Search Result
Results for "
hERG
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
8
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-163421
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Potassium Channel
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Cancer
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hERG-IN-2 (Compound 1) is a potent hERG inhibitor, with an IC50 of < 2 μM. hERG-IN-2 can be used for the research of cancer .
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- HY-155462
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Bacterial
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Infection
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hERG-IN-1 (compound 2a) is an antibacterial agent and inhibitor of hERG. hERG-IN-1 inhibits pulmonary infection caused by Pseudomonas aeruginosa strain ATCC 27853 .
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- HY-118172
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- HY-153690
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Others
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Others
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Progranulin modulator-1 (Compound 60) is an orally active enhancer of progranulin (PGRN) secretion. Progranulin modulator-1 enhances the potency of BV-2 cell to increase PGRN levels, has inhibitory effect on hERG and Low cytotoxicity, the PGRN EC50 and hERG IC50 were 83 and 3100 nM, respectively .
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- HY-160658
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CCR
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Inflammation/Immunology
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AZ760 is a CCR8 antagonist. AZ760 shows excellent potency, good lipophilicity and high free fraction in blood. AZ760 exhibits unacceptable hERG inhibition .
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- HY-17504D
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HMG-CoA Reductase (HMGCR)
Potassium Channel
Autophagy
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Cardiovascular Disease
Metabolic Disease
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(3S,5R)-Rosuvastatin is the (3S,5R)-enantiomer of Rosuvastatin. Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM . Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM . Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
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- HY-17504C
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HMG-CoA Reductase (HMGCR)
Potassium Channel
Autophagy
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Cardiovascular Disease
Metabolic Disease
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(3R,5R)-Rosuvastatin is the (3R,5R)-enantiomer of Rosuvastatin. Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM . Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM . Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
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- HY-17508
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Bacterial
Cytochrome P450
Autophagy
Antibiotic
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Infection
Cancer
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Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC50 (Ki) value of 56 (43) μM . Clarithromycin significantly inhibits the HERG potassium current .Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K .
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- HY-100321
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-
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- HY-17504B
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ZD 4522 Sodium; X-Plended Sodium; Crestor Sodium
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HMG-CoA Reductase (HMGCR)
Potassium Channel
Autophagy
Bacterial
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Cardiovascular Disease
Metabolic Disease
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Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
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- HY-149013
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Bacterial
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Infection
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Anti-MRSA agent 5 (B14) is a potent MRSAagent with MIC50 values of 0.38 μg/mL and has low hERG activity with an IC50 values of >40 μM. Anti-MRSA agent 5 (B14) also has low cytotoxicity to mammal cells and unlikely to acquire bacterial resistance .
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- HY-124687
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- HY-146328
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Bacterial
Antibiotic
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Infection
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PqsR/LasR-IN-2 (Compound 3) is a potent inhibitor of PqsR and LasR systems in P. aeruginosa. PqsR/LasR-IN-2 also inhibits hERG with the IC50 of 1.408 µM .
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- HY-146329
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Bacterial
Antibiotic
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Infection
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PqsR/LasR-IN-3 (Compound 7a) is a potent inhibitor of PqsR and LasR systems in P. aeruginosa. PqsR/LasR-IN-3 also inhibits hERG with the IC50 of 109.01 µM .
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- HY-156759
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METTL3
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Cancer
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METTL3-IN-5 (Compound 13) is a METTL3 inhibitor. METTL3-IN-5 inhibits MOLM-13 growth with an IC50 less than 2 μM. METTL3-IN-5 has weak hERG inhibitory activity (IC50 >30 μM). METTL3-IN-5 can be used for AML research .
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- HY-17504BS2
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ZD 4522-13C,d3 sodium; X-Plended-13C,d3 sodium; Crestor-13C,d3 sodium
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Autophagy
Bacterial
HMG-CoA Reductase (HMGCR)
Potassium Channel
Isotope-Labeled Compounds
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Cardiovascular Disease
Metabolic Disease
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Rosuvastatin- 13C,d3 sodium is 13C and deuterated labeled Rosuvastatin sodium (HY-17504B). Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
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- HY-17504
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Rosuvastatin hemicalcium; ZD 4522 Calcium
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HMG-CoA Reductase (HMGCR)
Autophagy
Potassium Channel
Bacterial
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Cardiovascular Disease
Metabolic Disease
Cancer
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Rosuvastatin Calcium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Calcium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Calcium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Calcium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
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- HY-16489
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Potassium Channel
mAChR
Calcium Channel
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Metabolic Disease
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Terodiline, an antispasmodic agent, blocks hERG current with the IC50 of 375 nM. Terodiline has both anticholinergic and calcium antagonist properties, and effectively reduces abnormal bladder contractions caused by detrusor instability. Terodiline can be used for the research of urinary incontinence .
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- HY-17504A
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ZD 4522
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HMG-CoA Reductase (HMGCR)
Autophagy
Potassium Channel
Bacterial
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Cardiovascular Disease
Metabolic Disease
Cancer
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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 .
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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
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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-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-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-157303
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Somatostatin Receptor
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Cardiovascular Disease
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SSTR5 antagonist 3 (Compound 23) is an orally active somatostatin receptor subtype 5 (SSTR5) antagonist with low hERG inhibition. SSTR5 antagonist 3 exhibits potency with IC50 values of 2.8 nM and 1.4 nM in human and mouse, respectively. SSTR5 antagonist 3 can be used for the research of anti-gallstone .
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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-14149
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R 51619; (±)-Cisaprid
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5-HT Receptor
Potassium Channel
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Neurological Disease
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Cisapride (R 51619) is an orally active 5-HT4 receptor agonist with an EC50 value of 140 nM. Cisapride is a hERG blocker with an IC50 value of 9.4 nM. Cisapride is a gastroprokinetic agent that stimulates gastrointestinal motor activity .
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- HY-147841
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HIV
Reverse Transcriptase
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Infection
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HIV-1 inhibitor-41 (Compound B23) is an orally active non-nucleoside HIV-1 reverse transcriptase inhibitor with EC50 values of 20.8 nM and 50 nM against HIV-1 WT and mutant E138K strain, respectively. HIV-1 inhibitor-41 shows low hERG, no apparent CYP enzymatic inhibition and no acute toxicity .
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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-144437
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TGF-β Receptor
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Cancer
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ALK5-IN-9 (Compound 8h) is a potent and orally active inhibitor of TGFβRI (ALK5). ALK5-IN-9 inhibits ALK5 autophosphorylation and NIH3T3 cell activity with IC50 values of 25 nM and 74.6 nM, respectively. ALK5-IN-9 also shows favorable pharmacokinetic profile and ameliorated hERG inhibition. ALK5-IN-9 has the potential for the research of cancer disease .
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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-14149A
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R 51619 monohydrate; (±)-Cisaprid monohydrate
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5-HT Receptor
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Neurological Disease
Metabolic Disease
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Cisapride monohydrate is an orally and potent 5-HT4 receptor agonist and hERG inhibitor. Cisapride monohydrate is an prokinetic agent which facilitates or restores motility throughout the length of the gastrointestinal tract. Cisapride monohydrate stimulates gastrointestinal motor activity through an indirect mechanism involving the release of acetylcholine mediated by postganglionic nerve endings in the myenteric plexus of the gut .
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- HY-14149R
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5-HT Receptor
Potassium Channel
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Neurological Disease
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Cisapride (Standard) is the analytical standard of Cisapride. This product is intended for research and analytical applications. Cisapride (R 51619) is an orally active 5-HT4 receptor agonist with an EC50 value of 140 nM. Cisapride is a hERG blocker with an IC50 value of 9.4 nM. Cisapride is a gastroprokinetic agent that stimulates gastrointestinal motor activity .
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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-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-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-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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- 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-19620
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LMI070; NVS-SM1
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DNA/RNA Synthesis
Potassium Channel
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Cancer
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Branaplam (LMI070; NVS-SM1) is a highly potent, selective and orally active survival motor neuron-2 (SMN2) splicing modulator with an EC50 of 20 nM for SMN. Branaplam inhibits human-ether-a-go-go-related gene (hERG) with an IC50 of 6.3 μM. Branaplam elevates full-length SMN protein and extends survival in a severe spinal muscular atrophy (SMA) mouse model .
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- HY-19620A
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LMI070 hydrochloride; NVS-SM1 hydrochloride
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DNA/RNA Synthesis
Potassium Channel
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Cancer
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Branaplam (LMI070; NVS-SM1) hydrochloride is a highly potent, selective and orally active survival motor neuron-2 (SMN2) splicing modulator with an EC50 of 20 nM for SMN. Branaplam hydrochloride inhibits human-ether-a-go-go-related gene (hERG) with an IC50 of 6.3 μM. Branaplam hydrochloride elevates full-length SMN protein and extends survival in a severe spinal muscular atrophy (SMA) mouse model .
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- HY-17504AS
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-
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- HY-B2136
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-
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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-17504R
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Rosuvastatin hemicalcium (Standard); ZD 4522 Calcium (Standard)
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HMG-CoA Reductase (HMGCR)
Autophagy
Potassium Channel
Bacterial
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Cardiovascular Disease
Metabolic Disease
Cancer
|
Rosuvastatin (Calcium) (Standard) is the analytical standard of Rosuvastatin (Calcium). This product is intended for research and analytical applications. Rosuvastatin Calcium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Calcium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Calcium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Calcium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
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- HY-109968A
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CEP-26401 hydrochloride
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Histamine Receptor
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Neurological Disease
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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 .
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- HY-109968
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CEP-26401
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Histamine Receptor
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Neurological Disease
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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 .
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- HY-B2179
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- HY-B2133
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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-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-109036
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- HY-163155
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- HY-120375
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- HY-120713
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HCV
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Infection
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MK-8325 (dihydrochloride) is an inhibitor of HCV NS5A with oral activity. MK-8325 exhibits minimal inhibition on hERG at the concentration of 30 mM .
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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-P1440
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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-17508S1
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Isotope-Labeled Compounds
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Others
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Clarithromycin-d3is the deuterium labeledClarithromycin(HY-17508) . Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC50 (Ki) value of 56 (43) μM . Clarithromycin significantly inhibits the HERG potassium current .Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K .
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- HY-17508R
-
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Bacterial
Cytochrome P450
Autophagy
Antibiotic
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Infection
Cancer
|
Clarithromycin (Standard) is the analytical standard of Clarithromycin. This product is intended for research and analytical applications. Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC50 (Ki) value of 56 (43) μM . Clarithromycin significantly inhibits the HERG potassium current .Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K .
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- HY-N5006
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- HY-B0369AS
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iGluR
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Neurological Disease
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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-162359
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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
|
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-P5177
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- HY-122167
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- HY-10562
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- HY-N1933
-
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Potassium Channel
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Cardiovascular Disease
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Allocryptopine, a derivative of tetrahydropalmatine, is extracted from Macleaya cordata (Thunb.) Pers. Papaveraceae. Allocryptopine has antiarrhythmic effects and potently blocks human ether-a-go-go related gene (hERG) current .
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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-10562A
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- HY-101622
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5-HT Receptor
Dopamine Receptor
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5-HT6/7 antagonist 1 is a multifunctional ligand that antagonizes 5-HT6/7/2A and D2 receptors, without interacting with M1 receptors and hERG channels.
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- HY-N0221
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(R,R)-Daurisoline
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Autophagy
Potassium Channel
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Cancer
|
Daurisoline is a bis-benzylisoquinoline alkaloid that can be isolated from Menispermum dauricum and Rhizoma Menispermi. Daurisoline exerts a blocking effect on hERG and has antiarrhythmic effects. Daurisoline is a potent autophagy blocker that can be used for the research of cancer .
|
-
- HY-14848
-
PRX 00023
|
5-HT Receptor
Potassium Channel
|
Neurological Disease
|
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.
|
-
- HY-18719
-
|
Estrogen Receptor/ERR
Potassium Channel
|
Cancer
|
Endoxifen Z-isomer is the most important Tamoxifen metabolite, inducing an anti-estrogenic effect in breast cancer cells expressing ERα. Endoxifen Z-isomer inhibits hERG. This effect is concentration-dependent, with an IC50 value of 1.6 μM.
|
-
- HY-B1167
-
Cardiorythmine; (+)-Ajmaline
|
Sodium Channel
|
Cardiovascular Disease
|
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 .
|
-
- HY-153240
-
|
CXCR
|
Inflammation/Immunology
|
ACT-672125 is a potent CXCR3 antagonist with IC50 value of 239 nM in human blood. ACT-672125 has activity for hERG with IC50 value of 18μM. ACT-672125 can be used for the research of autoimmune diseases .
|
-
- HY-N1934
-
|
Potassium Channel
HSP
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
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 .
|
-
- HY-131350
-
|
Proteasome
Parasite
|
Infection
|
LXE408 is an orally active, non-competitive and kinetoplastid-selective proteasome inhibitor. LXE408 has an IC50 of 0.04 μM for L. donovani proteasome and an EC50 of 0.04 μM for L. donovani. LXE408 has a low propensity to cross the blood brain barrier. LXE408 has the potential for visceral leishmaniasis (VL) research .
|
-
- HY-158013
-
-
- HY-A0148AR
-
|
Parasite
|
Infection
|
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 .
|
-
- HY-100238
-
-
- HY-120356A
-
TAI-95 tosylate
|
Apoptosis
|
Cancer
|
T-1101 tosylate (TAI-95 tosylate) is a Hec1/Nek2 (Highly expressed in cancer 1 / NIMA-related kinase 2) inhibitor with antitumor activity. T-1101 tosylate is inactive toward normal cells, kinases and hERG
|
-
- HY-10562R
-
|
5-HT Receptor
Potassium Channel
Autophagy
|
Neurological Disease
|
Ketanserin (Standard) is the analytical standard of Ketanserin. This product is intended for research and analytical applications. Ketanserin is a selective 5-HT2 receptor antagonist. Ketanserin also blocks hERG current (IhERG) in a concentration-dependent manner (IC50=0.11 μM).
|
-
- HY-160031
-
|
GLP Receptor
|
Metabolic Disease
|
GLP-1R agonist 19 (M3190) is a potent and selective GLP-1R agonist. GLP-1R agonist 19 has excellent plasma stability, liver microsomal stability, and low hERG toxicity .
|
-
- HY-116838
-
|
Bacterial
|
Infection
|
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 .
|
-
- HY-14186
-
WYE-160020
|
Potassium Channel
|
Cardiovascular Disease
|
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 .
|
-
- HY-16916
-
NS1643
1 Publications Verification
|
Potassium Channel
Autophagy
|
Cancer
|
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 .
|
-
- HY-A0236A
-
|
Potassium Channel
|
Cardiovascular Disease
|
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.
|
-
- HY-102037
-
-
- HY-151191
-
|
Histone Demethylase
|
Cancer
|
LSD1-IN-22 is a potent Lysine-specific demethylase 1 (LSD1) inhibitor with a Ki value of 98 nM. LSD1-IN-22 has anti-proliferative activity against certain cancer cells .
|
-
- HY-P1440A
-
|
Potassium Channel
|
|
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.
|
-
- HY-124283A
-
|
Cannabinoid Receptor
|
Neurological Disease
|
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 .
|
-
- HY-157931
-
|
Histamine Receptor
|
Neurological Disease
|
Anticancer agent 192 (compound XXI) is a steroid-based histamine H3 receptor antagonist with no affinity for muscarinics and hERG. Anticancer agent 192 is quite stable in human and rat liver microsomes. Anticancer agent 192 can improve the cognitive level and reduce the degree of addiction in rats in the in vivo addiction test .
|
-
- HY-13044
-
-
- HY-B1193
-
-
- HY-100545
-
BAPTA-AM
Maximum Cited Publications
51 Publications Verification
|
Potassium Channel
|
Cardiovascular Disease
|
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 .
|
-
- HY-12533
-
Dicorantil; SC-7031
|
Sodium Channel
Potassium Channel
|
Cardiovascular Disease
|
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 .
|
-
- HY-134494
-
|
GPR68
|
Neurological Disease
|
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 .
|
-
- HY-12533A
-
Dicorantil phosphate; SC-7031 phosphate
|
Potassium Channel
Sodium Channel
|
Cardiovascular Disease
|
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 .
|
-
- HY-153952
-
-
- HY-N0221S
-
(R,R)-Daurisoline-d2
|
Isotope-Labeled Compounds
Potassium Channel
Autophagy
|
Cancer
|
Daurisoline-d2 is the deuterium labeled Daurisoline (HY-N0221). Daurisoline is a bis-benzylisoquinoline alkaloid that can be isolated from Menispermum dauricum and Rhizoma Menispermi. Daurisoline exerts a blocking effect on hERG and has antiarrhythmic effects. Daurisoline is a potent autophagy blocker that can be used for the research of cancer .
|
-
- HY-N0221S1
-
(R,R)-Daurisoline-d5
|
Isotope-Labeled Compounds
Potassium Channel
Autophagy
|
Cancer
|
Daurisoline-d5 is the deuterium labeled Daurisoline (HY-N0221). Daurisoline is a bis-benzylisoquinoline alkaloid that can be isolated from Menispermum dauricum and Rhizoma Menispermi. Daurisoline exerts a blocking effect on hERG and has antiarrhythmic effects. Daurisoline is a potent autophagy blocker that can be used for the research of cancer .
|
-
- HY-N0221S2
-
(R,R)-Daurisoline-d11
|
Isotope-Labeled Compounds
Potassium Channel
Autophagy
|
Cancer
|
Daurisoline-d11 is the deuterium labeled Daurisoline (HY-N0221). Daurisoline is a bis-benzylisoquinoline alkaloid that can be isolated from Menispermum dauricum and Rhizoma Menispermi. Daurisoline exerts a blocking effect on hERG and has antiarrhythmic effects. Daurisoline is a potent autophagy blocker that can be used for the research of cancer .
|
-
- HY-161349
-
|
Aminopeptidase
|
Inflammation/Immunology
|
LTA4H-IN-4 (compound 3) is an orally active LTA4H inhibitor. The IC50 value of LTA4H-IN-4 for hERG is 156 μM. LTA4H-IN-4 can be used in inflammation related studies .
|
-
- HY-B1167R
-
|
Sodium Channel
|
Cardiovascular Disease
|
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 .
|
-
- HY-12962
-
|
iGluR
|
Neurological Disease
|
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.
|
-
- HY-144341
-
|
Bacterial
|
Infection
|
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.
|
-
- HY-160656
-
|
5-HT Receptor
|
Neurological Disease
|
5-HT/NA Reuptake inhibitor-1 (compound 9) is a selective dual 5-HT and NA reuptake inhibitor with IC50 of 660 nM and 70 nM respectively. . 5-HT/NA Reuptake inhibitor-1 has good in vitro human metabolic stability, hERG selectivity and passive membrane permeability .
|
-
- HY-103268
-
|
Potassium Channel
|
Neurological Disease
|
(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 .
|
-
- HY-163387
-
|
Others
|
Inflammation/Immunology
Cancer
|
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 .
|
-
- HY-146327
-
|
Bacterial
Antibiotic
|
Infection
|
PqsR/LasR-IN-1 (compound 2a) is a potent PqsR and LasR systems inhibitor. PqsR/LasR-IN-1 has anti-virulence activity against Pseudomonas aeruginosa. PqsR/LasR-IN-1 can reduce production of biofilm, pyocyanin, and rhamnolipids in PA .
|
-
- HY-130244
-
|
Beta-secretase
|
Neurological Disease
|
BACE1-IN-5 (Compound 15) is a β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 9.1 nM, and also inhibits cellular amyloid-β (Aβ) with an IC50 of 0.82 nM. BACE1-IN-5 has a medicinal chemistry that improves hERG inhibition and P-gp efflux .
|
-
- HY-163110
-
|
HIV
Reverse Transcriptase
|
Infection
|
NNRT-IN-2 (compound 7w) is an orally available non-nucleoside reverse transcriptase inhibitor (NNRTI) with broad inhibitory effects on wild-type HIV-1 and mutant strains. NNRT-IN-2 inhibits HIV-1 reverse transcriptase with an EC50 of 22 nM. NNRT-IN-2 is insensitive to CYP and hERG and has good safety and pharmacokinetic characteristics .
|
-
- HY-16689
-
|
Potassium Channel
|
Others
|
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 .
|
-
- HY-111552
-
|
Pim
|
Cancer
|
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 .
|
-
- HY-107708
-
|
iGluR
Sigma Receptor
Potassium Channel
|
Neurological Disease
|
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 .
|
-
- HY-149305
-
-
- HY-160588
-
|
Sodium Channel
Potassium Channel
|
Neurological Disease
|
Nav1.8-IN-7 (Example 116) is a selective Nav1.8 inhibitor. Nav1.8-IN-7 shows an inhibition of >50% with 100 nM for Nav1.8. Nav1.8-IN-7 inhibits hERG with an IC50 of 15.6 μM. Nav1.8-IN-7 has the potential for pain research .
|
-
- HY-12533R
-
|
Sodium Channel
Potassium Channel
|
Cardiovascular Disease
|
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 .
|
-
- HY-12938
-
|
Beta-secretase
|
Neurological Disease
|
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 .
|
-
- HY-163154
-
-
- HY-B0480
-
(±)-Brompheniramine maleate
|
Histamine Receptor
mAChR
Potassium Channel
Sodium Channel
Calcium Channel
|
Neurological Disease
Inflammation/Immunology
Endocrinology
|
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 .
|
-
- HY-131335
-
|
p38 MAPK
|
Inflammation/Immunology
|
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 .
|
-
- HY-B0480A
-
-
- HY-157929
-
|
Keap1-Nrf2
|
Inflammation/Immunology
Cancer
|
Keap1-Nrf2-IN-19 (compound 33) is an oral active Keap1-Nrf2 protein–protein interaction (PPI) inhibitor with the Kd value of 0.0014 μM. Keap1-Nrf2-IN-19 exhibits less than 50% inhibition at 30 μM against hERG and 10 μM against CYPs .
|
-
- HY-121495
-
|
Parasite
|
Infection
|
BKI-1369 is a bumped kinase inhibitor (BKI). BKI-1369 increases human Ether-a-go-go-related gene (hERG)-inhibitory activity with an IC50 of 1.52 μM. BKI-1369 reduces the parasite burden and diseases severity in the gnotobiotic pig model. BKI-1369 has been well characterized for potency, stability, metabolism, toxicity, pharmacokinetics and is potent against C. parvum in infected mice and calves .
|
-
- HY-125820
-
|
Sigma Receptor
Potassium Channel
|
Neurological Disease
|
Sigma-1 receptor antagonist 3 (compound135) is a potent and selective Sigma-1 (σ1) receptor antagonist with a Ki of 1.14 nM. Sigma-1 receptor antagonist 3 inhibits Human Ether-a-go-go-Related Gene (hERG) with an IC50 of 1.54 μM. Sigma-1 receptor antagonist 3 has the potential for the neuropathic pain .
|
-
- HY-N1483
-
|
Potassium Channel
|
Cardiovascular Disease
|
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 .
|
-
- HY-133012
-
|
TRP Channel
|
Neurological Disease
|
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 .
|
-
- HY-149431
-
|
HSP
Potassium Channel
|
Cancer
|
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 .
|
-
- HY-163479
-
|
Eukaryotic Initiation Factor (eIF)
MNK
|
Cancer
|
MNK1/2-IN-7 (compound 20j) is an orally available inhibitor of MNK1/2 with anticancer activity and hERG safety. MNK1/2-IN-7 also inhibits the phosphorylation of eIF4E, inhibiting the MNK/eIF4E signaling pathway and cancer cell proliferation. MNK1/2-IN-7 is synergistic with Ibrutinib (HY-109970). .
|
-
- HY-158365
-
|
LRRK2
|
Neurological Disease
|
LRRK2-IN-14 (Compound 8) is an orally active LRRK2 inhibitor. LRRK2-IN-14 has an IC50 of 6.3 nM for LRRK2(G2019S) cell activity.LRRK2-IN-14 has an inhibitory effect on hERG (IC50=22 μM). LRRK2-IN-14 has blood-brain barrier permeability .
|
-
- HY-14188
-
|
Potassium Channel
Autophagy
|
Cardiovascular Disease
Cancer
|
Amiodarone hydrochloride, a benzofuran-based Class III antiarrhythmic agent, inhibits WT outwardIhERG tails with an IC50 of ∼45 nM . Amiodarone hydrochloride induces cell proliferation and myofibroblast differentiation via ERK1/2 and p38 MAPK signaling in fibroblasts . Amiodarone hydrochloride can be used in the research of both supraventricular and ventricular arrhythmias .
|
-
- HY-148144
-
-
- HY-151920
-
|
Btk
|
Inflammation/Immunology
|
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 .
|
-
- HY-148144A
-
-
- HY-100001
-
|
TRP Channel
CRAC Channel
Potassium Channel
Autophagy
Apoptosis
|
Cardiovascular Disease
Cancer
|
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 .
|
-
- HY-119101
-
|
CCR
Potassium Channel
P-glycoprotein
|
Inflammation/Immunology
|
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 .
|
-
- HY-146372
-
|
CXCR
|
Cancer
|
CXCR4 antagonist 5 (compound 23) is a highly potent CXCR4 antagonist with an IC50 value of 8.8 nM. CXCR4 antagonist 5 can inhibit CXCL12-induced cytosolic calcium increase (IC50 = 0.02 nM) and inhibits CXCR4/CXLC12-mediated chemotaxis. CXCR4 antagonist 5 has good physicochemical properties and in vitro safety profiles, inhibiting CYP isozymes and hERG marginally or moderately .
|
-
- HY-150562
-
|
CDK
|
Cancer
|
CDK9-IN-19 is a highly potent and selective CDK9 inhibitor with an IC50 value of 2.0 nM. CDK9-IN-19 has excellent cellular antiproliferative activity, moderate pharmacokinetic property and low hERG inhibition. CDK9-IN-19 significantly induces tumour growth inhibition in an MV4-11 xenograft mice model. CDK9-IN-19 can be used for researching acute myeloid leukaemia (AML) .
|
-
- HY-149432
-
|
HSP
Potassium Channel
|
Cancer
|
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 .
|
-
- HY-155195
-
|
Others
|
Cancer
|
FLT3/CHK-IN-1 (Compound 18) is a dual inhibitor of FLT3/CHK1. FLT3/CHK-IN-1 is more than 1700 times more selective to c-KI T and greatly reduces hERG affinity with an IC50 value of 58.4 μM. FLT3/CHK-IN-1 inhibits tumor growth in mouse xenotransplantation models inoculated with MV-4-11 cells .
|
-
- HY-103309
-
|
Calcium Channel
|
Neurological Disease
|
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 .
|
-
- HY-103309A
-
|
Calcium Channel
|
Neurological Disease
|
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 .
|
-
- HY-148825
-
-
- HY-126257
-
|
Akt
Apoptosis
|
Cancer
|
AKT-IN-3 (compound E22) is a potent, orally active low hERG blocking Akt inhibitor, with 1.4 nM, 1.2 nM and 1.7 nM for Akt1, Akt2 and Akt3, respectively. AKT-IN-3 (compound E22) also exhibits good inhibitory activity against other AGC family kinases, such as PKA, PKC, ROCK1, RSK1, P70S6K, and SGK. AKT-IN-3 (compound E22) induces apoptosis and inhibits metastasis of cancer cells .
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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-157425
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5-HT Receptor
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Neurological Disease
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5-HT2CR agonist 1 (compound 8), a 7-chloro analogue, is a selective 5-HT2CR partial agonist (Emax=71.09%) with an EC50 value of 121.5 nM and no observed activity toward 5-HT2AR or 5-HT2BR. 5-HT2CR agonist 1 exhibits no recruitment activity for β-arrestin and shows low inhibition of hERG at 10 μM .
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- HY-126123
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iGluR
Potassium Channel
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Neurological Disease
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NR2B-selective NMDA receptor antagonist 1 (compound 29) is a potent antagonist of NR1/NR2B receptors, with IC50s of 0.05 μM, 0.73 μM, 2.4 μM to NR1/NR2B NMDA receptor, hERG, α1-AdR, respectivity. NR2B-selective NMDA receptor antagonist 1 exhibites efficient permeability across the blood–brain barrier .
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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-132310
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MAGL
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Neurological Disease
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MAGL-IN-4 is an orally active, selective and reversible monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 6.2 nM. MAGL-IN-4 can penetrate the blood-brain barrier (BBB). MAGL-IN-4 enhances endocannabinoid signaling mostly by the increase in the level of 2-AG via selective MAGL inhibition in the brain .
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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-12736
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Syk
PERK
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Inflammation/Immunology
Cancer
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GSK143 is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.5. GSK143 inhibits phosphorylated Erk (pErk: pIC50=7.1) . GSK143 reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice .
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- HY-12736A
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Syk
PERK
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Inflammation/Immunology
Cancer
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GSK143 dihydrochloride is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.5. GSK143 dihydrochloride inhibits phosphorylated Erk (pErk: pIC50=7.1) . GSK143 dihydrochloride reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice .
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- HY-16697
-
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GPR55
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Cancer
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CID 16020046 is a potent and selective GPR55 antagonist and inhibits GPR55 constitutive activity with an IC50 of 0.15 μM. CID 16020046 inhibits GPR55-mediated Ca 2+ signaling and GPR55-mediated ERK1/2 phosphorylation. CID 16020046 reduces wound healing in endothelial cells and is involved in the regulation of platelet function .
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- HY-163403
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VEGFR
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Cardiovascular Disease
Cancer
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VEGFR-2-IN-43 (compound 16) is an orally active inhibitor of VEGFR2, with an IC50 of 39.91 μM. VEGFR-2-IN-43 can be used for wet age-related macular degeneration (w-AMD) disease research .
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- HY-120355A
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Potassium Channel
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Cardiovascular Disease
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AP14145 hydrochloride is a potent KCa2 (SK) channel negative allosteric modulator with an IC50 of 1.1 μM for KCa2.2 (SK2) and KCa2.3 (SK3) channels. AP14145 hydrochloride inhibition strongly depends on two amino acids, S508 and A533 in the channel. AP14145 hydrochloride prolonged atrial effective refractory period (AERP) in rats and demonstrates antiarrhythmic effects in a Vernakalant-resistant porcine model of atrial fibrillation (AF) .
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Cat. No. |
Product Name |
Type |
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- HY-100545
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Biochemical Assay Reagents
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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-P1440
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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-P5177
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- HY-P1440A
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Potassium Channel
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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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Target |
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* This product has been "discontinued".
Optimized version of product available:
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Cat. No. |
Product Name |
Chemical Structure |
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- HY-17504BS2
-
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Rosuvastatin- 13C,d3 sodium is 13C and deuterated labeled Rosuvastatin sodium (HY-17504B). Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
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- HY-17504AS
-
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Rosuvastatin-d3 is a deuterium labeled Rosuvastatin. Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM[1]. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals[2].
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- HY-17508S1
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Clarithromycin-d3is the deuterium labeledClarithromycin(HY-17508) . Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC50 (Ki) value of 56 (43) μM . Clarithromycin significantly inhibits the HERG potassium current .Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K .
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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-N0221S
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Daurisoline-d2 is the deuterium labeled Daurisoline (HY-N0221). Daurisoline is a bis-benzylisoquinoline alkaloid that can be isolated from Menispermum dauricum and Rhizoma Menispermi. Daurisoline exerts a blocking effect on hERG and has antiarrhythmic effects. Daurisoline is a potent autophagy blocker that can be used for the research of cancer .
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-
- HY-N0221S1
-
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Daurisoline-d5 is the deuterium labeled Daurisoline (HY-N0221). Daurisoline is a bis-benzylisoquinoline alkaloid that can be isolated from Menispermum dauricum and Rhizoma Menispermi. Daurisoline exerts a blocking effect on hERG and has antiarrhythmic effects. Daurisoline is a potent autophagy blocker that can be used for the research of cancer .
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- HY-N0221S2
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Daurisoline-d11 is the deuterium labeled Daurisoline (HY-N0221). Daurisoline is a bis-benzylisoquinoline alkaloid that can be isolated from Menispermum dauricum and Rhizoma Menispermi. Daurisoline exerts a blocking effect on hERG and has antiarrhythmic effects. Daurisoline is a potent autophagy blocker that can be used for the research of cancer .
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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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