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Pathways Recommended:	Membrane Transporter/Ion Channel

Results for "

hERG channel blocker

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (9) Adrenergic Receptor (5) Apoptosis (7) Arrestin (1) Autophagy (3) Calcium Channel (10) Caspase (3) Cytochrome P450 (3) Dopamine Receptor (3) Dopamine Transporter (4) Drug Metabolite (1) Endogenous Metabolite (1) Environmental Pollutants (1) Histamine Receptor (15) HSP (2) IFNAR (1) iGluR (1) Interleukin Related (1) IRAK (1) Isotope-Labeled Compounds (7) mAChR (8) Na+/Ca2+ Exchanger (3) Opioid Receptor (1) Parasite (1) Potassium Channel (48) Reference Standards (12) SARS-CoV (1) Serotonin Transporter (5) Sodium Channel (24) TNF Receptor (2) Trk Receptor (4)
By Research Areas:	Cancer (10) Cardiovascular Disease (27) Endocrinology (16) Infection (2) Inflammation/Immunology (20) Metabolic Disease (1) Neurological Disease (24)

By Targets:

5-HT Receptor (9)

Adrenergic Receptor (5)

Apoptosis (7)

Arrestin (1)

Autophagy (3)

Calcium Channel (10)

Caspase (3)

Cytochrome P450 (3)

Dopamine Receptor (3)

Dopamine Transporter (4)

Drug Metabolite (1)

Endogenous Metabolite (1)

Environmental Pollutants (1)

Histamine Receptor (15)

HSP (2)

IFNAR (1)

iGluR (1)

Interleukin Related (1)

IRAK (1)

Isotope-Labeled Compounds (7)

mAChR (8)

Na+/Ca2+ Exchanger (3)

Opioid Receptor (1)

Parasite (1)

Potassium Channel (48)

Reference Standards (12)

SARS-CoV (1)

Serotonin Transporter (5)

Sodium Channel (24)

TNF Receptor (2)

Trk Receptor (4)

By Research Areas:

Cancer (10)

Cardiovascular Disease (27)

Endocrinology (16)

Infection (2)

Inflammation/Immunology (20)

Metabolic Disease (1)

Neurological Disease (24)

Inhibitors & Agonists

Screening Libraries

Peptides

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Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-12708

Chlorpromazine Maximum Cited Publications 128 Publications Verification	Dopamine Receptor Cytochrome P450 Autophagy 5-HT Receptor	Cardiovascular Disease Neurological Disease Cancer
Chlorpromazine is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT_2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine 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 also blocks hNa_v1.7 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 also can inhibit clathrin-mediated endocytosis .

HY-B0407A

Chlorpromazine hydrochloride Maximum Cited Publications 128 Publications Verification	Dopamine Receptor Autophagy Cytochrome P450 5-HT Receptor	Cardiovascular Disease Neurological Disease Cancer
Chlorpromazine hydrochloride is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT_2A, 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 hNa_v1.7 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 .

HY-B2136

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

HY-15551

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

HY-B1193

Terfenadine 4 Publications Verification (±)-Terfenadine; MDL-991	Potassium Channel Histamine Receptor Na+/Ca2+ Exchanger Caspase Apoptosis	Inflammation/Immunology Endocrinology Cancer
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 Ca ²⁺ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9 .

HY-B0527A

Amitriptyline hydrochloride 5+ Cited Publications	Serotonin Transporter 5-HT Receptor mAChR Histamine Receptor Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis	Neurological Disease Inflammation/Immunology Endocrinology
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-B0527

Amitriptyline 5+ Cited Publications	Serotonin Transporter Trk Receptor Sodium Channel 5-HT Receptor Histamine Receptor Adrenergic Receptor mAChR Potassium Channel Dopamine Transporter Apoptosis	Neurological Disease Inflammation/Immunology Endocrinology
Amitriptyline is an orally active tricyclic antidepressant (TCA). Amitriptyline 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 is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline can reduce inflammation, angiogenesis and fibrosis. Amitriptyline binds to DAT (with K_i = 2.58 μM). Amitriptyline 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 can block sodium channels and hERG potassium channel (IC₅₀ = 4.78 μM) and it has cardiotoxicity .

HY-12532

Astemizole 5+ Cited Publications R 43512	Histamine Receptor Potassium Channel	Inflammation/Immunology Endocrinology
Astemizole (R 43512), a second-generation antihistamine agent 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-N1934

Dihydroberberine	Potassium Channel HSP	Cardiovascular Disease Inflammation/Immunology Cancer
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-B0480

Brompheniramine maleate 2 Publications Verification (±)-Brompheniramine maleate	Histamine Receptor mAChR Potassium Channel Sodium Channel Calcium Channel	Neurological Disease Inflammation/Immunology Endocrinology
Brompheniramine ((±)-Brompheniramine) maleate is a potent and orally active antihistamine of the alkylamine class. Brompheniramine maleate is a selective histamine H1 receptor antagonist with a K_d of 6.06 nM. Brompheniramine maleate can block the **hERG channels*, calcium channels, and sodium channels* with IC₅₀s of 0.90 μM, 16.12 μM and 21.26 μM, respectively. Brompheniramine maleate has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research .

HY-B1167

Ajmaline Cardiorythmine; (+)-Ajmaline	Sodium Channel	Cardiovascular Disease
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-12533

Disopyramide 2 Publications Verification Dicorantil; SC-7031	Sodium Channel Potassium Channel	Cardiovascular Disease
Disopyramide (Dicorantil) is a class IA antiarrhythmic agent with efficacy in ventricular and atrial arrhythmias. Disopyramide blocks the fast inward sodium current of cardiac muscle and prolongs the duration of cardiac action potentials. Disopyramide inhibits HERG encoded potassium channels. Disopyramide also exhibits complex protein binding, and has a potent negative inotropic action .

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-12533A

Disopyramide phosphate 2 Publications Verification Dicorantil phosphate; SC-7031 phosphate	Potassium Channel Sodium Channel	Cardiovascular Disease
Disopyramide phosphate is a class IA antiarrhythmic agent with efficacy in ventricular and atrial arrhythmias. Disopyramide phosphate blocks the fast inward sodium current of cardiac muscle and prolongs the duration of cardiac action potentials. Disopyramide phosphate inhibits HERG encoded potassium channels. Disopyramide phosphate also exhibits complex protein binding, and has a potent negative inotropic action .

HY-136832

Noribogaine hydrochloride	Serotonin Transporter Potassium Channel Arrestin Opioid Receptor	Cardiovascular Disease Neurological Disease
Noribogaine hydrochloride is an orally active, blood-brain barrier permeable SERT inhibitor (IC₅₀=50-300 nM) and *hERG* channel blocker. Noribogaine hydrochloride enhances serotonergic transmission, activates the κ-opioid receptor (OPRK) G protein signaling pathway and inhibits β-arrestin recruitment. Meanwhile, Noribogaine hydrochloride blocks the μ-opioid receptor (OPRM) signaling pathway as well as ion channels associated with cardiac repolarization. Noribogaine hydrochloride induces neuritogenesis, upregulates GDNF mRNA expression, and modulates opioid tolerance. Noribogaine hydrochloride reduces alcohol-seeking behavior in experimental animals, and is widely used in studies related to depression, addiction, alcoholism, and cardiotoxicity .

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-18600A

Azimilide dihydrochloride 2 Publications Verification NE-10064 dihydrochloride	Potassium Channel Calcium Channel Sodium Channel	Cardiovascular Disease
Azimilide (NE-10064) 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 .

HY-B0480A

Brompheniramine 2 Publications Verification (±)-Brompheniramine	Histamine Receptor mAChR Potassium Channel Sodium Channel Calcium Channel	Neurological Disease Inflammation/Immunology Endocrinology
Brompheniramine ((±)-Brompheniramine) is a potent and orally active antihistamine of the alkylamine class. Brompheniramine is a selective histamine H1 receptor antagonist with a K_d of 6.06 nM. Brompheniramine can block the **hERG channels*, calcium channels, and sodium channels* with IC₅₀s of 0.90 μM, 16.12 μM and 21.26 μM, respectively. Brompheniramine has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research .

HY-18600

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

HY-B1193R

Terfenadine (Standard) (±)-Terfenadine (Standard); MDL-991 (Standard)	Reference Standards Potassium Channel Histamine Receptor Na+/Ca2+ Exchanger Caspase Apoptosis	Inflammation/Immunology Endocrinology Cancer
Terfenadine (Standard) is the analytical standard of Terfenadine. This product is intended for research and analytical applications. 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 .

HY-B0527AR

Amitriptyline hydrochloride (Standard) 4 Publications Verification	Reference Standards Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis	Neurological Disease Inflammation/Immunology Endocrinology
Amitriptyline hydrochloride (Standard) is the analytical standard of Amitriptyline hydrochloride (HY-B0527A). This product is intended for research and analytical applications. 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-W516880

Desmethylastemizole O-Demethylastemizole	Drug Metabolite Parasite Histamine Receptor Potassium Channel	Infection Cardiovascular Disease
Desmethylastemizole (O-Demethylastemizole) , a metabolite of Astemizole (HY-12532), is a β-hematin (βH) inhibitor. Desmethylastemizole has an antiplasmodium activity against P. falciparum with IC₅₀ of 0.12, 0.11 and 0.06  μM for Pf3D7, PfDd2, and PfItG strains, respectively. Desmethylastemizole is also a Histamine H1 receptor antagonist. Desmethylastemizole significantly blocks hERG K ⁺ channels and also inhibits histone-lysine N-methyltransferase EZH2 activity. Desmethylastemizole can be used for long QT syndrome and malaria research .

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-B0527AS

Amitriptyline-d6 hydrochloride	Isotope-Labeled Compounds Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis	Neurological Disease Inflammation/Immunology Endocrinology
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-15551R

E-4031 (Standard)	Potassium Channel Reference Standards	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-12532S

Astemizole-d3	Isotope-Labeled Compounds Histamine Receptor Potassium Channel	Inflammation/Immunology Endocrinology
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-N1934R

Dihydroberberine (Standard)	Reference Standards Potassium Channel HSP	Cardiovascular Disease Inflammation/Immunology Cancer
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-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-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-14848

Naluzotan PRX 00023	5-HT Receptor Potassium Channel	Neurological Disease
Naluzotan 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-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 .

HY-172903

Nav1.8-IN-16	Sodium Channel	Neurological Disease Inflammation/Immunology
Nav1.8-IN-16 (Compound (R)-40) is an orally active and selective hNaV 1.8 inhibitor (IC₅₀: 5.9 nM). Nav1.8-IN-16 exerts analgesic effects by blocking NaV1.8 channels without significantly affecting other NaV subtypes or hERG channels. Nav1.8-IN-16 exhibits dose-dependent analgesic effects in postoperative pain and inflammatory pain models and can be used in pain-related research .

HY-12532R

Astemizole (Standard) R 43512 (Standard)	Reference Standards Histamine Receptor Potassium Channel	Inflammation/Immunology Endocrinology
Astemizole (Standard) is the analytical standard of Astemizole. This product is intended for research and analytical applications. Astemizole (R 43512), a second-generation antihistamine agent 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-B0407AR

Chlorpromazine hydrochloride (Standard)	Reference Standards Dopamine Receptor Autophagy Cytochrome P450 5-HT Receptor	Cardiovascular Disease Neurological Disease Cancer
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 .

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-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-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-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-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-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-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-B1167R

Ajmaline (Standard) Cardiorythmine (Standard); (+)-Ajmaline (Standard)	Reference Standards Sodium Channel	Cardiovascular Disease
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-14186

KVI-020 WYE-160020	Potassium Channel	Cardiovascular Disease
KVI-020 is an orally active, potent and selective blocker of the atrial potassium channel Kv1.5, with an IC₅₀ of 480 nM. KVI-020 can inhibits *hERG, with an IC₅₀* of 15100 nM. KVI-020 is a potent antiarrhythmic agent, and can be used for atrial fibrillation (AF) research .

HY-19117

BRL-32872	Potassium Channel	Cardiovascular Disease
BRL-32872 is a potent human ether-a-go-go-related gene (hERG) potassium channel blocker (IC₅₀=241 nM in isolated cardiomyocytes; 19.8 nM in HEK293 cells). BRL-32872 is promising for research of cardiac arrhythmias (e.g., atrial/ventricular rhythms) .

HY-B0480AR

Brompheniramine (Standard) (±)-Brompheniramine (Standard)	Reference Standards Histamine Receptor mAChR Potassium Channel Sodium Channel Calcium Channel	Neurological Disease Inflammation/Immunology Endocrinology
Brompheniramine (Standard) is the analytical standard of Brompheniramine. This product is intended for research and analytical applications. Brompheniramine ((±)-Brompheniramine) is a potent and orally active antihistamine of the alkylamine class. Brompheniramine is a selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine can block the hERG channels, calcium channels, and sodium channels with IC50s of 0.90 μM, 16.12 μM and 21.26 μM, respectively. Brompheniramine has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research [4].

HY-B0480R

Brompheniramine maleate (Standard) (±)-Brompheniramine maleate (Standard)	Reference Standards Histamine Receptor mAChR Potassium Channel Sodium Channel Calcium Channel	Neurological Disease Inflammation/Immunology Endocrinology
Brompheniramine (maleate) (Standard) is the analytical standard of Brompheniramine (maleate). This product is intended for research and analytical applications. Brompheniramine ((±)-Brompheniramine) maleate is a potent and orally active antihistamine of the alkylamine class. Brompheniramine maleate is a selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine maleate can block the hERG channels, calcium channels, and sodium channels with IC₅₀s of 0.90 μM, 16.12 μM and 21.26 μM, respectively. Brompheniramine maleate has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research .

HY-12533B

Disopyramide hydrochloride Dicorantil hydrochloride; SC-7031 hydrochloride	Sodium Channel Potassium Channel	Cardiovascular Disease
Disopyramide hydrochloride is a class IA antiarrhythmic agent with efficacy in ventricular and atrial arrhythmias. Disopyramide hydrochloride blocks the fast inward sodium current of cardiac muscle and prolongs the duration of cardiac action potentials. Disopyramide hydrochloride inhibits HERG encoded potassium channels. Disopyramide hydrochloride also exhibits complex protein binding, and has a potent negative inotropic action .

HY-153952

Immuno modulator-1	TNF Receptor Interleukin Related Potassium Channel	Inflammation/Immunology Cancer
Immuno modulator-1 (compound 22) inhibits TNFα and IL-2 secretion in human peripheral blood mononuclear cells (hPBMC), with IC₅₀ values of 4.7 and 26 nM, respectively. Immuno modulator-1 shows *hERG* potassium channel blocking effect, with Inhibitory percentage of 20% at 3 μM .

HY-18600AS

Azimilide-d8 dihydrochloride NE-10064-d8 dihydrochloride	Isotope-Labeled Compounds Potassium Channel Calcium Channel Sodium Channel	Cardiovascular Disease
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 .

Cat. No.	Product Name

HY-L225

Cardiotoxic Compound Library

258 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 258 cardiotoxicity compounds, including some FDA-approved drugs as well as inhibitors/blockers of the hERG potassium channel.

Cat. No.	Product Name	Target	Research Area

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 .

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.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-B2136

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

HY-N1934

Dihydroberberine	Cardiovascular Disease Alkaloids other families Classification of Application Fields Plants Isoquinoline Alkaloids Inflammation/Immunology Disease Research Fields Source Classification	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-B1167

Ajmaline Cardiorythmine; (+)-Ajmaline	Apocynaceae Cardiovascular Disease Alkaloids Piperidine Alkaloids Rauvolfia serpentina Classification of Application Fields Plants Disease Research Fields Indole Alkaloids Source Classification	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-N1934R

Dihydroberberine (Standard)	Alkaloids Structural Classification other families Plants Isoquinoline Alkaloids Source Classification	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-B1167R

Ajmaline (Standard) Cardiorythmine (Standard); (+)-Ajmaline (Standard)	Apocynaceae Alkaloids Piperidine Alkaloids Structural Classification Rauvolfia serpentina Plants Indole Alkaloids Source Classification	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-W041470R

4-Methyl-1-phenyl-2-pentanone (Standard)	Ketones, Aldehydes, Acids Endogenous metabolite Source Classification	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-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-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-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 .

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.

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