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Pathways Recommended:	Membrane Transporter/Ion Channel

Results for "

hERG potassium channels

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Calcium Channel (16) CRAC Channel (1) Potassium Channel (99) Sodium Channel (28) TRP Channel (3) 5-HT Receptor (12) Adrenergic Receptor (6) Antibiotic (2) Apoptosis (8) ASK1 (2) Autophagy (5) Bacterial (8) Caspase (3) CCR (1) Cytochrome P450 (9) Dipeptidyl Peptidase (2) Dopamine Receptor (5) Dopamine Transporter (4) Drug Derivative (1) Drug Metabolite (3) Endogenous Metabolite (2) Estrogen Receptor/ERR (1) GLP Receptor (1) Glucocorticoid Receptor (2) Glucokinase (1) Glutathione Peroxidase (1) Glycosidase (1) GPR119 (1) GPR68 (1) HCV Protease (2) HDAC (1) Histamine Receptor (18) Histone Demethylase (1) Histone Methyltransferase (1) HSP (4) iGluR (6) Interleukin Related (2) Isotope-Labeled Compounds (7) mAChR (8) MEK (1) Na+/Ca2+ Exchanger (3) Opioid Receptor (2) P-glycoprotein (1) p38 MAPK (1) Parasite (7) Phosphatase (1) Phosphodiesterase (PDE) (1) Phosphorylase (1) PI4K (1) Protease Activated Receptor (PAR) (1) Protein Arginine Deiminase (1) Ras (1) Reference Standards (14) Salt-inducible Kinase (SIK) (1) SARS-CoV (1) Serotonin Transporter (4) Sigma Receptor (1) SOS1 (1) Taste Receptor (3) Thyroid Hormone Receptor (1) TNF Receptor (3) Trk Receptor (4)
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144

Inhibitors & Agonists

Screening Libraries

Biochemical Assay Reagents

Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Potassium Channel Na+/K+ ATPase Chloride Channel Calcium Channel HCN Channel CRAC Channel TRP Channel Sodium Channel Piezo Channel

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-15551

E-4031 5 Publications Verification	Potassium Channel	Cardiovascular Disease
E-4031 is a selective *hERG* potassium channel blocker for use in class III anti-arrhythmic studies .

HY-153219A

P-CAB agent 2	Potassium Channel	Endocrinology
P-CAB agent 2 is a potent and orally active potassium-competitive acid blocker and a gastric acid secretion inhibitor. P-CAB agent 2 inhibits H ⁺/K ⁺-ATPase activity with an IC₅₀ value of <100 nM. P-CAB agent 2 inhibits the hERG potassium channel with an IC₅₀ value of 18.69 M. P-CAB agent 2 shows no acute toxicity and inhibits histamine (HY-B1204)-induced gastric acid secretion .

HY-153219

P-CAB agent 2 hydrochloride	Potassium Channel	Endocrinology
P-CAB agent 2 hydrochloride is a potent and orally active potassium-competitive acid blocker and a gastric acid secretion inhibitor. P-CAB agent 2 hydrochloride inhibits H ⁺/K ⁺-ATPase activity with an IC₅₀ value of <100 nM. P-CAB agent 2 hydrochloride inhibits the hERG potassium channel with an IC₅₀ value of 18.69 M. P-CAB agent 2 hydrochloride shows no acute toxicity and inhibits histamine (HY-B1204)-induced gastric acid secretion .

HY-108594

PD-118057	Potassium Channel	Metabolic Disease
PD-118057 is a **hERG channel** activator without causing hERG blockade. PD-118057 activates **hERG channel** to suppress changes in membrane excitability .

HY-15551A

E-4031 free base	Potassium Channel	Cardiovascular Disease
E-4031 free base is a selective *hERG* potassium channel blocker for use in class III anti-arrhythmic studies .

HY-15551R

E-4031 (Standard)	Potassium Channel	Cardiovascular Disease
E-4031 (Standard) is the analytical standard of E-4031. This product is intended for research and analytical applications. E-4031 is a selective hERG potassium channel blocker for use in class III anti-arrhythmic studies .

HY-A0148

Halofantrine SKF-102886 free base; WR-171669	Parasite Potassium Channel	Infection Cancer
Halofantrine (SKF-102886 free base) is a highly lipophilic antimalarial active against Chloroquine-resistant strains of Plasmodium falciparum . Halofantrine blocks *HERG* potassium channels .

HY-176881

ASK1-IN-10	ASK1	Inflammation/Immunology
ASK1-IN-10 (Compound 27) is an apoptosis signal-regulating kinase 1 (ASK1) inhibitor with an IC₅₀ <200 nM. ASK1-IN-10 also shows inhibitory activity to hERG potassium channels. ASK1-IN-10 can be used for the research of inflammation .

HY-132201

MK-8153	Potassium Channel	Metabolic Disease
MK-8153 is a potent, selective and orally active inhibitor of *renal outer medullary potassium channel* (ROMK), with IC₅₀*s of 5 nM, 34 μM for ROMK electrophysiology (EP) and hERG* EP, respectively. MK-8153 can be used as the diuretic/atriuretic .

HY-176882

ASK1-IN-11	ASK1 TNF Receptor	Inflammation/Immunology
ASK1-IN-11 (Compound 7) is an apoptosis signal-regulating kinase 1 (ASK1) inhibitor with an IC₅₀ <200 nM. ASK1-IN-11 also shows inhibitory activities to TNF-α, MYLK/MLCK Kinase and hERG potassium channels . ASK1-IN-11 can be used for the research of inflammation .

HY-B1167A

Ajmaline hydrochloride Cardiorythmine hydrochloride; (+)-Ajmaline hydrochloride	Others	Cardiovascular Disease
Ajmaline hydrochloride is a Class Ia antiarrhythmic agent. It inhibits HERG potassium channels with IC50s of 1.0 μmol/l and 42.3 μmol/l in HEK cells and moth spider oocytes respectively. The inhibitory effect of Ajmaline hydrochloride is rapid, reversible, and positive frequency dependent. It acts primarily on the open state of the HERG channel and may also be combined with the inactivated state. The inhibitory effect of ajmaline hydrochloride is dependent on aromatic residues in the S6 domain, and the sensitivity is significantly reduced in the inactivation-deficient HERG S620T channel. It can also slightly affect the activation voltage of HERG channels. Ajmaline hydrochloride's inhibitory effect on HERG channels may contribute to both its potent antiarrhythmic effects and its potential proarrhythmic risk.

HY-108586

NS3623	Potassium Channel	Neurological Disease
NS3623 is an activator of human ether-a-go-go-related gene (hERG1/K_V11.1) potassium channels. NS3623 activates the IKr and Ito currents and has antiarrhythmic effect. NS3623 has a dual mode of action, being an inhibitor of hERG1 channels .

HY-B2136

Tannic acid 5+ Cited Publications	Potassium Channel	Inflammation/Immunology Cancer
Tannic acid is a novel **hERG channel blocker with IC₅₀** of 3.4 μM.

HY-N7511

O-Nornuciferine	Potassium Channel Endogenous Metabolite	Metabolic Disease
O-Nornuciferine, an aporphine-type alkaloid from lotus leaf, is a potent *hERG* channel inhibitor .

HY-118172

PD-307243	Potassium Channel	Cardiovascular Disease
PD-307243 is a **hERG channel** activator. PD-307243 can be used for research of arrhythmias .

HY-12082A

GSK369796 Dihydrochloride	Potassium Channel Parasite	Infection
GSK369796 Dihydrochloride is an affordable and effective antimalarial and inhibits **hERG potassium ion channel repolarization with an IC₅₀** of 7.5 μM.

HY-P5177

GsAF-II	Sodium Channel Potassium Channel	Neurological Disease
GsAF-II is a peptide toxin that blocks hERG1 subtype potassium channels in a voltage-dependent manner. GsAF-II blocks Nav1.x subtype sodium channels .

HY-175289

hERG-IN-3	Potassium Channel Sodium Channel Adrenergic Receptor	Neurological Disease
hERG-IN-3 is an orally active *hERG* blocker with an IC₅₀ of 44.5 nM. hERG-IN-3 exhibits a K_i for β2-adrenergic receptor of 14 nM. hERG-IN-3 exhibits the skeletal muscle Nav1.4 and sodium channel-blocking activities (IC₅₀ = 4.4 μM, 3-fold increasement than hNav1.5). hERG-IN-3 displays a potent antimyotonic activity in an animal model. hERG-IN-3 can be used for the study of Myotonia Congenita .

HY-173330

HDAC-IN-89	HDAC	Cancer
HDAC-IN-89 is an inhibitor of HDAC1 (IC₅₀: 0.95 nM), HDAC2 (IC₅₀: 0.86 nM), HDAC3 (IC₅₀: 1.06 nM) and HDAC8 (IC₅₀: 4.24 nM). HDAC-IN-89 blocks the cell cycle and induces apoptosis. HDAC-IN-89 has anti-tumor activity .

HY-16915

RPR-260243 1 Publications Verification	Potassium Channel	Cardiovascular Disease
RPR-260243, a potent activator of human ether-a-go-go-related gene (hERG), slows deactivation and attenuates inactivation of hERG1 channels. RPR260243-modified HERG currents are inhibited by Dofetilide (IC₅₀=58 nM). RPR260243 displays no activator-like effects on other voltage-dependent ion channels, including the closely related ERG3 K+ channel . RPR-260243 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-124702

ICA-105574 1 Publications Verification	Potassium Channel	Cardiovascular Disease
ICA-105574 is a potent and efficacious **hERG channel** activator. The primary mechanism by which ICA-105574 potentiates hERG channel activity is by removing hERG channel inactivation. ICA-105574 steeply potentiates current amplitudes more than 10-fold with an EC₅₀ value of 0.5 +/- 0.1 μM and a Hill slope (n(H)) of 3.3 +/- 0.2. ICA-105574 can prevent arrhythmias induced by cardiac delayed repolarization. ICA-105574 shortens action potential duration in ventricular myocytes concentration-dependently .

HY-169624

GPV574	Potassium Channel	Cardiovascular Disease
GPV574 is a derivative of the antiarrhythmic compound propafenone, capable of inhibiting *HERG* channels (IC₅₀ = 5.04 μM).

HY-111747

TBAJ-587 3 Publications Verification	Bacterial	Infection Cardiovascular Disease
TBAJ-587, a potent anti-tuberculosis agent, inhibits M.tb strain H37Rv growth with MIC₉₀s of 0.006 and <0.02 μg/mL in MABA and LORA assay, respectively. TBAJ-587 inhibits hERG channel minimally, attenuates inhibition of the cardiac potassium channel protein coded by the hERG, which is important for cardiac repolarization .

HY-19927A

DA-6886 monohydrochloride	5-HT Receptor	Neurological Disease Endocrinology
DA-6886 is a 5-Hydroxytryptamine receptor 4 (5-HT4) agonist. DA-6886 induces relaxation of the rat oesophagus preparation in a 5-HT4 receptor antagonist-sensitive manner. The evaluation of DA-6886 in CHO cells expressing hERG channels reveals that it inhibits hERG channel current with an pIC₅₀ value of 4.3, indicating that the compound is 1000-fold more selective for the 5-HT4 receptor over hERG channels. DA-6886 can be used in the study of constipated irritable bowel syndrome .

HY-112075

Lidoflazine	Potassium Channel Calcium Channel	Cardiovascular Disease
Lidoflazine is a high affinity blocker of the HERG (human ether-a-go-go-related gene) K ⁺ channel. Lidoflazine is an antianginal calcium channel blocker that carries a significant risk of QT interval prolongation and ventricular arrhythmia .

HY-120375

LUF7346	Potassium Channel	Cardiovascular Disease
LUF7346 is a potent Kv11.1 (hERG) channel negative allosteric modulator, with an IC₅₀ of 35.6 ± 3.2 nM .

HY-113673

A-935142	Potassium Channel	Cardiovascular Disease
A-935142 is a human ether-a-go-go-related gene (hERG, Kv 11.1) channel activator. A-935142 enhances hERG current in a complex manner by facilitation of activation, reduction of inactivation, and slowing of deactivation, and abbreviates atrial and ventricular repolarization .

HY-147256

Cavutilide Niferidil	Potassium Channel	Cardiovascular Disease
Cavutilide (Niferidil) is a class III antiarrhythmic agent that inhibits **hERG K ⁺ channel**. Cavutilide has the potential for the study of persistent atrial fibrillation .

HY-122024

AZSMO-23	Potassium Channel	Cardiovascular Disease
AZSMO-23 is a potent **hERG K ⁺ channel** activator. AZSMO-23 activats WT hERG pre-pulse and tail current with EC₅₀ values of 28.6, 11.2 µM, respectively. AZSMO-23 has the potential for the research of long QT syndrome .

HY-156976A

Sulcardine hydrochloride	Calcium Channel Sodium Channel	Cardiovascular Disease
Sulcardine hydrochloride is a multi-ion channel blocker that can reduce I_Na and I_Ca with IC₅₀ values of 26.9 µM and 69.2 µM, respectively. Sulcardine hydrochloride is a potent hNav1.5 channel blocker with a mild inhibitory effect on *hERG* channels. Sulcardine hydrochloride has anti-arrhythmic effects .

HY-156976

Sulcardine	Calcium Channel Sodium Channel	Cardiovascular Disease
Sulcardine is a multi-ion channel blocker that can reduce I_Na and I_Ca with IC₅₀ values of 26.9 µM and 69.2 µM, respectively. Sulcardine is a potent hNav1.5 channel blocker with a mild inhibitory effect on *hERG* channels. Sulcardine has anti-arrhythmic effects .

HY-124687

ROMK-IN-32	Potassium Channel	Cardiovascular Disease
ROMK-IN-32 is a renal outer medullary potassium channel (ROMK) inhibitor with an IC₅₀ of 35 nM. ROMK-IN-32 also inhibits hERG with an IC₅₀ of 22 μM .

HY-B1482A

Mesoridazine TPS-23	Potassium Channel	Neurological Disease
Mesoridazine (TPS-23) , a metabolite of Thioridazine (HY-B0965A), acts as an orally active phenothiazine antipsychotic agent. Mesoridazine is a potent and rapid open-channel blocker of human ether-a-go-go related gene (hERG) channels and blocks hERG currents with an IC₅₀ of 550 nM (at 0 mV) in human embryonic kidney 293 cells .Mesoridazine can be used for the research of schizophrenia, as well as certain other psychiatric disorders .

HY-B1482

Mesoridazine benzenesulfonate TPS-23 benzenesulfonate	Potassium Channel	Neurological Disease
Mesoridazine (TPS-23) benzenesulfonate, a metabolite of Thioridazine (HY-B0965A), acts as an orally active phenothiazine antipsychotic agent. Mesoridazine benzenesulfonate is a potent and rapid open-channel blocker of human ether-a-go-go related gene (hERG) channels and blocks hERG currents with an IC₅₀ of 550 nM (at 0 mV) in human embryonic kidney 293 cells .Mesoridazine benzenesulfonate can be used for the research of schizophrenia, as well as certain other psychiatric disorders .

HY-N5006

Guanfu base G	Potassium Channel	Cardiovascular Disease
Guanfu base G is an antiarrhythmic alkaloid isolated from Aconitum coreanum. Guanfu base G inhibits *HERG* channel current with an IC₅₀ of 17.9 μM .

HY-133925

6-O-Desmethyl donepezil	Drug Metabolite Potassium Channel	Inflammation/Immunology
6-O-Desmethyl donepezil is the metabolite of Donepezil (HY-14566). 6-O-Desmethyl donepezil is an inhibitor for **hERG channel with an IC₅₀** of 1 μM .

HY-B0369AS

Orphenadrine-d3 citrate	Isotope-Labeled Compounds iGluR	Neurological Disease
Orphenadrine-d₃ (citrate) is the deuterium labeled Orphenadrine citrate. Orphenadrine citrate is a NMDA receptor antagonist with Ki of 6.0 +/- 0.7 μM, HERG potassium channel blocker.

HY-133926

5-O-Desmethyl donepezil	Drug Metabolite Potassium Channel	Inflammation/Immunology
5-O-Desmethyl donepezil is a metabolite of Donepezil (HY-14566). 5-O-Desmethyl donepezil is an inhibitor for *hERG* channel with an IC₅₀ of 1.5 μM .

HY-A0148A

Halofantrine hydrochloride 2 Publications Verification SKF-102886; WR-171669 hydrochloride	Parasite	Infection
Halofantrine hydrochloride (SKF-102886) is a blocker of delayed rectifier potassium current via the inhibition of human-ether-a-go-go-related gene (HERG) channel and a potent antimalarial compound .

HY-122167

L-869298	Phosphodiesterase (PDE)	Inflammation/Immunology
L-869298 is a potent and selective PDE4 inhibitor with an IC₅₀ of 0.5 nM for PDE4A. L-869298 shows less active against hERG potassium channel .

HY-172374

KV1.3-IN-2	Potassium Channel	Inflammation/Immunology
KV1.3-IN-2 (Compound I) inhibits kv1.3 potassium channel without affecting **hERG channel**. KV1.3-IN-2 can be used in research of immune-related diseases such as psoriasis, rheumatoid arthritis, and systemic lupus erythematosus .

HY-B1482AS

Mesoridazine-d3	Isotope-Labeled Compounds Potassium Channel	Neurological Disease
Mesoridazine-d₃ is the deuterium labeled Mesoridazine (HY-B1482A). Mesoridazine (TPS-23) , a metabolite of Thioridazine (HY-B0965A), acts as an orally active phenothiazine antipsychotic agent. Mesoridazine is a potent and rapid open-channel blocker of human ether-a-go-go related gene (hERG) channels and blocks hERG currents with an IC₅₀ of 550 nM (at 0 mV) in human embryonic kidney 293 cells .Mesoridazine can be used for the research of schizophrenia, as well as certain other psychiatric disorders .

HY-P1440A

BeKm-1 TFA	Potassium Channel	Neurological Disease
BeKm-1 TFA is a potent and selective KV11.1 (hERG) channel blocker. BeKm-1 TFA is selective for KV11.1 over a panel of 14 other potassium channels. BeKm-1 TFA dose-dependently prolongs QTc interval in isolated rabbit heart.

HY-100545

BAPTA-AM Maximum Cited Publications 101 Publications Verification	Potassium Channel	Cardiovascular Disease
BAPTA-AM is a well-known membrane permeable Ca ²⁺ chelator. BAPTA-AM inhibits *hERG* channels, hKv1.3 and hKv1.5 channels in HEK 293 cells with IC₅₀s of 1.3 μM, 1.45 μM and 1.23 μM, respectively .

HY-163590

PRMT5-IN-41	Histone Methyltransferase Potassium Channel	Cancer
PRMT5-IN-41 (compound 130) is a potent and orally active PRMT5 inhibitor. PRMT5-IN-41 inhibits hERG ion channel with IC₅₀ value of 1.36 µM .

HY-162555

BMS-986308	Potassium Channel	Cardiovascular Disease
BMS-986308 is a selective and orally active renal outer medullary potassium (ROMK) channel inhibitor. BMS-986308 is selective for ROMK over hERG. BMS-986308 can be used for heart failure research .

HY-14848A

Naluzotan hydrochloride PRX 00023 hydrochloride	5-HT Receptor Potassium Channel	Neurological Disease
Naluzotan hydrochloride is a novel, potent, and selective amidosulfonamide 5-HT1A agonist with IC₅₀ and K_i of appr 20 nM and 5.1 nM, used for the treatment of anxiety and depression; Also a weak **hERG K ⁺ channel** blocker, with IC₅₀ of 3800 nM.

HY-146380

S1427	Histone Demethylase	Cancer
S1427 is a tranylcypromine-derived LSD1 inhibitor with the IC₅₀ of 390 nM and K_i of 80 nM. S1427 exhibits desirable hERG channel inhibition and microsomal stability profiles. Inhibition of LSD1 partially reduces the proliferation of cancer cells .

HY-106912A

L-706000 free base MK 499 free base	Potassium Channel	Cardiovascular Disease
L-706000 (MK 499) free base is a potent **hERG channel blocker with an IC₅₀** of 32 nM. L-706000 free base is a class III antiarrhythmic agent that can be used for the study of malignant ventricular tachyarrhythmias .

HY-101622

5-HT6/7 antagonist 1	5-HT Receptor Dopamine Receptor	Neurological Disease
5-HT6/7 antagonist 1 is a multifunctional ligand that antagonizes 5-HT6/7/2A and D2 receptors, without interacting with M1 receptors and hERG channels.

Cat. No.	Product Name

HY-L923

Ion Channel Lead-like Compound Library

9000 compounds

Ion channels are key proteins on the cell membrane that regulate the flow of ions across membranes. They participate in nearly all physiological processes, including nerve conduction, muscle contraction, heart rhythm, and pain perception. Abnormalities in their function can lead to various serious diseases such as arrhythmia, epilepsy, hypertension, neuropathic pain, and cancer. Therefore, ion channels are highly valuable drug targets—over 15% of approved drugs target ion channels currently, demonstrating their irreplaceable therapeutic value in cardiovascular, neurological, and analgesic fields.

MCE has collected a library of over 5,000 reported ion channel-related bioactive compounds targeting major sites such as Na+ channels, K+ channels, Ca2+ channels, GABA receptors, iGluRs, and others. Using AI models, these compounds are characterized through both 2D representations (molecular fingerprints, pharmacophores) and 3D representations (3D conformation) to screen for a collection of lead-like compounds highly similar to known active molecules. Additionally, an hERG channel prediction algorithm integrating XGB and ISE mapping strategy is employed to assess and exclude potential cardiotoxicity in the library.. This step significantly reduces safety risks in subsequent screenings, particularly for ion channel drug development related to cardiovascular systems (e.g., Nav1.5, Cav1.2), effectively minimizing failures due to hERG inhibition and serving as a valuable tool for ion channel drug screening.

HY-L225

Cardiotoxic Compound Library

257 compounds

Drug development is both expensive and time-consuming, with approximately one-third of drug discontinuations caused by severe adverse drug reactions (ADRs). Among these, drug-induced cardiotoxicity (DICT) is one of the primary reasons for late-stage clinical drug failures and market withdrawals. To date, cardiotoxicity has been observed in multiple drug classes, such as anticancer drugs, antipsychotics, antidepressants, antibiotics, and neurodegenerative disease medications. To reduce cardiac ADRs, it is crucial to determine the clinical relevance of DICT to treatment, elucidate the underlying molecular mechanisms, identify reliable biomarkers, and develop new diagnostic and therapeutic approaches.

MCE offers 257 cardiotoxicity compounds, including some FDA-approved drugs as well as inhibitors/blockers of the hERG potassium channel.

Cat. No.	Product Name	Type

HY-100545

BAPTA-AM 100+ Cited Publications	Chelators
BAPTA-AM is a well-known membrane permeable Ca ²⁺ chelator. BAPTA-AM inhibits *hERG* channels, hKv1.3 and hKv1.5 channels in HEK 293 cells with IC₅₀s of 1.3 μM, 1.45 μM and 1.23 μM, respectively .

HY-100545R

BAPTA-AM (Standard)	Chelators
BAPTA-AM (Standard) is the analytical standard of BAPTA-AM. This product is intended for research and analytical applications. BAPTA-AM is a well-known membrane permeable Ca2+ chelator. BAPTA-AM inhibits hERG channels, hKv1.3 and hKv1.5 channels in HEK 293 cells with IC50s of 1.3 μM, 1.45 μM and 1.23 μM, respectively .

Cat. No.	Product Name	Target	Research Area

HY-P5177

GsAF-II	Sodium Channel Potassium Channel	Neurological Disease
GsAF-II is a peptide toxin that blocks hERG1 subtype potassium channels in a voltage-dependent manner. GsAF-II blocks Nav1.x subtype sodium channels .

HY-P1440A

BeKm-1 TFA	Potassium Channel	Neurological Disease
BeKm-1 TFA is a potent and selective KV11.1 (hERG) channel blocker. BeKm-1 TFA is selective for KV11.1 over a panel of 14 other potassium channels. BeKm-1 TFA dose-dependently prolongs QTc interval in isolated rabbit heart.

HY-P5795

GsAF-I	Sodium Channel Potassium Channel	Neurological Disease
GsAF-I is a potent Na_v and *hERG1* channels blocker with IC₅₀s of 0.36, 0.6, 1.28, 0.33, 1.2, 0.04 and 4.8 μM against Na_v1.1, Na_v1.2, Na_v1.3, Na_v1.4, Na_v1.6, Na_v1.7 and hERG1, respectively .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-B2136

Tannic acid 5+ Cited Publications	Liliaceae Classification of Application Fields Anti-aging Ketones, Aldehydes, Acids Source classification Phenols Polyphenols Polygonatum odoratum (Mill.) Druce Plants Inflammation/Immunology Disease Research Fields Cancer	Potassium Channel
Tannic acid is a novel **hERG channel blocker with IC₅₀** of 3.4 μM.

HY-N7511

O-Nornuciferine	Alkaloids Monophenols other families Classification of Application Fields Source classification Phenols Metabolic Disease Plants Isoquinoline Alkaloids Disease Research Fields	Potassium Channel Endogenous Metabolite
O-Nornuciferine, an aporphine-type alkaloid from lotus leaf, is a potent *hERG* channel inhibitor .

HY-N5006

Guanfu base G	Cardiovascular Disease Alkaloids Classification of Application Fields Source classification Ranunculaceae Aconitum carmichaeli Debx. Plants Disease Research Fields Indole Alkaloids	Potassium Channel
Guanfu base G is an antiarrhythmic alkaloid isolated from Aconitum coreanum. Guanfu base G inhibits *HERG* channel current with an IC₅₀ of 17.9 μM .

HY-B1167

Ajmaline Cardiorythmine; (+)-Ajmaline	Apocynaceae Cardiovascular Disease Alkaloids Piperidine Alkaloids Rauvolfia serpentina Classification of Application Fields Source classification Plants Disease Research Fields Indole Alkaloids	Sodium Channel
Ajmaline (Cardiorythmine) is a sodium channel blocking, class 1A anti-arrhythmic agent. Ajmaline blocks HERG currents with an IC₅₀ of 1 μM in HEK cells and 42.3 μM in Xenopus oocytes. Ajmaline can be used for the research of the ventricular tachyarrhythmia .

HY-N1934

Dihydroberberine	Cardiovascular Disease Alkaloids other families Classification of Application Fields Source classification Plants Isoquinoline Alkaloids Inflammation/Immunology Disease Research Fields	Potassium Channel HSP
Dihydroberberine is a naturally occurring isoquinoline alkaloid with anti-inflammatory, anti-atherosclerotic, hypolipidemic and anti-tumor activities. Dihydroberberine inhibits the human ether-related gene (hERG) channel and significantly reduces the expression of heat shock protein 90 (Hsp90) and its interaction with hERG. Dihydroberberine also blocks the TLR4/MyD88/NF-κB signaling pathway to reduce pro-inflammatory cytokines and immunoglobulins, and has inhibitory effects on DSS (HY-116282C)-induced experimental colitis. Dihydroberberine also increases the sensitivity of lung cancer to sunitinib (HY-10255A), with synergistic efficacy .

HY-N1483

Guanfu base A	Cardiovascular Disease Alkaloids Classification of Application Fields Other Alkaloids Ranunculaceae Source classification Aconitum carmichaeli Debx. Plants Disease Research Fields	Potassium Channel
Guanfu base A is an antiarrhythmic alkaloid isolated from Aconitum coreanum and is a potent noncompetitive CYP2D6 inhibitor, with a K_i of 1.20 μM in human liver microsomes (HLMs) and a K_i of 0.37 μM for the human recombinant form (rCYP2D6). Guanfu base A is also a potent competitive inhibitor of CYP2D in monkey (K_i of 0.38 μM) and dog (K_i of 2.4 μM) microsomes . Guanfu base A also inhibits *HERG* channel current .

HY-B1167A

Ajmaline hydrochloride Cardiorythmine hydrochloride; (+)-Ajmaline hydrochloride	Rauvolfia verticillata (Lour.) Baill. Apocynaceae Natural Products Source classification Plants	Others
Ajmaline hydrochloride is a Class Ia antiarrhythmic agent. It inhibits HERG potassium channels with IC50s of 1.0 μmol/l and 42.3 μmol/l in HEK cells and moth spider oocytes respectively. The inhibitory effect of Ajmaline hydrochloride is rapid, reversible, and positive frequency dependent. It acts primarily on the open state of the HERG channel and may also be combined with the inactivated state. The inhibitory effect of ajmaline hydrochloride is dependent on aromatic residues in the S6 domain, and the sensitivity is significantly reduced in the inactivation-deficient HERG S620T channel. It can also slightly affect the activation voltage of HERG channels. Ajmaline hydrochloride's inhibitory effect on HERG channels may contribute to both its potent antiarrhythmic effects and its potential proarrhythmic risk.

HY-B1167R

Ajmaline (Standard) Cardiorythmine (Standard); (+)-Ajmaline (Standard)	Apocynaceae Alkaloids Piperidine Alkaloids Rauvolfia serpentina Source classification Plants Indole Alkaloids	Reference Standards Sodium Channel
Ajmaline (Standard) is the analytical standard of Ajmaline. This product is intended for research and analytical applications. Ajmaline (Cardiorythmine) is a sodium channel blocking, class 1A anti-arrhythmic agent. Ajmaline blocks HERG currents with an IC₅₀ of 1 μM in HEK cells and 42.3 μM in Xenopus oocytes. Ajmaline can be used for the research of the ventricular tachyarrhythmia .

HY-N1934R

Dihydroberberine (Standard)	Alkaloids other families Source classification Plants Isoquinoline Alkaloids	Reference Standards Potassium Channel HSP
Dihydroberberine (Standard) is the analytical standard of Dihydroberberine. This product is intended for research and analytical applications. Dihydroberberine is a naturally occurring isoquinoline alkaloid with anti-inflammatory, anti-atherosclerotic, hypolipidemic and anti-tumor activities. Dihydroberberine inhibits the human ether-related gene (hERG) channel and significantly reduces the expression of heat shock protein 90 (Hsp90) and its interaction with hERG. Dihydroberberine also blocks the TLR4/MyD88/NF-κB signaling pathway to reduce pro-inflammatory cytokines and immunoglobulins, and has inhibitory effects on DSS (HY-116282C)-induced experimental colitis. Dihydroberberine also increases the sensitivity of lung cancer to sunitinib (HY-10255A), with synergistic efficacy .

HY-W041470R

4-Methyl-1-phenyl-2-pentanone (Standard)	Ketones, Aldehydes, Acids Source classification Endogenous metabolite	Reference Standards Endogenous Metabolite
Chlorpromazine (hydrochloride) (Standard) is the analytical standard of Chlorpromazine (hydrochloride). This product is intended for research and analytical applications. Chlorpromazine hydrochloride is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine hydrochloride exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine hydrochloride also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine hydrochloride also can inhibit clathrin-mediated endocytosis .

Cat. No.	Product Name	Chemical Structure

HY-B0527AS

Amitriptyline-d6 hydrochloride

Amitriptyline-d₆ hydrochloride is the deuterium labeled Amitriptyline hydrochloride (HY-B0527A). Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (K_i = 3.45 nM) and NET (K_i = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with K_i = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (K_i = 11-24 nM), H1 receptors (K_i = 0.5-1.1 nM), adrenergic α1 receptors (K_i = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC₅₀ = 4.78 μM) and it has cardiotoxicity.

HY-B0369AS

Orphenadrine-d3 citrate
Orphenadrine-d₃ (citrate) is the deuterium labeled Orphenadrine citrate. Orphenadrine citrate is a NMDA receptor antagonist with Ki of 6.0 +/- 0.7 μM, HERG potassium channel blocker.

HY-B1482AS

Mesoridazine-d3

Mesoridazine-d₃ is the deuterium labeled Mesoridazine (HY-B1482A). Mesoridazine (TPS-23) , a metabolite of Thioridazine (HY-B0965A), acts as an orally active phenothiazine antipsychotic agent. Mesoridazine is a potent and rapid open-channel blocker of human ether-a-go-go related gene (hERG) channels and blocks hERG currents with an IC₅₀ of 550 nM (at 0 mV) in human embryonic kidney 293 cells .Mesoridazine can be used for the research of schizophrenia, as well as certain other psychiatric disorders .

HY-103309S

ML218-d9

ML218-d₉ is the deuterium labeled ML218. ML218 is a potent, selective and orally active T-type Ca2+ channels (Cav3.1, Cav3.2, Cav3.3) inhibitor with IC₅₀s of 310 nM and 270 nM for Cav3.2 and Cav3.3, respectively. ML218 inhibits the burst activity in subthalamic nucleus (STN) neurons. ML218 has no significant inhibition of L- or N-type calcium channels, KATP or hERG potassium channels. ML218 can penetrate the blood-brain barrier .

HY-12532S

Astemizole-d3
Astemizole-d₃ is the deuterium labeled Astemizole. Astemizole (R 43512), a second-generation antihistamine drug to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC₅₀ of 4 nM. Astemizole also shows potent hERG K+ channel blocking activity with an IC₅₀ of 0.9 nM. Astemizole has antipruritic effects .

HY-B1193S

Terfenadine-d3

Terfenadine-d₃ ((±)-Terfenadine-d₃) is the deuterium labeled Terfenadine. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC₅₀ of 204 nM . Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9[2].

HY-W710915

Aprindine hydrochloride-d10

Aprindine hydrochloride-d₁₀ is the deuterium labeled Aprindine hydrochloride (HY-A0236A). Aprindine hydrochloride is a class I-b anti-arrhythmic agent and a hERG channel blocker with an IC₅₀ of 0.23 μM. Aprindine hydrochloride has inhibitory effects on Na+/Ca2+ exchanger currents, which is partly responsible for their antiarrhythmic and cardioprotective effects. Aprindine hydrochloride is widely used for trial and ventricular tachyarrhythmias research research.

HY-18600AS

Azimilide-d8 dihydrochloride

Azimilide-d₈ (NE-10064-d₈) dihydrochloride is the deuterium labeled Azimilide dihydrochloride (HY-18600A). Azimilide dihydrochloride is a class III antiarrhythmic agent, which works by blocking potassium channels in the heart. Azimilide dihydrochloride is a dual blocker of I_Ks (IC₅₀ = 2.6 μM (2mM [K⁺]ₑ)) and I_Kr (IC₅₀ = 1 μM (4 mM [K⁺])). Azimilide dihydrochloride blocked HERG channel at 0.1 and 1 Hz with IC₅₀s of 1.4 μM and 5.2 μM respectively. Azimilide dihydrochloride also inhibits L-type calcium current (I_Ca) (IC₅₀ = 17.8 μM) and sodium current (I_Na) (IC₅₀ = 19 μM). Azimilide dihydrochloride can be used for the study of atrial fibrillation and ventricular fibrillation .

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