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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
56 Results for "
hERG current
" in MedChemExpress (MCE) Product Catalog:
Products (56)
56 Results for "hERG current" in MCE Product Catalog:
Target:
製品番号: HY-B1482AS
CAS 番号: 2514954-64-2
製品番号: HY-12533B
CAS 番号: 54687-36-4
別名: Dicorantil hydrochloride; SC-7031 hydrochloride
Target:
研究分野:
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 .
製品番号: HY-10562AR
CAS 番号: 83846-83-7
別名: R41468 tartrate (Standard)
Ketanserin (tartrate) (Standard) is the analytical standard of Ketanserin (tartrate). This product is intended for research and analytical applications. Ketanserin (R41468) tartrate is a selective 5-HT2 receptor antagonist. Ketanserin tartrate also blocks hERG current (IhERG) in a concentration-dependent manner (IC50=0.11 μM).
Target:
製品番号: HY-12533AR
CAS 番号: 22059-60-5
別名: Dicorantil phosphate (Standard); SC-7031 phosphate (Standard)
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 (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 .
製品番号: HY-W710915
製品番号: HY-18600AS
別名: NE-10064-d8 dihydrochloride
製品番号: HY-109968A
CAS 番号: 1005398-61-7
別名: CEP-26401 hydrochloride
Target:
研究分野:
Irdabisant (CEP-26401) hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant hydrochloride has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant hydrochloride has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant hydrochloride can be used to research schizophrenia or cognitive impairment .
製品番号: HY-108586R
CAS 番号: 343630-41-1
Target:
研究分野:
NS3623 (Standard) is the analytical standard of NS3623 (HY-108586). This product is intended for research and analytical applications. 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 .
製品番号: HY-17504AR
CAS 番号: 287714-41-4
別名: ZD 4522 (Standard)
研究分野:
Rosuvastatin (Standard) is the analytical standard of Rosuvastatin (HY-17504A). This product is intended for research and analytical applications. Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks hERG current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
製品番号: HY-182589
CAS 番号: 2290606-49-2
Target:
SRP-001 is an orally active, blood-brain barrier-permeable analgesic and antipyretic agent. SRP-001 reduces the expression level of FAAH, mildly inhibits hERG currents, generates AM404 (HY-101388), and maintains the integrity of hepatic tight junctions. SRP-001 exerts analgesic, antipyretic, and antinociceptive effects .
製品番号: HY-182638
CAS 番号: 1829530-11-1
別名: CPL500036
研究分野:
Alofropodect is an orally active, blood-brain barrier permeable phosphodiesterase 10A (PDE10A) inhibitor with IC50 values of 1 nM (Reference 1) and 35 nM (Reference 2). Alofropodect acts as a negative allosteric modulator of the M2 muscarinic receptor with an IC50 of 9.2 μM. Alofropodect alters cyclic nucleotide levels in basal ganglia circuits, inhibits the hydrolysis of cAMP and cGMP, and suppresses hERG potassium channel tail currents. Alofropodect induces catalepsy in rats and reverses injury-induced contralateral forelimb use impairment. Alofropodect can be used in research related to schizophrenia, Parkinson's disease, and levodopa-induced dyskinesia .
製品番号: HY-109968R
CAS 番号: 1005402-19-6
別名: CEP-26401 (Standard)
Irdabisant (Standard) is the analytical standard of Irdabisant (HY-109968). This product is intended for research and analytical applications. Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment .
製品番号: 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.
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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
