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Results for "

hyperpolarize

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Antibiotic (2) Cholinesterase (ChE) (1) Drug Metabolite (3) EGFR (1) Epoxide Hydrolase (1) Fluorescent Dye (1) GABA Receptor (3) Galectin (1) Gap Junction Protein (1) HCN Channel (10) Insecticide (1) mAChR (1) p38 MAPK (1) Parasite (3) Phosphatase (1) PKA (1) Potassium Channel (15) Proton Pump (1) Ras (1) Reactive Oxygen Species (2)
By Research Areas:	Cancer (5) Cardiovascular Disease (11) Endocrinology (4) Infection (3) Inflammation/Immunology (4) Metabolic Disease (2) Neurological Disease (13)

Inhibitors & Agonists

Fluorescent Dye

Peptides

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-100945

Nitrocaramiphen hydrochloride	mAChR	Neurological Disease
Nitrocaramiphen hydrochloride is a selective M1 receptor antagonist (K_i: 5.5 nM). Nitrocaramiphen Hydrochloride inhibits the hyperpolarizing effect of muscarine in the muscle fibers .

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 .

HY-124424

VU0071063	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 .

HY-123264

RL648_81	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 .

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 .

HY-N12528

10,11-EDT	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 .

HY-164911

VU0546110	Potassium Channel	Endocrinology
VU0546110 is a selective inhibitor of the sperm-specific potassium channel SLO3, with IC₅₀s of 1.287 μM (SLO3) and 59.80 μM (SLO1) in HEK293 cells, respectively. VU0546110 blocks heterologous SLO3 currents and endogenous K ⁺ currents in human sperm. VU0546110 halts sperm hyperpolarization, induced acrosome reaction, and hyper-activated motility. VU0546110 has contraceptive potential .

HY-131281

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

HY-131282

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

HY-P3384

Pezadeftide	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 .

HY-131283

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

HY-100799

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

HY-133614

Dihydroisopimaric acid	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 .

HY-119102

BPU-11	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 .

HY-123708

SNAP 398299	Galectin	Others
SNAP 398299 is a Gal3 receptor antagonist with potential anxiolytic and antidepressant effects. SNAP 398299 can partially reverse the neuropeptide Galanin-induced inhibition of dorsal raphe cell firing and the Galanin-induced hyperpolarizing current.

HY-161092A

KIO-301 chloride (hydrochloride)	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) .

HY-137968

Avermectin B1a aglycon	Parasite	Infection
Avermectin B1a aglycon is an aglycone derivative of Avermectin B1a (HY-15308), an antiparasitic agent that paralyzes nematodes. Avermectin B1a aglycon hyperpolarizes P. crassipes muscle fibers, with a minimum effective concentration of 0.1 μM .

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 .

HY-B0162

Ivabradine	HCN Channel	Cardiovascular Disease Cancer
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 .

HY-108592

UCL 2077	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 .

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 .

HY-100418

SKA-111	Potassium Channel	Cardiovascular Disease
SKA-111 is a selective activator of potassium phannel K_Ca3.1 , evokes K_Ca3.1 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 .

HY-N0219

Bicuculline Maximum Cited Publications 26 Publications Verification (+)-Bicuculline; d-Bicuculline	GABA Receptor	Neurological Disease
Bicuculline ((+)-Bicuculline) is A competing neurotransmitter GABA_A 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 .

HY-163455

pan-HCN-IN-1	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 .

HY-111655

SKA-31 3 Publications Verification	Potassium Channel	Cardiovascular Disease
SKA-31 is a potent potassium channel activator with EC_50s 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 .

HY-163880

EGFR-IN-119	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 .

HY-B0162AR

Ivabradine (hydrochloride) (Standard)	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 .

HY-B0162S

Ivabradine-d6	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].

HY-N12788

T-Cadinol	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 .

HY-118689

RA-2	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 .

HY-N0219R

Bicuculline (Standard)	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 .

HY-P10817

Corza6	Proton Pump Reactive Oxygen Species	Metabolic Disease
Corza6 is a potent and selective human voltage-gated proton channel (hHv1) peptide inhibitor. Corza6 binds to the external voltage sensor domain (VSD) loop in hHv1 with a K_d of ~1 nM at the natural, hyperpolarized resting membrane potential (RMP) of mammalian cells. Corza6 allows capacitation in sperm and permits sustained reactive oxygen species (ROS) production in white blood cells (WBCs) .

HY-P5389

Connexin mimetic peptide 40GAP27	Gap Junction Protein	Others
Connexin mimetic peptide 40GAP27 is a biological active peptide. (This peptide corresponds to the GAP27 domain of the second extracellular loop of dominant vascular connexin (Cx40), designated as 40Gap 27. It was used to investigate mechanisms through which oxidant stress impairs communication via gap junctions. When administered, 40Gap27attenuates endothelium-dependent subintimal smooth muscle hyperpolarization.)

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 .

HY-170918

BKCa activator-1	Potassium Channel	Others
BKCa activator-1 (Compound 51b) is the orally active activator for the calcium-activated potassium channel BKCa with an EC₅₀ of 2.82 μM. BKCa activator-1 increases K+ efflux, leads to cell membrane hyperpolarization, thereby inhibiting smooth muscle contraction. BKCa activator-1 alleviates urinary incontinence in spontaneously hypertensive rat (SHR) model, exhibits antitussive effect in puinea pig cough model .

HY-108596

BL-1249	Potassium Channel	Inflammation/Immunology
BL-1249 is a nonsteroidal anti-inflammatory agent (NSAID) and a potassium channel activator. BL-1249 potently activates K_2P2.1 (TREK-1) and K_2P10.1 (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 K_2P subfamilies. BL-1249 exhibits more selective for the bladder (EC₅₀ of 1.26 μM) than vascular tissue (EC₅₀ of 21.0 μM) .

HY-102052

DCEBIO	Potassium Channel	Metabolic Disease
DCEBIO is a small/medium conductance calcium-activated potassium (SK_Ca/IK_Ca) channel opener and primary neuron signal blocker. It hyperpolarizes the membrane potential of C2C12 myoblasts by activating IK_Ca channels, thereby promoting myogenic differentiation. The specific biological activity of DCEBIO is manifested in increased myotube formation, enhanced myosin heavy chain II protein levels and myogenin mRNA levels. DCEBIO can be applied in the field of muscle research, especially in muscle-related degenerative diseases such as sarcopenia .

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 .

HY-D0085

DiSC3(5) 5+ Cited Publications	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 .

HY-171469

SKP-451	Potassium Channel	Cardiovascular Disease
SKP-451 is an ATP-sensitive potassium (K ⁺) channel agonist. SKP-451 activates the ATP-sensitive K ⁺ channels, promotes the efflux of K ⁺, causes membrane hyperpolarization, and inhibits the influx of Ca ²⁺, thereby relaxing the vascular smooth muscle. SKP-451 relaxs the canine coronary artery, rabbit basilar artery, and vertebral artery. SKP-451 also reduces the mean arterial blood pressure of conscious spontaneously hypertensive rats (SHR). SKP-451 is promising for research of cardiovascular diseases .

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 .

HY-B1194

Tetramisole hydrochloride (±)-Tetramisole hydrochloride; DL-Tetramisole hydrochloride; R-829	Parasite Phosphatase Antibiotic	Infection
Tetramisole hydrochloride is an orally active, selective inward rectifier potassium channel agonist with an EC₅₀ of approximately 30 μM for the Kir2.1 subunit. Tetramisole hydrochloride is also an anti-nematode agent that blocks neuromuscular transmission by non-competitive depolarization. Tetramisole hydrochloride promotes the forward transport of Kir2.1 channels, hyperpolarizes the resting potential (RP), shortens the action potential duration (APD), inhibits intracellular calcium overload and the PKA signaling pathway, and exerts anti-arrhythmic and anti-myocardial remodeling activities. Tetramisole hydrochloride can be used in cardiac electrophysiology research and research related to myocardial ischemia and heart failure .

HY-B1194A

Tetramisole	Cholinesterase (ChE) Insecticide	Neurological Disease
Tetramisole is an orally active, selective inward rectifier potassium channel agonist with an EC₅₀ of approximately 30 μM for the Kir2.1 subunit. Tetramisole is also an anti-nematode agent that blocks neuromuscular transmission by non-competitive depolarization. Tetramisole promotes the forward transport of Kir2.1 channels, hyperpolarizes the resting potential (RP), shortens the action potential duration (APD), inhibits intracellular calcium overload and the PKA signaling pathway, and exerts anti-arrhythmic and anti-myocardial remodeling activities. Tetramisole can be used in cardiac electrophysiology research and research related to myocardial ischemia and heart failure .

Cat. No.	Product Name	Type

HY-D0085

DiSC3(5) 5+ Cited Publications	Fluorescent Dyes/Probes
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)

5+ Cited Publications

Fluorescent Dyes/Probes

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 .

Cat. No.	Product Name	Target	Research Area