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Pathways Recommended:	Membrane Transporter/Ion Channel

Results for "

hERG channel inhibition

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (3) Autophagy (3) Bacterial (4) Calcium Channel (4) Cytochrome P450 (3) Dipeptidyl Peptidase (1) Dopamine Receptor (3) Endogenous Metabolite (1) GPR119 (1) Histone Demethylase (1) IFNAR (1) Interleukin Related (1) IRAK (1) MAP4K (1) p38 MAPK (1) Parasite (1) Phosphodiesterase (PDE) (1) PI3K (1) PI4K (1) Potassium Channel (2) PPAR (1) Reference Standards (3) Salt-inducible Kinase (SIK) (1) SARS-CoV (1) Sodium Channel (1) TNF Receptor (2)
By Research Areas:	Cancer (4) Cardiovascular Disease (4) Infection (6) Inflammation/Immunology (4) Metabolic Disease (2) Neurological Disease (8)

By Targets:

5-HT Receptor (3)

Autophagy (3)

Bacterial (4)

Calcium Channel (4)

Cytochrome P450 (3)

Dipeptidyl Peptidase (1)

Dopamine Receptor (3)

Endogenous Metabolite (1)

GPR119 (1)

Histone Demethylase (1)

IFNAR (1)

Interleukin Related (1)

IRAK (1)

MAP4K (1)

p38 MAPK (1)

Parasite (1)

Phosphodiesterase (PDE) (1)

PI3K (1)

PI4K (1)

Potassium Channel (2)

PPAR (1)

Reference Standards (3)

Salt-inducible Kinase (SIK) (1)

SARS-CoV (1)

Sodium Channel (1)

TNF Receptor (2)

By Research Areas:

Cancer (4)

Cardiovascular Disease (4)

Infection (6)

Inflammation/Immunology (4)

Metabolic Disease (2)

Neurological Disease (8)

Inhibitors & Agonists

Screening Libraries

Natural
Products

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-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-103309

ML218 2 Publications Verification	Calcium Channel	Neurological Disease
ML218 is a potent, selective and orally active *T-type Ca ²⁺ 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, K_ATP or hERG potassium channels. ML218 can penetrate the blood-brain barrier .

HY-175479

GLPG4970	Salt-inducible Kinase (SIK) TNF Receptor Interleukin Related	Inflammation/Immunology
GLPG4970 is a potent, selective and orally active salt-inducible kinase 2/3 (SIK2/SIK3) dual inhibitor with IC₅₀ values of 0.3 nM and 0.7 nM. GLPG4970 has weak inhibition of hERG channel with an IC₅₀ of 29 μM. GLPG4970 can decrease TNFα release and increase IL-10 release GLPG4970 can be used for the researches of inflammation and immunology, such as colitis .

HY-131335

p38α inhibitor 2	p38 MAPK	Inflammation/Immunology
p38α inhibitor 2 is a highly potent and selective p38α MAPK inhibitor, with a pIC₅₀ of 9.6. p38α inhibitor 2 inhibits the hERG ion channel (IC₅₀=27 μM) and shows a promising selectivity profile when tested in a panel of 51 other protein kinases (<30% inhibition at 10 μM concentration) and a panel of 141 other biological targets .

HY-178494

Nav1.7-IN-19	Sodium Channel Potassium Channel	Neurological Disease
Nav1.7-IN-19 is a potent, selective and orally active Nav1.7 inhibitor with an IC₅₀ of 0.49 μM. Nav1.7-IN-19 shows high selectivity for Nav1.7, with selectivities of 312-fold and 662-fold against Nav1.1 and Nav1.5 in the inactivated state. Nav1.7-IN-19 exhibits weak inhibition on hERG potassium channels. Nav1.7-IN-19 exhibits analgesic effect and can be used for the research of neurological disease .

HY-144341

DprE1-IN-1	Bacterial	Infection
DprE1-IN-1 is a potent, orally active DprE1 inhibitor with favorable hepatocyte stability, low cytotoxicity and low hERG channel inhibition. DprE1-IN-1 displays potent activity against both agent-susceptible and clinically isolated drug-resistant Tuberculosis strains with MICs10 CFU reduction in macrophages.

HY-W064918

NITD-304	Bacterial	Infection
NITD-304 is an orally active anti-tuberculosis agent. NITD-304 exerts inhibitory and bactericidal activities gainst Mycobacterium tuberculosis and multidrug-resistant Mycobacterium tuberculosis. NITD-304 inhibits mycobacterial cell wall biosynthesis and demonstrates synergistic or additive growth inhibitory activity with select antibacterial agents. NITD-304 shows low risk of cardiotoxicity and drug-drug interactions, with no inhibition of major cytochrome P-450 enzymes or hERG channel. NITD-304 can be used for the research of tuberculosis and multidrug-resistant tuberculosis .

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-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-178775

PI4K-IN-3	PI4K Parasite MAP4K PI3K	Infection
PI4K-IN-3 (Compound 27) is an orally active PI4K inhibitor with an IC₅₀ of 1.9  nM for Plasmodium vivax PI4K. PI4K-IN-3 has no hERG channel inhibition and mammalian cytotoxicity. PI4K-IN-3 has significant selectivity against the human MINK1 and MAP4K4 kinases but with low selectivity against human PI3Kα and PI4Kβ. PI4K-IN-3 has potent antimalarial activity and significantly reduces parasitaemia in NSG mice mouse models of Plasmodium falciparum malaria .

HY-103309A

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

HY-103309S

ML218-d9	Calcium Channel	Neurological Disease
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-W041470R

4-Methyl-1-phenyl-2-pentanone (Standard)	Reference Standards Endogenous Metabolite	Metabolic Disease
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-146468

DPP-4/GPR119 modulator 1	Dipeptidyl Peptidase GPR119 Potassium Channel	Metabolic Disease
DPP-4/GPR119 modulator 1 (Compound 22) is an orally active dipeptidyl peptidase IV (DPP-IV) inhibitor and GPR119 agonist. DPP-4/GPR119 modulator 1 shows blood glucose-lowering effect and moderate inhibition on **hERG channel with an IC₅₀** of 4.9 μM. DPP-4/GPR119 modulator 1 can be used for diabetes research . DPP-4/GPR119 modulator 1 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-181745

Pks13-IN-3	Bacterial	Infection
Pks13-IN-3 is a furo[2,3-b]isoquinoline derivative and Pks13 inhibitor with an IC₅₀ of 1.12 μM. Pks13-IN-3 reduces inhibition of the *hERG* ion channel. Pks13-IN-3 can be used for the research of tuberculosis .

HY-175804

M2 ion channel blocker-2	SARS-CoV	Infection
M2 ion channel blocker-2 (Compound 10) is a M2 channel blocker. M2 ion channel blocker-2 significantly blocks wild-type and mutant M2 (L27F and V27A) ion channels. M2 ion channel blocker-2 has potent antiviral activity against HCoV-229E (EC₅₀: 4.7  μM in cytopathic effect) but not against influenza A virus. M2 ion channel blocker-2 has no significant inhibition of hERG and cytochrome P450 (CYP1A2, CYP2C19, and CYP3A4) activity .

HY-103309R

ML218 (Standard)	Reference Standards Calcium Channel	Neurological Disease
ML218 (Standard) is the analytical standard of ML218 (HY-103309). This product is intended for research and analytical applications. 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-179580

EL244	PPAR Phosphodiesterase (PDE)	Inflammation/Immunology
EL244 is a dua Autotaxin (ATX) (IC₅₀ = 50 nM) inhibitor and PPARγ (IC₅₀ = 1.3 μM; K_d = 1.3 μM) agonist. EL244 demonstrates low cytotoxicity in human HepG2 cells (EC₅₀ = 81.2 μM) with minimal inhibition of the cardiac hERG potassium channel (12% at 25 μM). EL244 significantly reduces pulmonary Lysophosphatidic Acid (LPA) levels, attenuates fibrosis, and restores respiratory function with limited systemic absorption in vivo. EL244 can be used for idiopathic pulmonary fibrosis and interstitial lung disease (ILD) research .

HY-180579

IRAK4-IN-33	IRAK TNF Receptor IFNAR	Inflammation/Immunology
IRAK4-IN-33 (Compound 22) is a selective, potent and orally active interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor with an IC₅₀ 0.36 nM. IRAK4-IN-33 can block the pro-inflammatory signaling pathway mediated by IRAK4 and inhibit the release of TNFα and IFNα. IRAK4-IN-33 shows weak inhibition for hERG channel (IC₅₀ > 30 μM). IRAK4-IN-33 can be used for the research of inflammation and immunology, such as rheumatoid arthritis .

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.

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.

Cat. No.	Product Name	Category	Target	Chemical Structure

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-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 .

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 .

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