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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
25 Results for "
hERG ion channels
" in MedChemExpress (MCE) Product Catalog:
Products (25)
25 Results for "hERG ion channels" in MCE Product Catalog:
2
2 Cited Publications
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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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1 Cited Publications
Cat. No.: HY-16915
CAS No.: 668463-35-2
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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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1 Cited Publications
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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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1 Cited Publications
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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 .
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 .
Cat. No.: HY-136832
CAS No.: 110514-35-7
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Noribogaine hydrochloride is an orally active, blood-brain barrier permeable SERT inhibitor (IC50=50-300 nM) and hERG channel blocker. Noribogaine hydrochloride enhances serotonergic transmission, activates the κ-opioid receptor (OPRK) G protein signaling pathway and inhibits β-arrestin recruitment. Meanwhile, Noribogaine hydrochloride blocks the μ-opioid receptor (OPRM) signaling pathway as well as ion channels associated with cardiac repolarization. Noribogaine hydrochloride induces neuritogenesis, upregulates GDNF mRNA expression, and modulates opioid tolerance. Noribogaine hydrochloride reduces alcohol-seeking behavior in experimental animals, and is widely used in studies related to depression, addiction, alcoholism, and cardiotoxicity .
Cat. No.: HY-117948
CAS No.: 1560968-49-1
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ML399 is a Menin-MLL1 protein-protein interaction inhibitor with an IC50 of 90 nM. ML399 inhibits the proliferation of transformed mouse bone marrow cells. ML399 binds to the hERG potassium channel, exhibits superior in vitro physicochemical, drug metabolism and pharmacokinetic (DMPK) parameters, and has an extended half-life in rodents. ML399 can be used for research on acute myeloid leukemia and acute lymphoblastic leukemia .
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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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BI 653048, a chemical probe, 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 (Compound 103) is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus .
Cat. No.: HY-12946A
CAS No.: 1198784-97-2
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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 .
Cat. No.: HY-12082
CAS No.: 459133-38-1
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GSK369796 is an affordable and effective antimalarial and inhibits hERG potassium ion channel repolarization with an IC50 of 7.5 μM .
Cat. No.: HY-156976
CAS No.: 343935-60-4
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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 .
Cat. No.: HY-156976A
CAS No.: 343935-48-8
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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 .
Cat. No.: HY-163590
CAS No.: 3034034-32-4
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PRMT5-IN-41 (compound 130) is a potent and orally active PRMT5 inhibitor. PRMT5-IN-41 inhibits hERG ion channel with IC50 value of 1.36 µM .
Cat. No.: HY-170511
CAS No.: 2757506-39-9
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GLP-1 receptor agonist 15 (Example 4) is a GLP receptor agonist with an EC50 of 0.74 nM. The IC50 for the hERG potassium ion channel is 10.1 μM. GLP-1 receptor agonist 15 can be used for research in the field of diabetes .
Cat. No.: HY-103268
CAS No.: 1227163-56-5
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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 .
Cat. No.: HY-L923
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.: HY-187550
CAS No.: 1771650-41-9
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BRD7929 is an orally active phenylalanyl-tRNA synthetase (PheRS) inhibitor and parasiticide, with an IC50 value of 0.023 μM against Plasmodium falciparum PheRS. BRD7929 inhibits the aminoacylation activity of the target enzyme, blocking protein synthesis, DNA replication and parasite nuclear division. BRD7929 clears the asexual blood stage, liver stage and mature gametocyte stage of malaria parasite species, and prevents parasite transmission to mosquitoes. BRD7929 shows moderate cytotoxicity against mammalian cells and inhibits hERG ion channels. BRD7929 achieves cure of malaria in animal models. BRD7929 can be used in research related to cryptosporidiosis and malaria .
Cat. No.: HY-175804
CAS No.: 2260797-32-6
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 .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
