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hERG binding

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-124283A
    LEI-101

    		Cannabinoid Receptor Neurological Disease
    LEI-101 is a potent, selective, and orally bioavailable cannabinoid CB2 receptor agonist, with a pEC50 of 8 for hCB2, and a pKi of less than 4 for hERG. LEI-101 is ~100-fold more potent in binding to CB2 receptors than to CB1 receptors .
    LEI-101
  • HY-12533
    Disopyramide
    1 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 .
    Disopyramide
  • HY-12533A
    Disopyramide phosphate
    1 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 .
    Disopyramide phosphate
  • HY-111552
    PIM1-IN-1

    		Pim Cancer
    PIM1-IN-1 is a potent and highly selective PIM1/3 inhibitor, with IC50s of 7, 5530 and 70 nM for PIM1, PIM2, and PIM3, respectively, inhibits the phosphorylation of BAD, a downstream target of PIM, with an EC50 of 262 nM. PIM1-IN-1 shows no obvious effect on FLT3 or hERG binding. Antiproliferative and anti-cancer activity .
    PIM1-IN-1
  • HY-12938
    AMG-8718

    		Beta-secretase Neurological Disease
    AMG-8718 is a potent, selective and orally active BACE1 inhibitor with IC50 values of 0.0007, 0.005 µM for BACE1 and BACE2, respectively. AMG-8718 significantly decreases Aβ40 levels in the CSF and brain .
    AMG-8718
  • 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 .
    Protease-Activated Receptor-1 antagonist 3
  • HY-161873
    PW507

    		Sigma Receptor Neurological Disease
    PW507 is a potent, brain-penetrant and selective sigma 1 receptor (S1R) antagonist with a Ki of 7.5 nM for human S1R. PW507 displays a low binding affinity to S2R and hERG. PW507 can be used for the study of painful diabetic neuropathy (PDN) .
    PW507
  • 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 .
    Disopyramide hydrochloride
  • 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-12533R
    Disopyramide (Standard)

    Dicorantil (Standard); SC-7031 (Standard)

    		 Reference Standards Sodium Channel Potassium Channel Cardiovascular Disease
    Disopyramide (Standard) is the analytical standard of Disopyramide. This product is intended for research and analytical applications. 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 .
    Disopyramide (Standard)
  • HY-12533AR
    Disopyramide phosphate (Standard)

    		Potassium Channel Sodium Channel Cardiovascular Disease
    Disopyramide (phosphate) (Standard) is the analytical standard of Disopyramide (phosphate). This product is intended for research and analytical applications. 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 .
    Disopyramide phosphate (Standard)
  • HY-172090
    MASP-2-IN-1

    		Ser/Thr Protease Potassium Channel Inflammation/Immunology
    MASP-2-IN-1 (Compound 77) is the inhibitor for mannan-binding lectin-associated serine protease (MASP), that inhibits MASP2 and MASP3 with IC50 of 11.4 nM and 13.2 µM. MASP-2-IN-1 exhibits a weak inhibitory activity against hERG with an IC50 of 175 µM. MASP-2-IN-1 reveals a poor stability in mouse plasma with a half-life of 4.4 hours .
    MASP-2-IN-1
  • HY-119101
    AZD-5672
    1 Publications Verification

    		 CCR Potassium Channel P-glycoprotein Inflammation/Immunology
    AZD-5672 is an orally active, potent, and selective CCR5 antagonist (IC50=0.32 nM). AZD-5672 shows moderate activity against the hERG ion channel (binding IC50=7.3 μM). AZD5672 is a substrate of human P-gp, and inhibits P-gp-mediated digoxin transport (IC50=32 μM). AZD-5672 can be used for the research of rheumatoid arthritis .
    AZD-5672
  • HY-17442
    Azathramycin

    Azaerythromycin A; Desmethyl Azithromycin

    		 Bacterial Antibiotic Infection
    Azathramycin (Desmethyl Azithromycin) is a macrolide antibiotic. Azathramycin is a derivative of the anti-ribosomal antibiotic Azithromycin (HY-17506). Azathramycin exerts its antibacterial activity by binding to ribosomes and inhibiting bacterial protein synthesis. Azathramycin can selectively target and kill human senescent fibroblasts and is expected to be used in anti-aging research. Azathramycin affects multiple ion channels such as SCN5A, hERG, KCNQ1 + KCNE1, L-type Ca ++ and Kir2.1 .
    Azathramycin
  • HY-124283
    LEI-101 free base

    		Endogenous Metabolite Inflammation/Immunology
    LEI-101 free base is a selective and orally bioavailable CB2 receptor agonist with the potential to inhibit diseases associated with inflammation and/or oxidative stress. LEI-101 free base has a binding potency to CB2 receptors that is approximately 100 times higher than that to CB1 receptors. Its pEC50 value on CB2 receptors is 8, while its pKi value on hERG is less than 4. LEI-101 may have an inhibitory effect on conditions such as kidney disease .
    LEI-101 free base
  • HY-119886
    BMS-986169

    		iGluR 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 Ki 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 .
    BMS-986169
  • HY-159958
    KNa1.1-IN-2

    		Potassium Channel Neurological Disease
    KNa1.1-IN-2 (Compound Z05) is a selective KNa1.1 channel inhibitor with blood-brain barrier penetration, particularly effective against the hERG channel. KNa1.1-IN-2 works by binding to the KNa1.1 channel and blocking the channel activity induced by Gain-of-function (GOF) mutations, effectively intervening in KCNT1-related epilepsy. Additionally, KNa1.1-IN-2 inhibits the GOF mutant Y796H. KNa1.1-IN-2 holds promise for research into KCNT1-related epilepsy disorders .
    KNa1.1-IN-2

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