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Results for "

hERG inhibition

" in MedChemExpress (MCE) Product Catalog:

30

Inhibitors & Agonists

1

Natural
Products

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-A0148A
    Halofantrine hydrochloride
    2 Publications Verification

    SKF-102886; WR-171669 hydrochloride

    		 Parasite Infection
    Halofantrine hydrochloride (SKF-102886) is a blocker of delayed rectifier potassium current via the inhibition of human-ether-a-go-go-related gene (HERG) channel and a potent antimalarial compound .
    Halofantrine hydrochloride
  • HY-102037
    SSTR5 antagonist 1

    		Somatostatin Receptor Metabolic Disease Endocrinology
    SSTR5 antagonist 1 (compound 25a) is a selective and orally available somatostatin receptor subtype 5 (SSTR5) antagonist with IC50s of 9.6 and 57 nM for hSSTR5 and mSSTR5, respectively .
    SSTR5 antagonist 1
  • HY-111747
    TBAJ-587
    2 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 .
    TBAJ-587
  • HY-146380
    S1427

    		Histone Demethylase Cancer
    S1427 is a tranylcypromine-derived LSD1 inhibitor with the IC50 of 390 nM and Ki of 80 nM. S1427 exhibits desirable hERG channel inhibition and microsomal stability profiles. Inhibition of LSD1 partially reduces the proliferation of cancer cells .
    S1427
  • HY-120713
    MK-8325 dihydrochloride

    		HCV Infection
    MK-8325 (dihydrochloride) is an inhibitor of HCV NS5A with oral activity. MK-8325 exhibits minimal inhibition on hERG at the concentration of 30 mM .
    MK-8325 dihydrochloride
  • 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 .
    AZ760
  • HY-163718
    Ferroptosis-IN-9

    		Ferroptosis Neurological Disease
    Ferroptosis-IN-9 (compound 23b) is a ferroptosis inhibitor with an IC50 value of >30uM for hERG inhibition. Ferroptosis-IN-9 is a ROS scavenger. Ferroptosis-IN-9 can be used in neurodegenerative disease research .
    Ferroptosis-IN-9
  • HY-A0148AR
    Halofantrine (hydrochloride) (Standard)

    		Parasite Infection
    Halofantrine (hydrochloride) (Standard) is the analytical standard of Halofantrine (hydrochloride). This product is intended for research and analytical applications. Halofantrine hydrochloride (SKF-102886) is a blocker of delayed rectifier potassium current via the inhibition of human-ether-a-go-go-related gene (HERG) channel and a potent antimalarial compound .
    Halofantrine (hydrochloride) (Standard)
  • HY-169916
    GuaB-IN-1

    		Bacterial Estrogen Receptor/ERR Infection
    GuaB-IN-1 (Compound 15) exhibits high potency against M.tb with a MIC value of 0.25 μM. GuaB-IN-1 has a favorable 28% hERG inhibition profile at 10 μM. GuaB-IN-1 is promising for research of tuberculosis .
    GuaB-IN-1
  • 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.
    DprE1-IN-1
  • 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 (kinact/Ki) of 23000 M −1s −1 .
    MPO-IN-5
  • 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 .
    SSTR5 antagonist 3
  • HY-150562
    CDK9-IN-19

    		CDK Cancer
    CDK9-IN-19 is a highly potent and selective CDK9 inhibitor with an IC50 value of 2.0 nM. CDK9-IN-19 has excellent cellular antiproliferative activity, moderate pharmacokinetic property and low hERG inhibition. CDK9-IN-19 significantly induces tumour growth inhibition in an MV4-11 xenograft mice model. CDK9-IN-19 can be used for researching acute myeloid leukaemia (AML) .
    CDK9-IN-19
  • HY-130244
    BACE1-IN-5

    		Beta-secretase Neurological Disease
    BACE1-IN-5 (Compound 15) is a β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 9.1 nM, and also inhibits cellular amyloid-β (Aβ) with an IC50 of 0.82 nM. BACE1-IN-5 has a medicinal chemistry that improves hERG inhibition and P-gp efflux .
    BACE1-IN-5
  • 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 .
    HIV-1 inhibitor-41
  • HY-160588
    Nav1.8-IN-7

    		Sodium Channel Potassium Channel Neurological Disease
    Nav1.8-IN-7 (Example 116) is a selective Nav1.8 inhibitor. Nav1.8-IN-7 shows an inhibition of >50% with 100 nM for Nav1.8. Nav1.8-IN-7 inhibits hERG with an IC50 of 15.6 μM. Nav1.8-IN-7 has the potential for pain research .
    Nav1.8-IN-7
  • 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 .
    p38α inhibitor 2
  • HY-157929
    Keap1-Nrf2-IN-19

    		Keap1-Nrf2 Inflammation/Immunology Cancer
    Keap1-Nrf2-IN-19 (compound 33) is an oral active Keap1-Nrf2 protein–protein interaction (PPI) inhibitor with the Kd value of 0.0014 μM. Keap1-Nrf2-IN-19 exhibits less than 50% inhibition at 30 μM against hERG and 10 μM against CYPs .
    Keap1-Nrf2-IN-19
  • 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 .
    ALK5-IN-9
  • HY-12708
    Chlorpromazine
    Maximum Cited Publications
    66 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-HT2A, 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 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 also can inhibit clathrin-mediated endocytosis .
    Chlorpromazine
  • HY-B0407A
    Chlorpromazine hydrochloride
    Maximum Cited Publications
    66 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-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 .
    Chlorpromazine hydrochloride
  • 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, KATP or hERG potassium channels. ML218 can penetrate the blood-brain barrier .
    ML218
  • 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, KATP or hERG potassium channels. ML218 hydrochloride can penetrate the blood-brain barrier .
    ML218 hydrochloride
  • HY-B0407AR
    Chlorpromazine (hydrochloride) (Standard)

    		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 .
    Chlorpromazine (hydrochloride) (Standard)
  • HY-W041470R
    4-Methyl-1-phenyl-2-pentanone (Standard)

    		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 .
    4-Methyl-1-phenyl-2-pentanone (Standard)
  • HY-157425
    5-HT2CR agonist 1

    		5-HT Receptor Neurological Disease
    5-HT2CR agonist 1 (compound 8), a 7-chloro analogue, is a selective 5-HT2CR partial agonist (Emax=71.09%) with an EC50 value of 121.5 nM and no observed activity toward 5-HT2AR or 5-HT2BR. 5-HT2CR agonist 1 exhibits no recruitment activity for β-arrestin and shows low inhibition of hERG at 10 μM .
    5-HT2CR agonist 1
  • 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[1].
    ML218-d9
  • HY-163982
    FOXJ1 agonist 1

    		NF-κB FOXO Inflammation/Immunology
    FOXJ1 agonist 1 (compound 16c) is an orally effective small molecule that can effectively enhance the expression of FOXJ1. Foxj1-IN-1 acts on the mammalian airway system composed of multiciliated cells (MCC) to prevent the development and onset of chronic obstructive pulmonary disease (COPD). Foxj1-IN-1 can induce the production of motile cilia in the respiratory system of zebrafish and mammals, and inhibit elastase-induced COPD mouse models. Foxj1-IN-1 has good liver microsomal stability, in vivo PK curve and AUC; it has no significant inhibition of CYP and hERG, and does not have significant cytotoxicity .
    FOXJ1 agonist 1
  • 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.
    DPP-4/GPR119 modulator 1
  • 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 .
    5-HT2A/5-HT2C inverse agonist 1

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