Search Result
Results for "
hERG channel
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
2
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-124702
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Potassium Channel
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Cardiovascular Disease
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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 .
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- HY-15551
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- HY-153219A
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Potassium Channel
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Endocrinology
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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 .
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- HY-153219
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Potassium Channel
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Endocrinology
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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 .
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- HY-108594
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Potassium Channel
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Metabolic Disease
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PD-118057 is a hERG channel activator without causing hERG blockade. PD-118057 activates hERG channel to suppress changes in membrane excitability .
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- HY-106912A
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MK 499 free base
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Potassium Channel
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Cardiovascular Disease
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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 .
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- HY-A0148
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SKF-102886 free base; WR-171669
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Parasite
Potassium Channel
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Infection
Cancer
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Halofantrine (SKF-102886 free base) is a highly lipophilic antimalarial active against Chloroquine-resistant strains of Plasmodium falciparum . Halofantrine blocks HERG potassium channels .
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- HY-146380
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Histone Demethylase
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Cancer
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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 .
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- HY-132201
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Potassium Channel
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Metabolic Disease
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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 .
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- HY-B1167A
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Cardiorythmine hydrochloride; (+)-Ajmaline hydrochloride
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Others
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Cardiovascular Disease
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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.
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- HY-108586
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Potassium Channel
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Neurological Disease
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NS3623 is an activator of human ether-a-go-go-related gene (hERG1/KV11.1) 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 .
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- HY-B2136
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- HY-N7511
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- HY-12082A
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Potassium Channel
Parasite
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Infection
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GSK369796 Dihydrochloride is an affordable and effective antimalarial and inhibits hERG potassium ion channel repolarization with an IC50 of 7.5 μM.
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- HY-118172
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- HY-P5177
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- HY-16915
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Potassium Channel
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Cardiovascular Disease
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RPR-260243, a potent activator of human ether-a-go-go-related gene (hERG), slows deactivation and attenuates inactivation of hERG1 channels. RPR260243-modified HERG currents are inhibited by Dofetilide (IC50=58 nM). RPR260243 displays no activator-like effects on other voltage-dependent ion channels, including the closely related ERG3 K+ channel . RPR-260243 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-111747
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Bacterial
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Infection
Cardiovascular Disease
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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 .
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- HY-19927A
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5-HT Receptor
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Neurological Disease
Endocrinology
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DA-6886 is a 5-Hydroxytryptamine receptor 4 (5-HT4) agonist. DA-6886 induces relaxation of the rat oesophagus preparation in a 5-HT4 receptor antagonist-sensitive manner. The evaluation of DA-6886 in CHO cells expressing hERG channels reveals that it inhibits hERG channel current with an pIC50 value of 4.3, indicating that the compound is 1000-fold more selective for the 5-HT4 receptor over hERG channels. DA-6886 can be used in the study of constipated irritable bowel syndrome .
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- HY-112075
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Potassium Channel
Calcium Channel
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Cardiovascular Disease
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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 .
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- HY-120375
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- HY-113673
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Potassium Channel
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Cardiovascular Disease
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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 .
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- HY-B2136R
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Potassium Channel
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Inflammation/Immunology
Cancer
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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.
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- HY-122024
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Potassium Channel
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Cardiovascular Disease
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AZSMO-23 is a potent hERG K + channel activator. AZSMO-23 activats WT hERG pre-pulse and tail current with EC50 values of 28.6, 11.2 µM, respectively. AZSMO-23 has the potential for the research of long QT syndrome .
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- HY-156976
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Calcium Channel
Sodium Channel
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Cardiovascular Disease
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Sulcardine is a multi-ion channel blocker that can reduce INa and ICa 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 .
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- HY-156976A
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Calcium Channel
Sodium Channel
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Cardiovascular Disease
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Sulcardine hydrochloride is a multi-ion channel blocker that can reduce INa and ICa 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 .
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- HY-124687
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- HY-B1482
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TPS-23 benzenesulfonate
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Potassium Channel
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Neurological Disease
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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 .
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- HY-B1482A
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TPS-23
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Potassium Channel
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Neurological Disease
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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 .
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- HY-N5006
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- HY-B0369AS
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- HY-A0148A
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SKF-102886; WR-171669 hydrochloride
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Parasite
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Infection
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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 .
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- HY-122167
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- HY-P1440A
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Potassium Channel
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Neurological Disease
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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.
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- HY-100545
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BAPTA-AM
Maximum Cited Publications
63 Publications Verification
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Potassium Channel
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Cardiovascular Disease
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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 .
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- HY-162555
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Potassium Channel
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Cardiovascular Disease
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BMS-986308 is a selective and orally active renal outer medullary potassium (ROMK) channel inhibitor. BMS-986308 is selective for ROMK over hERG. BMS-986308 can be used for heart failure research .
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- HY-163590
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- HY-101622
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- HY-14848
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PRX 00023
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5-HT Receptor
Potassium Channel
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Neurological Disease
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Naluzotan is a novel, potent, and selective amidosulfonamide 5-HT1A agonist with IC50 and Ki 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.
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- HY-14848A
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PRX 00023 hydrochloride
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5-HT Receptor
Potassium Channel
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Neurological Disease
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Naluzotan hydrochloride is a novel, potent, and selective amidosulfonamide 5-HT1A agonist with IC50 and Ki 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.
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- HY-B0480
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(±)-Brompheniramine maleate
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Histamine Receptor
mAChR
Potassium Channel
Sodium Channel
Calcium Channel
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Neurological Disease
Inflammation/Immunology
Endocrinology
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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 .
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- HY-B0480A
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- HY-P5795
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Sodium Channel
Potassium Channel
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Neurological Disease
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GsAF-I is a potent Nav and hERG1 channels blocker with IC50s of 0.36, 0.6, 1.28, 0.33, 1.2, 0.04 and 4.8 μM against Nav1.1, Nav1.2, Nav1.3, Nav1.4, Nav1.6, Nav1.7 and hERG1, respectively .
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- HY-B1167
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Cardiorythmine; (+)-Ajmaline
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Sodium Channel
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Cardiovascular Disease
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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 .
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- HY-A0148AR
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Parasite
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Infection
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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 .
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- HY-100238
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- HY-B0480R
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Histamine Receptor
mAChR
Potassium Channel
Sodium Channel
Calcium Channel
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Neurological Disease
Inflammation/Immunology
Endocrinology
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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 .
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- HY-B0480AR
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Histamine Receptor
mAChR
Potassium Channel
Sodium Channel
Calcium Channel
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Neurological Disease
Inflammation/Immunology
Endocrinology
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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].
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- HY-143315
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Protease Activated Receptor (PAR)
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Cardiovascular Disease
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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 .
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- HY-116838
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Bacterial
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Infection
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TAM-16 is a potent and orally active polyketide synthase 13 (Pks13) inhibitor with an IC50 value of 0.32 μM. TAM-16 has promising activity against Mycobacterium tuberculosis. TAM-16 inhibits hERG cardiac ion channel .
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- HY-103309
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ML218
1 Publications Verification
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Calcium Channel
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Neurological Disease
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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 .
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- HY-103309A
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Calcium Channel
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Neurological Disease
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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 .
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- HY-14186
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WYE-160020
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Potassium Channel
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Cardiovascular Disease
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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 .
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- HY-16916
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NS1643
1 Publications Verification
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Potassium Channel
Autophagy
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Cancer
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NS1643 is a partial agonist of human ether-a-go-go-related gene (hERG) K + channels with an EC50 of 10.5 μM. NS1643 inhibits the growth of breast cancer tumors in TNBC mouse models. NS1643 inhibits cell migration and invasion of breast cancer cells .
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- HY-A0236A
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Potassium Channel
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Cardiovascular Disease
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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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- HY-14356
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- HY-153952
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- HY-13044
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- HY-B1193
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- HY-12532
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R 43512
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Histamine Receptor
Potassium Channel
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Inflammation/Immunology
Endocrinology
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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 .
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- HY-12533
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Dicorantil; SC-7031
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Sodium Channel
Potassium Channel
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Cardiovascular Disease
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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 .
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- HY-134494
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GPR68
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Neurological Disease
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MS48107 is a potent and selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68). MS48107 is selective for GPR68 over the closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. MS48107 can readily cross the blood-brain barrier (BBB) in mice .
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- HY-12533A
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Dicorantil phosphate; SC-7031 phosphate
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Potassium Channel
Sodium Channel
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Cardiovascular Disease
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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 .
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- HY-B1167R
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Sodium Channel
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Cardiovascular Disease
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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 .
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- HY-12533B
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Dicorantil hydrochloride; SC-7031 hydrochloride
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Sodium Channel
Potassium Channel
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Cardiovascular Disease
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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 .
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- HY-12962
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iGluR
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Neurological Disease
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NMDA-IN-1 is a potent and NR2B-selective NMDA antagonist with Ki of 0.85 nM; NR2B Ca2+ influx IC50 is 9.7 nM; no activities on NR2A, NR2C, NR2D, hERG-channel and α1-adrenergic receptor.
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- HY-144341
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Bacterial
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Infection
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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.
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- HY-120454
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MEK
Potassium Channel
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Cancer
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G-479 is the inhibitor for MEK and hERG channel (IC50=14 μM). G-479 inhibits the proliferation of HCT-116 and A375 with IC50 of 0.049 μM and 0.004 μM. G-479 exhibits good metabolic stability in liver microsomes and good pharmacokinetic characteristics in rats .
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- HY-103309S
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Calcium Channel
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Neurological Disease
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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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- HY-103268
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Potassium Channel
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Neurological Disease
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(Rac)-AZD3839 is an orally active beta-amyloid precursor protein cleaving enzyme (BACE1) inhibitor that is blood-brain barrier-permeable. (Rac)-AZD3839 has an affinity for the human ether-a-go-go related gene (hERG) ion channel. (Rac)-AZD3839 can be used in the research of Alzheimer's disease .
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- HY-163387
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Others
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Inflammation/Immunology
Cancer
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CHI3L1-IN-1 (Compound 30) is an inhibitor for Chitinase-3-like protein 1 (CHI3L1) (YKL-40) with IC50 of 50 nM. CHI3L1-IN-1 inhibits hERG channel with an IC50 of 2.3 μM .
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- HY-N1934
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Potassium Channel
HSP
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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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 .
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- HY-107708
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iGluR
Sigma Receptor
Potassium Channel
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Neurological Disease
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threo Ifenprodil hemitartrate is a σ receptor agonist, with Kis of 59.1 and 2 nM for σ1 and σ2 receptors, respectively. threo Ifenprodil hemitartrate is also a NR2B subunit-selective NMDA receptor antagonist (IC50=0.22 μM). threo Ifenprodil hemitartrate is a hERG potassium channel inhibitor, with an IC 50 of 88 nM, showing antiarrhythmic activity .
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- HY-12532R
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Histamine Receptor
Potassium Channel
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Inflammation/Immunology
Endocrinology
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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 .
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- HY-12533R
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Sodium Channel
Potassium Channel
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Cardiovascular Disease
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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 .
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- HY-16689
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Potassium Channel
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Others
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VU 0240551 is a potent neuronal K-Cl cotransporter KCC2 inhibitor (IC50=560 nM) and is selective versus NKCC1. VU 0240551 also inhibits hERG and L-type Ca 2+ channels. VU 0240551 attenuates GABA-induced hyperpolarization of P cells, produces a positive shift in the P cell GABA reversal potential and enhances P cell synaptic transmission .
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- HY-149305
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- HY-B1193R
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Potassium Channel
Histamine Receptor
Na+/Ca2+ Exchanger
Caspase
Apoptosis
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Inflammation/Immunology
Endocrinology
Cancer
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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 .
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- HY-131335
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p38 MAPK
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Inflammation/Immunology
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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 .
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- HY-N1934R
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Potassium Channel
HSP
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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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 .
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- HY-151920
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Btk
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Inflammation/Immunology
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BTK-IN-17 (compound 36R) is a selective and orally activeBTK inhibitor with an IC50 value of 13.7 nM. BTK-IN-17 decreases the expression of p-BTK Y223 and p-PLCγ2 Y1217. BTK-IN-17 shows anti-inflammatory effects .
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- HY-146158
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Bacterial
Potassium Channel
Antibiotic
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Infection
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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.
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- HY-N1483
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Potassium Channel
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Cardiovascular Disease
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Guanfu base A is an antiarrhythmic alkaloid isolated from Aconitum coreanum and is a potent noncompetitive CYP2D6 inhibitor, with a Ki of 1.20 μM in human liver microsomes (HLMs) and a Ki of 0.37 μM for the human recombinant form (rCYP2D6). Guanfu base A is also a potent competitive inhibitor of CYP2D in monkey (Ki of 0.38 μM) and dog (Ki of 2.4 μM) microsomes . Guanfu base A also inhibits HERG channel current .
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- HY-133012
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TRP Channel
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Neurological Disease
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GFB-8438 is a potent and subtype selective TRPC5 inhibitor, with IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. GFB-8438 shows excellent selectivity against TRPC6, other TRP family members, NaV 1.5, as well as limited activity against the hERG channel. GFB-8438 protects mouse podocytes from injury induced by protamine sulfate model .
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- HY-149431
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HSP
Potassium Channel
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Cancer
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NDNA4 (compound 17) is a selective inhibitor of Hsp90α (IC50: 0.34 μM). NDNA4 is a permanently charged analog with low membrane permeability and low cytotoxicity against Ovcar-8 and MCF-10A ((IC50 >100 μM)). NDNA4 prevents disruption of hERG channel maturation without generating a heat shock response or causing degradation of Hsp90α-dependent client proteins .
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- HY-100001
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TRP Channel
CRAC Channel
Potassium Channel
Autophagy
Apoptosis
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Cardiovascular Disease
Cancer
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SKF-96365 hydrochloride is a potent TRP channel blocker and a store-operated Ca 2+ entry (SOCE) inhibitor. SKF-96365 hydrochloride significantly inhibits hERG, hKCNQ1/hKCNE1, hKir2.1 and hKv4.3 current, and significantly prolongs the QTc interval in isolated guinea pig hearts. SKF-96365 hydrochloride exhibits potent anti-neoplastic activity by inducing cell-cycle arrest and apoptosis in colorectal cancer cells .
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- HY-119101
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CCR
Potassium Channel
P-glycoprotein
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Inflammation/Immunology
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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 .
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- HY-149432
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HSP
Potassium Channel
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Cancer
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NDNA3 (compound 14) is a selective inhibitor of Hsp90α (IC50: 0.51 μM). NDNA3 is a permanently charged analog with low membrane permeability and low toxicity to Ovcar-8 (IC50: 12.66 μM) and MCF-10A (IC50: 11.72 μM) cells. NDNA3 prevents disruption of hERG channel maturation without generating a heat shock response or causing degradation of Hsp90α-dependent client proteins .
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- HY-148825
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- HY-163765
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PI4K
Potassium Channel
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Infection
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Antimalarial agent 41 (Compound 17) exhibits antimalarial activity, which inhibits Plasmodium falciparum with an IC50 of 40 nM (NF54 strain) and 76 nM (K1 strain). Antimalarial agent 41 is an inhibitor for P. falciparum phosphatidylinositol-4-kinase β (Pf PI4K) and hERG channel, with an IC50 of 53 nM and 3 μM. Antimalarial agent 41 exhibits cytotoxicity to CHO cells with an IC50 of 34 μM. Antimalarial agent 41 ameliorates the malaria infection and exhibits good pharmacokinetic characters in mouse models .
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- HY-12946A
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Glucocorticoid Receptor
Cytochrome P450
HCV Protease
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Infection
Inflammation/Immunology
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BI 653048 phosphate is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM . BI 653048 phosphate inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM) . BI 653048 phosphate is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus .
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- HY-12946
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Glucocorticoid Receptor
Cytochrome P450
HCV Protease
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Infection
Inflammation/Immunology
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BI 653048 is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM . BI 653048 inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM) . BI 653048 is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus .
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- HY-119886
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Others
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Neurological Disease
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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 .
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- HY-12708
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Dopamine Receptor
Cytochrome P450
Autophagy
5-HT Receptor
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Cardiovascular Disease
Neurological Disease
Cancer
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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 .
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- HY-B0407A
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Dopamine Receptor
Autophagy
Cytochrome P450
5-HT Receptor
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Cardiovascular Disease
Neurological Disease
Cancer
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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 .
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- HY-146468
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Dipeptidyl Peptidase
GPR119
Potassium Channel
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Metabolic Disease
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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.
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- HY-147691
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Glutathione Peroxidase
Potassium Channel
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Inflammation/Immunology
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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 .
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| Cat. No. |
Product Name |
Type |
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- HY-100545
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Chelators
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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 .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P5177
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- HY-P1440A
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Potassium Channel
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Neurological Disease
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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.
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- HY-P5795
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Sodium Channel
Potassium Channel
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Neurological Disease
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GsAF-I is a potent Nav and hERG1 channels blocker with IC50s of 0.36, 0.6, 1.28, 0.33, 1.2, 0.04 and 4.8 μM against Nav1.1, Nav1.2, Nav1.3, Nav1.4, Nav1.6, Nav1.7 and hERG1, respectively .
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Category |
Target |
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* This product has been "discontinued".
Optimized version of product available:
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Product Name |
Chemical Structure |
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- HY-B0369AS
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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.
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- HY-103309S
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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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