10 Results for "

Cardiac safety

" in MedChemExpress (MCE) Product Catalog:
Products (10)

10 Results for "Cardiac safety" in MCE Product Catalog:

Cat. No.: HY-159821
CAS No.: 2830607-59-3
Synonyms: CK-4021586; CK-586
Target:  

Myosin

Research Areas:  

Cardiovascular Disease

Ulacamten (CK-4021586; CK-586) is an orally active cardiac myosin inhibitor and an inhibitor of the double-headed cardiac heavy meromyosin (HMM)ATPase (excluding single-headed myosin subfragment-1), with an EC50 of 2.9 μM. Ulacamten regulates cardiac myosin, reduces excessive myocardial contractility, and alleviates left ventricular outflow tract obstruction. Ulacamten increases the left ventricular short-axis systolic internal diameter, inhibits dobutamine-induced exacerbation of obstruction, and exerts only a mild reducing effect on left ventricular systolic function. Ulacamten also inhibits the fractional shortening of the short axis without altering calcium transients. Ulacamten shows good safety and tolerability in purpose-bred cats with naturally occurring obstructive hypertrophic cardiomyopathy .
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Cat. No.: HY-175188
CAS No.: 2404652-82-8
Synonyms: BPN-0027490
Target:  

Myosin

Research Areas:  

Neurological Disease

MT-110 (BPN-0027490) is a non-muscle myosin NMIIB-selective inhibitor with high brain penetration and favorable safety profile. MT-110 specifically disrupts NMIIB-dependent actin dynamics in dendritic spines, while it exerts no significant adverse effects on cardiac myosin II and cardiac functions (such as cardiac output and heart rate) at tested concentrations. A single administration of MT-110 produces long-lasting (sustained for several weeks) blockade of methamphetamine motivation associated with environmental cues. MT-110 exhibits extremely high specificity, with no interference with cocaine motivation, hippocampus-dependent memory, fear memory, or locomotor and anxiety-like behaviors. MT-110 serves as a valuable tool compound for investigating the mechanisms of methamphetamine use disorder .
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Cat. No.: HY-145285
CAS No.: 2135514-20-2
Target:  

Apelin Receptor (APJ)

Research Areas:  

Cardiovascular Disease

APJ receptor agonist 5 (compound 3) is a potent and orally active agonist of apelin receptor (APJ) with an EC50 of 0.4 nM. APJ receptor agonist 5 displays excellent pharmacokinetic profiles in the rodent heart failure (HF) model. APJ receptor agonist 5 also shows an acceptable safety profile in preclinical toxicology studies. APJ receptor agonist 5 leads to improved cardiac function and can be used for researching the HF disease .
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Cat. No.: HY-19004
CAS No.: 94899-83-9
Target:  

Sodium Channel

Research Areas:  

Cardiovascular Disease

711389-S hydrochloride is an antiarrhythmic compound that demonstrates its antiarrhythmic activity by increasing the ventricular fibrillation threshold (VFT). 711389-S hydrochloride also has strong anti-fibrillation effects and safety, and can be used in the study of ventricular fibrillation and sudden cardiac death. 711389-S hydrochloride also inhibits the sodium current .
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Cat. No.: HY-145284
CAS No.: 2762567-70-2
Target:  

Apelin Receptor (APJ)

Research Areas:  

Cardiovascular Disease

APJ receptor agonist 4 is a potent and orally active agonist of apelin receptor (APJ) with EC50 and Ki of 0.06 nM and 0.07 nM respectively. APJ receptor agonist 4 displays excellent pharmacokinetic profiles in the rodent heart failure (HF) model. APJ receptor agonist 4 also shows an acceptable safety profile in preclinical toxicology studies. APJ receptor agonist 4 leads to improved cardiac function and can be used for researching the HF disease .
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Cat. No.: HY-163403
Target:  

VEGFR

Research Areas:  

Cardiovascular Disease Cancer

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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Cat. No.: HY-P992108
CAS No.: 3061442-66-5
Synonyms: RELAX10

Research Areas:  

Cardiovascular Disease

Efadirelaxin alfa (RELAX10) is a highly selective agonist of relaxin/insulin-like family peptide receptor RXFP1. After subcutaneous administration in animal experiments, Efadirelaxin alfa exhibits a significantly prolonged terminal half-life (7 days in mice, 3.75 days in rats), and shows no activity against related receptors such as RXFP2 and RXFP3. Efadirelaxin alfa has significant anti-cardiac hypertrophy and anti-fibrotic effects. Efadirelaxin alfa effectively attenuates and reverses cardiac hypertrophy and collagen deposition by regulating the TGF-β1/Smad2 and AKT/eNOS signaling pathways. Efadirelaxin alfa improves cardiac systolic function without causing fluctuations in blood pressure or heart rate, demonstrating favorable safety. Efadirelaxin alfa is currently mainly used in studies related to heart failure .
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Cat. No.: HY-182011
CAS No.: 3029155-57-2
Target:  

GPR6

Research Areas:  

Neurological Disease

GPR6 inverse agonist 2 (Compound 575) is a selective GPR6 inverse agonist, with IC50 values of < 0.1 μM and 1~30 μM against GPR6 and GPR3, respectively. GPR6 inverse agonist 2 exhibits preliminary cardiac safety, with an IC50 of 21.71 μM for hERG. GPR6 inverse agonist 2 can be used in the research of movement disorders such as Parkinson's disease .
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Cat. No.: HY-184478
CAS No.: 3103822-75-6
Target:  

GABA Receptor

Research Areas:  

Neurological Disease

GABAA receptor modulator-14 is an orally active, blood-brain barrier permeable selective positive allosteric modulator (PAM) of extrasynaptic δ-containing GABAA receptors (α4β3δ subtype) with an EC50 of 0.8 μM. GABAA receptor modulator-14 selectively enhances tonic neuronal inhibition by potentiating GABA-evoked currents mediated by extrasynaptic δ-GABAARs, produces rapid sustained antidepressant effects, elevates slow-wave NREM sleep and shows no addiction liability in mice. GABAA receptor modulator-14 can be applied to major depressive disorder (MDD) and comorbid insomnia research .
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Cat. No.: HY-L118
197 compounds

Sodium channels conduct sodium ions (Na+) through a cell's plasma membrane that are the source of excitatory currents for the nervous system and muscle. Na channels are classified according to the trigger that opens the channel for such ions, i.e. either a voltage-change (Voltage-gated, voltage-sensitive, or voltage-dependent sodium channel also called VGSCs or Nav channel) or a binding of a substance (a ligand) to the channel (ligand-gated sodium channels). Dysfunction in voltage-gated sodium channels correlates with neurological and cardiac diseases, including epilepsy, myopathies, pain and cardiac arrhythmias. Sodium channel blockers are used in the treatment of cardiac arrhythmia, pain and convulsion.

MCE offers a unique collection of 197 sodium channel blocker and antagonists, all of which have the identified inhibitory effect on sodium channels. MCE Sodium Channel Blocker Library can be used for neurological and cardiac diseases drug discovery and sodium channel research.