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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 "
cardiac repolarization
" in MedChemExpress (MCE) Product Catalog:
Products (19)
19 Results for "cardiac repolarization" in MCE Product Catalog:
30
Research Areas:
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 .
3
3 Cited Publications
Target:
Research Areas:
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 .
2
2 Cited Publications
Synonyms: R 51619; (±)-Cisaprid
Target:
Research Areas:
Cisapride (R 51619) is an orally active, selective 5-HT4 receptor agonist with an EC50 of 140 nM. Cisapride also acts as an hERG potassium channel blocker with an IC50 of 9.4 nM. Cisapride exerts gastrointestinal prokinetic effects by activating 5-HT4 receptors, but it also blocks the hERG potassium channel responsible for the repolarization phase of cardiac action potentials, delaying repolarization and thus prolonging the action potential duration . Cisapride can be used in research related to gastrointestinal dysfunction, gastroesophageal reflux disease, functional dyspepsia, chronic gastritis, gastroparesis, ulcerative colitis and necrotizing enterocolitis .
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Target:
Research Areas:
Eleclazine (GS 6615) hydrochloride is a selective cardiac late sodium current inhibitor and a weak inhibitor of potassium current with IC50 value of <1 μM and approximately 14.2 μM, respectively. Eleclazine hydrochloride shows concurrent protection against autonomically induced atrial premature beats, repolarization alternans and heterogeneity, and atrial fibrillation in porcine model. Eleclazine hydrochloride can be used to research cardiac arrhythmias .
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Target:
Research Areas:
Eleclazine (GS 6615) is a selective cardiac late sodium current inhibitor and a weak inhibitor of potassium current with IC50 of <1 μM and approximately 14.2 μM, respectively. Eleclazine shows concurrent protection against autonomically induced atrial premature beats, repolarization alternans and heterogeneity, and atrial fibrillation in porcine model. Eleclazine can be used to research cardiac arrhythmias .
2
2 Cited Publications
Cat. No.: HY-14149A
CAS No.: 260779-88-2
Synonyms: R 51619 monohydrate; (±)-Cisaprid monohydrate
Research Areas:
Cisapride (R 51619) monohydrate is an orally active, selective 5-HT4 receptor agonist with an EC50 of 140 nM. Cisapride monohydrate also acts as an hERG potassium channel blocker with an IC50 of 9.4 nM. Cisapride monohydrate exerts gastrointestinal prokinetic effects by activating 5-HT4 receptors, but it also blocks the hERG potassium channel responsible for the repolarization phase of cardiac action potentials, delaying repolarization and thus prolonging the action potential duration . Cisapride monohydrate can be used in research related to gastrointestinal dysfunction, gastroesophageal reflux disease, functional dyspepsia, chronic gastritis, gastroparesis, ulcerative colitis and necrotizing enterocolitis .
1
1 Cited Publications
Target:
Research Areas:
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. ICA-105574 can prevent arrhythmias induced by cardiac delayed repolarization. ICA-105574 shortens action potential duration in ventricular myocytes concentration-dependently .
Cat. No.: HY-136832
CAS No.: 110514-35-7
Research Areas:
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-17504AS1
CAS No.: 2070009-40-2
Synonyms: ZD 4522-d6
Cat. No.: HY-17504AS
CAS No.: 1133429-16-9
Synonyms: ZD 4522 d3
Rosuvastatin-d3 is the deuterated-labeled Rosuvastatin (HY-17504A). 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 .
Cat. No.: HY-12773A
CAS No.: 86383-32-6
Synonyms: GPV-129 hydrochloride
Target:
Research Areas:
5-Hydroxy Propafenone (hydrochloride) is an inhibitor of cardiac myocyte repolarizing currents. 5-Hydroxy Propafenone is an active metabolite of propafenone. 5-Hydroxy Propafenone (hydrochloride) inhibits transient outward potassium current (Ito) in isolated human arterial myocytes with an IC50 of 1.5 μM. 5-Hydroxy Propafenone (hydrochloride) is potent Ito inhibitor in neonatal rat ventricular myocytes .
Cat. No.: HY-14149R
CAS No.: 81098-60-4
Synonyms: R 51619 (Standard); (±)-Cisaprid (Standard)
Research Areas:
Cisapride (R 51619) (Standard) is the analytical standard of Cisapride (HY-14149). This product is intended for research and analytical applications. Cisapride (R 51619) is an orally active, selective 5-HT4 receptor agonist with an EC50 of 140 nM. Cisapride also acts as an hERG potassium channel blocker with an IC50 of 9.4 nM. Cisapride exerts gastrointestinal prokinetic effects by activating 5-HT4 receptors, but it also blocks the hERG potassium channel responsible for the repolarization phase of cardiac action potentials, delaying repolarization and thus prolonging the action potential duration . Cisapride can be used in research related to gastrointestinal dysfunction, gastroesophageal reflux disease, functional dyspepsia, chronic gastritis, gastroparesis, ulcerative colitis and necrotizing enterocolitis .
Cat. No.: HY-14149S
CAS No.: 2738376-71-9
Synonyms: R51619-d6; (±)-Cisaprid-d6
Research Areas:
Cisapride-d6 (R51619-d6) is the deuterated-labeled Cisapride (HY-14149). Cisapride (R 51619) is an orally active, selective 5-HT4 receptor agonist with an EC50 of 140 nM. Cisapride also acts as an hERG potassium channel blocker with an IC50 of 9.4 nM. Cisapride exerts gastrointestinal prokinetic effects by activating 5-HT4 receptors, but it also blocks the hERG potassium channel responsible for the repolarization phase of cardiac action potentials, delaying repolarization and thus prolonging the action potential duration . Cisapride can be used in research related to gastrointestinal dysfunction, gastroesophageal reflux disease, functional dyspepsia, chronic gastritis, gastroparesis, ulcerative colitis and necrotizing enterocolitis .
Cat. No.: HY-W777120
CAS No.: 1285970-69-5
Synonyms: R 51619-13C,d3; (±)-Cisaprid-13C,d3
Research Areas:
Cisapride- 13C,d3 (R 51619- 13C,d3) is the deuterated, 13C-labeled Cisapride (HY-14149). Cisapride (R 51619) is an orally active, selective 5-HT4 receptor agonist with an EC50 of 140 nM. Cisapride also acts as an hERG potassium channel blocker with an IC50 of 9.4 nM. Cisapride exerts gastrointestinal prokinetic effects by activating 5-HT4 receptors, but it also blocks the hERG potassium channel responsible for the repolarization phase of cardiac action potentials, delaying repolarization and thus prolonging the action potential duration . Cisapride can be used in research related to gastrointestinal dysfunction, gastroesophageal reflux disease, functional dyspepsia, chronic gastritis, gastroparesis, ulcerative colitis and necrotizing enterocolitis .
Cat. No.: HY-16738AR
CAS No.: 1448754-43-5
Synonyms: GS 6615 hydrochloride (Standard)
Research Areas:
Eleclazine (hydrochloride) (Standard) is the analytical standard of Eleclazine (hydrochloride). This product is intended for research and analytical applications. Eleclazine (GS 6615) hydrochloride is a selective cardiac late sodium current inhibitor and a weak inhibitor of potassium current with IC50 value of <1 μM and approximately 14.2 μM, respectively. Eleclazine hydrochloride shows concurrent protection against autonomically induced atrial premature beats, repolarization alternans and heterogeneity, and atrial fibrillation in porcine model. Eleclazine hydrochloride can be used to research cardiac arrhythmias .
Cat. No.: HY-111747R
CAS No.: 2252316-16-6
Target:
Research Areas:
TBAJ-587 (Standard) is the analytical standard of TBAJ-587 (HY-111747). This product is intended for research and analytical applications. 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 .
Cat. No.: HY-17504AR
CAS No.: 287714-41-4
Synonyms: ZD 4522 (Standard)
Research Areas:
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 .
Cat. No.: HY-13551C
CAS No.: 80277-14-1
Synonyms: m-AMSA isethionate; Acridinyl anisidide isethionate
Target:
Topoisomerase DNA/RNA Synthesis DNA Alkylator/Crosslinker ERK Akt GSK-3 Bcl-2 Family Caspase Apoptosis Potassium Channel
Research Areas:
Amsacrine isethionate (m-AMSA isethionate) is a Topoisomerase II inhibitor. Amsacrine isethionate intercalates into DNA. Amsacrine isethionate induces Ca 2+-mediated inactivation of ERK, and also downregulates AKT, promoting MCL1 downregulation mediated by GSK3β via reducing the phosphorylation level of GSK3β. Amsacrine isethionate induces Apoptosis by activating Caspase-9 and Caspase-3. Amsacrine isethionate blocks HERG potassium channels in the open/inactivated state. Amsacrine isethionate induces chromosomal aberrations and sister chromatid exchanges, and inhibits the synthesis of RNA and DNA. Amsacrine isethionate exhibits anti-leukemic activity. Amsacrine isethionate causes cardiac repolarization disorders, QT interval prolongation, ventricular arrhythmias, and increases the risk of sudden cardiac death. Amsacrine isethionate can be used in research related to acute myeloid leukemia, lymphoma and progressive malignancies .
Cat. No.: HY-13551D
CAS No.: 80277-11-8
Synonyms: m-AMSA lactate; Acridinyl anisidide lactate
Target:
Topoisomerase DNA/RNA Synthesis DNA Alkylator/Crosslinker ERK Akt GSK-3 Bcl-2 Family Caspase Apoptosis Potassium Channel
Research Areas:
Amsacrine lactate (m-AMSA lactate) is a Topoisomerase II inhibitor. Amsacrine lactate intercalates into DNA. Amsacrine lactate induces Ca 2+-mediated inactivation of ERK, and also downregulates AKT, promoting MCL1 downregulation mediated by GSK3β via reducing the phosphorylation level of GSK3β. Amsacrine lactate induces Apoptosis by activating Caspase-9 and Caspase-3. Amsacrine lactate blocks HERG potassium channels in the open/inactivated state. Amsacrine lactate induces chromosomal aberrations and sister chromatid exchanges, and inhibits the synthesis of RNA and DNA. Amsacrine lactate exhibits anti-leukemic activity. Amsacrine lactate causes cardiac repolarization disorders, QT interval prolongation, ventricular arrhythmias, and increases the risk of sudden cardiac death. Amsacrine lactate can be used in research related to acute myeloid leukemia, lymphoma and progressive malignancies .
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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
