Search Result

Results for "

hERG

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (16) Adrenergic Receptor (1) Akt (1) Aminopeptidase (1) Antibiotic (5) Apoptosis (4) Autophagy (21) Bacterial (16) Beta-secretase (2) Btk (1) Calcium Channel (12) Cannabinoid Receptor (1) Caspase (2) CCR (2) CDK (1) CRAC Channel (1) CXCR (2) Cytochrome P450 (9) Dipeptidyl Peptidase (1) DNA/RNA Synthesis (2) Dopamine Receptor (3) Dopamine Transporter (3) Endogenous Metabolite (2) Epigenetic Reader Domain (1) ERK (2) Estrogen Receptor/ERR (1) Eukaryotic Initiation Factor (eIF) (1) Ferroptosis (1) GLP Receptor (1) Glucocorticoid Receptor (2) Glutathione Peroxidase (1) GPR119 (1) GPR55 (1) GPR68 (1) HCV (1) HCV Protease (2) Histamine Receptor (13) Histone Demethylase (2) Histone Methyltransferase (1) HIV (3) HMG-CoA Reductase (HMGCR) (8) HSP (4) iGluR (5) Interleukin Related (1) IRAK (1) Isotope-Labeled Compounds (7) Keap1-Nrf2 (1) LRRK2 (1) mAChR (5) MAGL (1) MCHR1 (GPR24) (1) MEK (1) METTL3 (1) MNK (1) Na+/Ca2+ Exchanger (2) Opioid Receptor (2) P-glycoprotein (1) p38 MAPK (1) Parasite (6) Phosphodiesterase (PDE) (1) PI4K (1) Pim (1) Potassium Channel (107) Protease Activated Receptor (PAR) (1) Proteasome (1) Reverse Transcriptase (3) Sigma Receptor (3) Sodium Channel (16) Somatostatin Receptor (2) Syk (2) TGF-β Receptor (1) TNF Receptor (1) TRP Channel (2) VEGFR (1)
By Research Areas:	Cancer (49) Cardiovascular Disease (52) Endocrinology (14) Infection (25) Inflammation/Immunology (38) Metabolic Disease (18) Neurological Disease (57)

By Targets:

5-HT Receptor (16)

Adrenergic Receptor (1)

Akt (1)

Aminopeptidase (1)

Antibiotic (5)

Apoptosis (4)

Autophagy (21)

Bacterial (16)

Beta-secretase (2)

Btk (1)

Calcium Channel (12)

Cannabinoid Receptor (1)

Caspase (2)

CCR (2)

CDK (1)

CRAC Channel (1)

CXCR (2)

Cytochrome P450 (9)

Dipeptidyl Peptidase (1)

DNA/RNA Synthesis (2)

Dopamine Receptor (3)

Dopamine Transporter (3)

Endogenous Metabolite (2)

Epigenetic Reader Domain (1)

ERK (2)

Estrogen Receptor/ERR (1)

Eukaryotic Initiation Factor (eIF) (1)

Ferroptosis (1)

GLP Receptor (1)

Glucocorticoid Receptor (2)

Glutathione Peroxidase (1)

GPR119 (1)

GPR55 (1)

GPR68 (1)

HCV (1)

HCV Protease (2)

Histamine Receptor (13)

Histone Demethylase (2)

Histone Methyltransferase (1)

HIV (3)

HMG-CoA Reductase (HMGCR) (8)

HSP (4)

iGluR (5)

Interleukin Related (1)

IRAK (1)

Isotope-Labeled Compounds (7)

Keap1-Nrf2 (1)

LRRK2 (1)

mAChR (5)

MAGL (1)

MCHR1 (GPR24) (1)

MEK (1)

METTL3 (1)

MNK (1)

Na+/Ca2+ Exchanger (2)

Opioid Receptor (2)

P-glycoprotein (1)

p38 MAPK (1)

Parasite (6)

Phosphodiesterase (PDE) (1)

PI4K (1)

Pim (1)

Potassium Channel (107)

Protease Activated Receptor (PAR) (1)

Proteasome (1)

Reverse Transcriptase (3)

Sigma Receptor (3)

Sodium Channel (16)

Somatostatin Receptor (2)

Syk (2)

TGF-β Receptor (1)

TNF Receptor (1)

TRP Channel (2)

VEGFR (1)

By Research Areas:

Cancer (49)

Cardiovascular Disease (52)

Endocrinology (14)

Infection (25)

Inflammation/Immunology (38)

Metabolic Disease (18)

Neurological Disease (57)

193

Inhibitors & Agonists

Biochemical Assay Reagents

Peptides

Natural
Products

Recombinant Proteins

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-124702

ICA-105574	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 .

HY-15551

E-4031 3 Publications Verification	Potassium Channel	Cardiovascular Disease
E-4031 is a selective *hERG* potassium channel blocker for use in class III anti-arrhythmic studies .

HY-17508

Clarithromycin 10+ Cited Publications	Bacterial Cytochrome P450 Autophagy Antibiotic	Infection Cancer
Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC₅₀ (K_i) value of 56 (43) μM . Clarithromycin significantly inhibits the HERG potassium current .Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K .

HY-163421

hERG-IN-2	Potassium Channel	Cancer
hERG-IN-2 (Compound 1) is a potent *hERG* inhibitor, with an IC₅₀ of < 2 μM. hERG-IN-2 can be used for the research of cancer .

HY-155462

hERG-IN-1	Bacterial	Infection
hERG-IN-1 (compound 2a) is an antibacterial agent and inhibitor of hERG. hERG-IN-1 inhibits pulmonary infection caused by Pseudomonas aeruginosa strain ATCC 27853 .

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-153690

Progranulin modulator-1	Others	Others
Progranulin modulator-1 (Compound 60) is an orally active enhancer of progranulin (PGRN) secretion. Progranulin modulator-1 enhances the potency of BV-2 cell to increase PGRN levels, has inhibitory effect on *hERG* and Low cytotoxicity, the PGRN EC₅₀ and hERG IC₅₀ were 83 and 3100 nM, respectively .

HY-160658

AZ760	CCR	Inflammation/Immunology
AZ760 is a CCR8 antagonist. AZ760 shows excellent potency, good lipophilicity and high free fraction in blood. AZ760 exhibits unacceptable *hERG* inhibition .

HY-17504D

(3S,5R)-Rosuvastatin	HMG-CoA Reductase (HMGCR) Potassium Channel Autophagy	Cardiovascular Disease Metabolic Disease
(3S,5R)-Rosuvastatin is the (3S,5R)-enantiomer of Rosuvastatin. Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC₅₀ of 11 nM . Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC₅₀ of 195 nM . Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .

HY-17504C

(3R,5R)-Rosuvastatin	HMG-CoA Reductase (HMGCR) Potassium Channel Autophagy	Cardiovascular Disease Metabolic Disease
(3R,5R)-Rosuvastatin is the (3R,5R)-enantiomer of Rosuvastatin. Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC₅₀ of 11 nM . Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC₅₀ of 195 nM . Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .

HY-100321

MCHR1 antagonist 2	MCHR1 (GPR24) Potassium Channel	Metabolic Disease Endocrinology
MCHR1 antagonist 2 is an antagonist of melanin concentrating hormone receptor 1, with an IC₅₀ of 65 nM; MCHR1 antagonist 2 also inhibits *hERG, with an IC₅₀* of 4.0 nM in IMR-32 cells .

HY-17504B

Rosuvastatin Sodium 10+ Cited Publications ZD 4522 Sodium; X-Plended Sodium; Crestor Sodium	HMG-CoA Reductase (HMGCR) Potassium Channel Autophagy Bacterial	Cardiovascular Disease Metabolic Disease Cancer
Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC₅₀ of 11 nM. Rosuvastatin Sodium potently blocks *hERG* current with an IC₅₀ of 195 nM . Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .

HY-149013

Anti-MRSA agent 5	Bacterial	Infection
Anti-MRSA agent 5 (B14) is a potent MRSA agent with MIC₅₀ values of 0.38 μg/mL and has low hERG activity with an IC₅₀ values of >40 μM. Anti-MRSA agent 5 (B14) also has low cytotoxicity to mammal cells and unlikely to acquire bacterial resistance .

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-146328

PqsR/LasR-IN-2	Bacterial Antibiotic	Infection
PqsR/LasR-IN-2 (Compound 3) is a potent inhibitor of PqsR and LasR systems in P. aeruginosa. PqsR/LasR-IN-2 also inhibits hERG with the IC₅₀ of 1.408 µM .

HY-146329

PqsR/LasR-IN-3	Bacterial Antibiotic	Infection
PqsR/LasR-IN-3 (Compound 7a) is a potent inhibitor of PqsR and LasR systems in P. aeruginosa. PqsR/LasR-IN-3 also inhibits hERG with the IC₅₀ of 109.01 µM .

HY-156759

METTL3-IN-5	METTL3	Cancer
METTL3-IN-5 (Compound 13) is a METTL3 inhibitor. METTL3-IN-5 inhibits MOLM-13 growth with an IC₅₀ less than 2 μM. METTL3-IN-5 has weak hERG inhibitory activity (IC₅₀ >30 μM). METTL3-IN-5 can be used for AML research .

HY-17504BS2

Rosuvastatin-13C,d3 sodium ZD 4522-₁₃C,d₃ sodium; X-Plended-₁₃C,d₃ sodium; Crestor-₁₃C,d₃ sodium	Autophagy Bacterial HMG-CoA Reductase (HMGCR) Potassium Channel Isotope-Labeled Compounds	Cardiovascular Disease Metabolic Disease
Rosuvastatin- ¹³C,d₃ sodium is ¹³C and deuterated labeled Rosuvastatin sodium (HY-17504B). Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC₅₀ of 11 nM. Rosuvastatin Sodium potently blocks *hERG* current with an IC₅₀ of 195 nM . Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .

HY-17504

Rosuvastatin Calcium 10+ Cited Publications Rosuvastatin hemicalcium; ZD 4522 Calcium	HMG-CoA Reductase (HMGCR) Autophagy Potassium Channel Bacterial	Cardiovascular Disease Metabolic Disease Cancer
Rosuvastatin Calcium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC₅₀ of 11 nM. Rosuvastatin Calcium potently blocks *hERG* current with an IC₅₀ of 195 nM . Rosuvastatin Calcium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Calcium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .

HY-16489

Terodiline	Potassium Channel mAChR Calcium Channel	Metabolic Disease
Terodiline, an antispasmodic agent, blocks *hERG* current with the IC₅₀ of 375 nM. Terodiline has both anticholinergic and calcium antagonist properties, and effectively reduces abnormal bladder contractions caused by detrusor instability. Terodiline can be used for the research of urinary incontinence .

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-17504A

Rosuvastatin ZD 4522	HMG-CoA Reductase (HMGCR) Autophagy Potassium Channel Bacterial	Cardiovascular Disease Metabolic Disease Cancer
Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC₅₀ of 11 nM. Rosuvastatin potently blocks *hERG* current with an IC₅₀ of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .

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-143315

Protease-Activated Receptor-1 antagonist 3	Protease Activated Receptor (PAR)	Cardiovascular Disease
Protease-Activated Receptor-1 antagonist 3 is a potent protease-activated receptor-1 antagonist with an IC₅₀ value of 7 nM. Protease-Activated Receptor-1 antagonist 3 shows binding affinity for hERG K ⁺ channel with an IC₅₀ value of 9 µM .

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-157303

SSTR5 antagonist 3	Somatostatin Receptor	Cardiovascular Disease
SSTR5 antagonist 3 (Compound 23) is an orally active somatostatin receptor subtype 5 (SSTR5) antagonist with low hERG inhibition. SSTR5 antagonist 3 exhibits potency with IC₅₀ values of 2.8 nM and 1.4 nM in human and mouse, respectively. SSTR5 antagonist 3 can be used for the research of anti-gallstone .

HY-119886

BMS-986169	Others	Neurological Disease
BMS-986169 is an inhibitor of the glutamate N-methyl-D-aspartate 2B receptor (GluN2B). BMS-986169 has a high binding affinity for the allosteric regulatory site of the GluN2B subunit, with a K_i value of 4.03-6.3 nM. BMS-986169 can inhibit the function of GluN2B receptors in Xenopus oocytes, with an IC₅₀ value of 24.1 nM. BMS-986169 can also inhibit the activity of the hERG channel, with an IC₅₀ value of 28.4 μM. BMS-986169 can be used in research on treatment-resistant depression .

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-14149

Cisapride 1 Publications Verification R 51619; (±)-Cisaprid	5-HT Receptor Potassium Channel	Neurological Disease
Cisapride (R 51619) is an orally active 5-HT₄ receptor agonist with an EC₅₀ value of 140 nM. Cisapride is a *hERG* blocker with an IC₅₀ value of 9.4 nM. Cisapride is a gastroprokinetic agent that stimulates gastrointestinal motor activity .

HY-12532R

Astemizole (Standard)	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-147841

HIV-1 inhibitor-41	HIV Reverse Transcriptase	Infection
HIV-1 inhibitor-41 (Compound B23) is an orally active non-nucleoside HIV-1 reverse transcriptase inhibitor with EC₅₀ values of 20.8 nM and 50 nM against HIV-1 WT and mutant E138K strain, respectively. HIV-1 inhibitor-41 shows low hERG, no apparent CYP enzymatic inhibition and no acute toxicity .

HY-144437

ALK5-IN-9	TGF-β Receptor	Cancer
ALK5-IN-9 (Compound 8h) is a potent and orally active inhibitor of TGFβRI (ALK5). ALK5-IN-9 inhibits ALK5 autophosphorylation and NIH3T3 cell activity with IC₅₀ values of 25 nM and 74.6 nM, respectively. ALK5-IN-9 also shows favorable pharmacokinetic profile and ameliorated hERG inhibition. ALK5-IN-9 has the potential for the research of cancer disease .

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 IC₅₀s of 5 nM, 34 μM for ROMK electrophysiology (EP) and hERG EP, respectively. MK-8153 can be used as the diuretic/atriuretic .

HY-14149R

Cisapride (Standard)	5-HT Receptor Potassium Channel	Neurological Disease
Cisapride (Standard) is the analytical standard of Cisapride. This product is intended for research and analytical applications. Cisapride (R 51619) is an orally active 5-HT₄ receptor agonist with an EC₅₀ value of 140 nM. Cisapride is a *hERG* blocker with an IC₅₀ value of 9.4 nM. Cisapride is a gastroprokinetic agent that stimulates gastrointestinal motor activity .

HY-14149A

Cisapride monohydrate R 51619 monohydrate; (±)-Cisaprid monohydrate	5-HT Receptor	Neurological Disease Metabolic Disease
Cisapride monohydrate is an orally and potent 5-HT₄ receptor agonist and *hERG* inhibitor. Cisapride monohydrate is an prokinetic agent which facilitates or restores motility throughout the length of the gastrointestinal tract. Cisapride monohydrate stimulates gastrointestinal motor activity through an indirect mechanism involving the release of acetylcholine mediated by postganglionic nerve endings in the myenteric plexus of the gut .

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-146158

WX-081	Bacterial Potassium Channel Antibiotic	Infection
WX-081, an anti-tuberculosis agent, displays excellent anti-mycobacterial activity against M. tuberculosis H37Rv and low cytotoxicity. WX-081 exhibits potent activity with MIC50s of 0.083 and 0.11 μg/mL for agent susceptible tuberculosis (DS-TB) and multidrug resistant tuberculosis (MDR-TB) strains. WX-081 also inhibits hERG channel with the IC50 of 1.89 μM.

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-147691

MPO-IN-5	Glutathione Peroxidase Potassium Channel	Inflammation/Immunology
MPO-IN-5 (compound 1) is a potent, irreversible MPO (myeloperoxidase) inhibitor. MPO-IN-5 inhibits MPO peroxidation and *hERG* binding, with IC₅₀ values of 0.22 and 2.8 μM, respectively. MPO-IN-5 shows rapid kinetics of inhibition, with enzyme inactivation rate (k_inact/K_i) of 23000 M ⁻¹s ⁻¹ .

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-19620

Branaplam 10+ Cited Publications LMI070; NVS-SM1	DNA/RNA Synthesis Potassium Channel	Cancer
Branaplam (LMI070; NVS-SM1) is a highly potent, selective and orally active survival motor neuron-2 (SMN2) splicing modulator with an EC₅₀ of 20 nM for SMN. Branaplam inhibits human-ether-a-go-go-related gene (hERG) with an IC₅₀ of 6.3 μM. Branaplam elevates full-length SMN protein and extends survival in a severe spinal muscular atrophy (SMA) mouse model .

HY-19620A

Branaplam hydrochloride 10+ Cited Publications LMI070 hydrochloride; NVS-SM1 hydrochloride	DNA/RNA Synthesis Potassium Channel	Cancer
Branaplam (LMI070; NVS-SM1) hydrochloride is a highly potent, selective and orally active survival motor neuron-2 (SMN2) splicing modulator with an EC₅₀ of 20 nM for SMN. Branaplam hydrochloride inhibits human-ether-a-go-go-related gene (hERG) with an IC₅₀ of 6.3 μM. Branaplam hydrochloride elevates full-length SMN protein and extends survival in a severe spinal muscular atrophy (SMA) mouse model .

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-17504AS

Rosuvastatin-d3 ZD 4522 d₃	Isotope-Labeled Compounds HMG-CoA Reductase (HMGCR) Autophagy Potassium Channel	Cardiovascular Disease Metabolic Disease
Rosuvastatin-d₃ is a deuterium labeled Rosuvastatin. Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM[1]. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals[2].

HY-B2136

Tannic acid 3 Publications Verification	Potassium Channel	Inflammation/Immunology Cancer
Tannic acid is a novel hERG channel blocker with IC₅₀ of 3.4 μM.

HY-169001

5-HT2A/5-HT2C inverse agonist 1	5-HT Receptor	Neurological Disease
5-HT2A/5-HT2C inverse agonist 1 is a potent and dual 5-HT2A and 5-HT2C receptor inverse agonist with a *hERG* inhibitions, thus avoiding cardiovascular risks. 5-HT2A/5-HT2C inverse agonist 1 shows significant antipsychotic efficacy in the MK-801 (HY-15084B)-induced mouse model. 5-HT2A/5-HT2C inverse agonist 1 is promising for research of psychosis .

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-109968A

Irdabisant hydrochloride CEP-26401 hydrochloride	Histamine Receptor	Neurological Disease
Irdabisant (CEP-26401) hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with K_i values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant hydrochloride has relatively low inhibitory activity against hERG current with an IC₅₀ of 13.8 μM. Irdabisant hydrochloride has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant hydrochloride can be used to research schizophrenia or cognitive impairment .

HY-109968

Irdabisant CEP-26401	Histamine Receptor	Neurological Disease
Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with K_i values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC₅₀ of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment .

Cat. No.	Product Name	Type

HY-100545

BAPTA-AM 60+ 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-123445

AZD7009	Biochemical Assay Reagents
AZD7009 is a novel antiarrhythmic agrnt. AZD7009 inhibits hKv1.5 and hKv4.3/hKChIP2.2 currents with IC₅₀s of 27.0 and 23.7 muM, respectively .

Cat. No.	Product Name	Target	Research Area

HY-P1440

BeKm-1	Potassium Channel	Cardiovascular Disease
BeKm-1 is a HERG (human ether-a-go-go-related gene) blocking compound. BeKm-1 can be used for the research of heart disease .

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 3 Publications Verification	Structural Classification Classification of Application Fields Anti-aging Source classification Plants Liliaceae Ketones, Aldehydes, Acids Phenols Polyphenols Polygonatum odoratum (Mill.) Druce 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 Structural Classification 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-N1933

Allocryptopine	Cardiovascular Disease Alkaloids Structural Classification Classification of Application Fields Source classification Macleaya cordata (Willd.) R. Br. Plants Isoquinoline Alkaloids Disease Research Fields Papaveraceae	Potassium Channel
Allocryptopine, a derivative of tetrahydropalmatine, is extracted from Macleaya cordata (Thunb.) Pers. Papaveraceae. Allocryptopine has antiarrhythmic effects and potently blocks human ether-a-go-go related gene *(hERG)* current .

HY-N0221

Daurisoline 2 Publications Verification (R,R)-Daurisoline	Alkaloids Structural Classification other families Classification of Application Fields Source classification Phenols Polyphenols Plants Isoquinoline Alkaloids Disease Research Fields Cancer	Autophagy Potassium Channel
Daurisoline is a bis-benzylisoquinoline alkaloid that can be isolated from Menispermum dauricum and Rhizoma Menispermi. Daurisoline exerts a blocking effect on *hERG* and has antiarrhythmic effects. Daurisoline is a potent autophagy blocker that can be used for the research of cancer .

HY-B1167

Ajmaline Cardiorythmine; (+)-Ajmaline	Apocynaceae Cardiovascular Disease Alkaloids Piperidine Alkaloids Structural Classification 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 Structural Classification 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-B1167A

Ajmaline hydrochloride Cardiorythmine hydrochloride; (+)-Ajmaline hydrochloride	Rauvolfia verticillata (Lour.) Baill. Apocynaceae Structural Classification 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-B2136R

Tannic acid (Standard)	Structural Classification Liliaceae Ketones, Aldehydes, Acids Source classification Phenols Polyphenols Polygonatum odoratum (Mill.) Druce Plants	Potassium Channel
Tannic acid (Standard) is the analytical standard of Tannic acid. This product is intended for research and analytical applications. Tannic acid is a novel hERG channel blocker with IC50 of 3.4 μM.

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-N1933R

Allocryptopine (Standard)	Alkaloids Structural Classification Source classification Macleaya cordata (Willd.) R. Br. Plants Isoquinoline Alkaloids Papaveraceae	Potassium Channel
Allocryptopine (Standard) is the analytical standard of Allocryptopine. This product is intended for research and analytical applications. Allocryptopine, a derivative of tetrahydropalmatine, is extracted from Macleaya cordata (Thunb.) Pers. Papaveraceae. Allocryptopine has antiarrhythmic effects and potently blocks human ether-a-go-go related gene (hERG) current .

HY-N1934R

Dihydroberberine (Standard)	Alkaloids Structural Classification other families Source classification Plants Isoquinoline Alkaloids	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)	Apocynaceae Alkaloids Piperidine Alkaloids Structural Classification Rauvolfia serpentina Source classification Plants Indole Alkaloids	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-N1483

Guanfu base A	Cardiovascular Disease Alkaloids Classification of Application Fields Source classification Ranunculaceae 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 .

Cat. No.	Compare	Product Name	Species	Source

HY-P701834

	hERG Protein, Human (HEK293, GFP, His) KCNH2; Potassium voltage-gated channel subfamily H member 2; Eag homolog; Ether-a-go-go-related gene potassium channel 1; ERG-1; Eag-related protein 1; Ether-a-go-go-related protein 1; H-ERG; hERG-1; hERG1; Voltage-gated potassium channel subunit Kv11.1	Human	HEK293
	The hERG protein is the α subunit of voltage-gated potassium channels and is critical for mediating cardiac delayed rectifier potassium current (IKr). It lacks individual channel activity but dynamically affects properties by forming heterotetramers with other isoforms. hERG Protein, Human (HEK293, GFP, His) is the recombinant human-derived hERG protein, expressed by HEK293 , with C-10*His, C-GFP labeled tag.

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Cat. No.	Product Name	Chemical Structure

HY-17504BS2

Rosuvastatin-13C,d3 sodium

Rosuvastatin- ¹³C,d₃ sodium is ¹³C and deuterated labeled Rosuvastatin sodium (HY-17504B). Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC₅₀ of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC₅₀ of 195 nM . Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .

HY-17504AS

Rosuvastatin-d3
Rosuvastatin-d₃ is a deuterium labeled Rosuvastatin. Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM[1]. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals[2].

HY-17508S1

Clarithromycin-d3

Clarithromycin-d₃is the deuterium labeledClarithromycin(HY-17508) . Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC₅₀ (K_i) value of 56 (43) μM . Clarithromycin significantly inhibits the HERG potassium current .Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K .

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-N0221S

Daurisoline-d2
Daurisoline-d₂ is the deuterium labeled Daurisoline (HY-N0221). Daurisoline is a bis-benzylisoquinoline alkaloid that can be isolated from Menispermum dauricum and Rhizoma Menispermi. Daurisoline exerts a blocking effect on *hERG* and has antiarrhythmic effects. Daurisoline is a potent autophagy blocker that can be used for the research of cancer .

HY-N0221S1

Daurisoline-d5
Daurisoline-d₅ is the deuterium labeled Daurisoline (HY-N0221). Daurisoline is a bis-benzylisoquinoline alkaloid that can be isolated from Menispermum dauricum and Rhizoma Menispermi. Daurisoline exerts a blocking effect on *hERG* and has antiarrhythmic effects. Daurisoline is a potent autophagy blocker that can be used for the research of cancer .

HY-N0221S2

Daurisoline-d11
Daurisoline-d₁₁ is the deuterium labeled Daurisoline (HY-N0221). Daurisoline is a bis-benzylisoquinoline alkaloid that can be isolated from Menispermum dauricum and Rhizoma Menispermi. Daurisoline exerts a blocking effect on *hERG* and has antiarrhythmic effects. Daurisoline is a potent autophagy blocker that can be used for the research of cancer .

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[1].

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