enhancing the inward rectifier potassium current (IK1) in rabbit hearts. Zacopride also exhibits significant antiarrhythmic effects, inhibiting ventricular arrhythmias by increasing IK1 without affecting atrial arrhythmias. Zacopride can hyperpolarize the resting membrane potential and shorten the action potential duration (APD) in a concentration-dependent manner. Zacopride significantly reduced the incidence of compound-induced early afterdepolarizations (EADs) at 1 μmol/L .
    Zacopride
  • HY-108596

    Potassium Channel Inflammation/Immunology
    BL-1249 is a nonsteroidal anti-inflammatory agent (NSAID) and a potassium channel activator. BL-1249 potently activates K2P2.1 (TREK-1) and K2P10.1 (TREK-2) with EC50 values of 5.5 μM and 8.0 μM, respectively. BL-1249 extracellular application activates all TREK subfamily members but has no effect on other K2P subfamilies. BL-1249 exhibits more selective for the bladder (EC50 of 1.26 μM) than vascular tissue (EC50 of 21.0 μM) .
    BL-1249
  • HY-13422A
    Zatebradine
    1 Publications Verification

    UL-FS-49 free base; UL-FS-49CL free base

    HCN Channel Cardiovascular Disease
    Zatebradine (UL-FS-49 (free base); UL-FS-49CL (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 value of 1.96 µM. Zatebradine blocks the slow inward current through human HCN1, HCN2, HCN3 and HCN4 channels, with IC50 values of 1.83 µM, 2.21 µM, 1.90 µM and 1.88 µM, respectively .
    Zatebradine
  • HY-D0085
    DiSC3(5)
    5 Publications Verification

    Fluorescent Dye Others
    DiSC3(5) is a fluorescent probe commonly used as a tracer dye to evaluate mitochondrial membrane potential. The excitation/emission wavelength of DiSC3(5) is up to 622/670 nm. DiSC3(5) can inhibit the respiratory system associated with mitochondrial NAD, and the IC50 value is 8 μM. DiSC3(5) in the presence of Na +/K +-ATPase inhibitor ouabain 2 can induce membrane hyperpolarization of Ehrlich ascites tumor cells .
    DiSC3(5)
  • HY-N6789
    KT5720
    3 Publications Verification

    PKA Neurological Disease Cancer
    KT5720 is a potent, cell-permeable, specific, reversible and ATP-competitive PKA inhibitor (IC50=3.3 μM). KT5720 is effective in reversing MDR1-mediated multidrug resistance. KT5720 also reduces the excitability of dorsal root ganglion (DRG) neurons by attenuating Hyperpolarization-activated cyclic nucleotide-gated (HCN) channel activity and reducing intracellular Ca2 + concentrations. KT5720 can be used in the study of haematological malignancies as well as HCN and DRG neuron-related diseases .
    KT5720

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