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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
19 Results for "
hERG binding
" in MedChemExpress (MCE) Product Catalog:
Products (19)
19 Results for "hERG binding" in MCE Product Catalog:
2
2 Cited Publications
Synonyms: Dicorantil; SC-7031
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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 .
2
2 Cited Publications
Synonyms: Dicorantil phosphate; SC-7031 phosphate
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Research Areas:
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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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 .
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 .
Cat. No.: HY-128866
CAS No.: 2332841-25-3
TBAJ-876 is an orally active diarylquinoline anti-Mycobacterium agent. TBAJ-876 regulates energy metabolism by targeting the c and ε subunits of Mycobacterium tuberculosis F-ATP synthase, exerts bactericidal activity against replicating Mycobacterium tuberculosis, and retains activity against strains carrying the Rv0678 mutation. TBAJ-876 undergoes N-demethylation in vivo to form its major active metabolite TBAJ-876-M3, which has lower lipophilicity and hERG potassium channel binding affinity. TBAJ-876 is well tolerated in BALB/c mice and significantly reduces the colony-forming units of Mycobacterium tuberculosis in the lungs. In addition, TBAJ-876 exhibits inhibitory activity against Mycobacterium abscessus, reduces bacterial loads in the lungs and spleens of infected mice, and shows no antagonistic effect when used in combination with common antibiotics. TBAJ-876 can be used in studies related to tuberculosis and Mycobacterium abscessus pulmonary diseases .
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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 .
Cat. No.: HY-12938
CAS No.: 1215868-94-2
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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 .
Cat. No.: HY-161873
CAS No.: 2573850-59-4
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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) .
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Sodium Channel inhibitor 1 is a state-dependent voltage-gated NaV1.7 inhibitor with an IC50 of 0.087 μM. Sodium Channel inhibitor 1 can be used for research of pain .
Cat. No.: HY-143315
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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 .
Cat. No.: HY-12533B
CAS No.: 54687-36-4
Synonyms: Dicorantil hydrochloride; SC-7031 hydrochloride
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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 .
Cat. No.: HY-147691
CAS No.: 2476764-11-9
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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 .
Cat. No.: HY-12533AR
CAS No.: 22059-60-5
Synonyms: Dicorantil phosphate (Standard); SC-7031 phosphate (Standard)
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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 .
Research Areas:
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 .
Cat. No.: HY-119886
CAS No.: 1801151-08-5
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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 .
Cat. No.: HY-159958
CAS No.: 3037315-44-6
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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 .
Cat. No.: HY-124283
CAS No.: 1228660-00-1
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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 .
Cat. No.: HY-125447
CAS No.: 145941-07-7
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Cat. No.: HY-182385
CAS No.: 1628945-93-6
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BPN-14136 is an orally effective retinol-binding protein 4 (RBP4) inhibitor. BPN-14136 inhibits the binding of retinol to RBP4 with an IC50 of 12.8 nM. BPN-14136 inhibits retinol-dependent RBP4-transthyretin interaction (IC50 = 43.6 nM) and reduces circulating plasma RBP4 levels in vivo. BPN-14136 decreases the formation of cytotoxic bisretinoids in retinal pigment epithelial cells. BPN-14136 can be used for the research of atrophic age-related macular degeneration and Stargardt disease .
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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
