Arrhythmias

Amiodarone, a benzofuran-based Class III antiarrhythmic agent, inhibits WT outward ionic current (IhERG) tails with an IC₅₀ of ∼45 nM. Amiodarone induces cell proliferation and myofibroblast differentiation via ERK1/2 and p38 MAPK signaling in fibroblasts. Amiodarone can be used in the research of both supraventricular and ventricular arrhythmias.

ATX-II is a selective sodium channel modulator toxin. ATX-II enhances late sodium current, prevents full sodium channel inactivation, and generates persistent current fractions. ATX-II has pro-arrhythmic effect. ATX-II slows intrinsic heart rate, prolongs QT interval and sinus node recovery time, and causes sinus pauses and arrests. ATX-II can be used for the research of atrial fibrillation, long QT syndrome, and long QT3 syndrome.

ATX-II TFA is a selective sodium channel modulator toxin. ATX-II TFA enhances late sodium current, prevents full sodium channel inactivation, and generates persistent current fractions. ATX-II TFA has pro-arrhythmic effect. ATX-II TFA slows intrinsic heart rate, prolongs QT interval and sinus node recovery time, and causes sinus pauses and arrests. ATX-II TFA can be used for the research of atrial fibrillation, long QT syndrome, and long QT3 syndrome.

TMDJ-035 is a high-affinity, selective RyR2 inhibitor with an EC₅₀ of 0.0130 μM. TMDJ-035 reduces RyR2 protein expression without affecting action potential-induced Ca²⁺ transients. TMDJ-035 decreases ATP content and intracellular Ca²⁺ levels. TMDJ-035 inhibits arrhythmias in a CPVT mouse model carrying mutant RyR2s. TMDJ-035 has no effect on electrocardiogram parameters or cardiac systolic function. TMDJ-035 exacerbates heart failure in mouse myocardial infarction models and hypoxic cardiomyocytes by altering cardiac function, causing tissue damage, promoting inflammatory infiltration, collagen deposition, and changes in Myosin heavy chain/actin expression. TMDJ-035 can be used in studies related to heart failure, catecholaminergic polymorphic ventricular tachycardia, and arrhythmias.

Magnesium sulfate heptahydrate, for cell culture (Epsom salts, for cell culture) is a hydrate of magnesium sulfate (HY-Y1267) suitable for cell culture applications. Magnesium sulfate is a calcium antagonist and a potent L-type calcium channel inhibitor, as well as a tocolytic. Magnesium sulfate has anti-inflammatory, anticonvulsant, vasodilatory, and neuroprotective effects. Magnesium sulfate can be used in the research of diseases such as preeclampsia/eclampsia.

Cassaine (Nervocidine) is a Na⁺/K⁺-ATPase inhibitor. Cassaine stabilizes phosphorylated intermediates, slows spontaneous dephosphorylation and blocks potassium-stimulated dephosphorylation. Cassaine exhibits non-competitive inhibition with respect to K⁺, shows inhibition enhanced by Pi and antagonized by Na⁺. Cassaine induces positive inotropic effects in perfused hearts with faster inotropy offset. Cassaine can be used for research on cardiac arrhythmias.

Etafenone is an antiarrhythmic agent and vasodilator. Etafenone exerts β-adrenergic agonistic effects. Etafenone inhibits the automaticity of sinoatrial nodes, atrioventricular junctions and Purkinje fibers, prolongs action potential duration and refractory period, slows the rising rate of action potentials, and prolongs conduction time. Etafenone enhances collateral circulation after coronary occlusion and suppresses ventricular premature beats. Etafenone delays ischemic myocardial energy imbalance, improves the recovery of high-energy phosphates after ischemia, and reduces myocardial oxygen consumption. Etafenone can be used in research related to ischemic heart disease, arrhythmia and angina pectoris.

Bucumolol is an orally active β-adrenergic receptor blocker. Bucumolol inhibits Renin release. Bucumolol exhibits activities including local anesthesia, antiarrhythmia, antihypertension, heart rate reduction, negative inotropy, cardiac action potential inhibition, and action potential duration shortening. Bucumolol does not increase cardiac electrical threshold, prolong atrial refractory period, or affect body weight in rodents. Bucumolol can be used in research related to arrhythmia and hypertension.

(-)-N6-phenylisopropyl adenosine (L-Phenylisopropyladenosine) is a selective A1 adenosine receptor agonist. (-)-N6-phenylisopropyl adenosine inhibits K⁺-induced Ca²⁺ uptake with an IC₅₀ value of 0.5 µM. (-)-N6-phenylisopropyl adenosine protects against ischemia-induced ventricular arrhythmias and atrial fibrillation, and exacerbates ethanol withdrawal symptoms. (-)-N6-phenylisopropyl adenosine also has analgesic effects.

UCL 2077 is a potassium channel and slow afterhyperpolarization (sAHP) inhibitor. UCL 2077 selectively blocks sAHP channels without affecting L-type Ca²⁺ currents. UCL 2077 blocks KCNQ1- and KCNQ2-containing K⁺ channels, decreases erg current amplitude, increases erg deactivation rate. UCL 2077 can be used for the research of hippocampus-dependent memory retrieval deficit and cardiac arrhythmias.

(E)-KN-93 phosphate is a Ca²⁺/calmodulin-dependent protein kinase II (CaMKII) inhibitor with IC₅₀ values of 9 μM and 3 μM against CaMKIIδ_Monomer and CaMKIIδ_Dodecamer, respectively. (E)-KN-93 phosphate can be used in research on epilepsy, depression, and arrhythmias..

Sophoramine ((-)-Sophoramine) is a prejunctional α₂-adrenoceptor inhibitor that can be found in the seeds of Sophora alopecuroides. Sophoramine inhibits prejunctional α2-adrenoceptors to facilitate norepinephrine release from adrenergic nerves. Sophoramine shows cytotoxic activity against human cancer cells, positive inotropic activity, and activity in rodent arrhythmia models. Sophoramine can be used for the research of arrhythmias.

(17R,18S)-Epoxyeicosatetraenoic acid (17 (R),18 (S)-EETeTr) is a physiologically active fatty acid metabolite and also a vasodilator targeting BKα. (17R,18S)-Epoxyeicosatetraenoic acid activates the outward potassium current mediated by BK channels, and this effect is independent of the BKβ1 subunit, intracellular/extracellular calcium levels, and sarcoplasmic reticulum calcium release regulated by RyR3. (17R,18S)-Epoxyeicosatetraenoic acid is produced by the epoxidation of eicosapentaenoic acid mediated by CYP1A1 variants. (17R,18S)-Epoxyeicosatetraenoic acid is applicable to research related to arrhythmia.

AVE-0118 is a Kv1.5 potassium channel blocker and antiarrhythmic agent. AVE-0118 blocks neuronal Kv1.5 potassium channels, thereby enhancing the release of norepinephrine. AVE-0118 enhances field stimulation-induced neurogenic contraction, an effect sensitive to α1-adrenergic receptor blockade. AVE-0118 terminates persistent atrial fibrillation in some dogs. AVE-0118 is applicable to research related to atrial fibrillation and persistent atrial fibrillation.

Chiisanogenin is an orally active triterpenoid. Chiisanogenin reduces postprandial blood glucose by promoting GLUT4 translocation and glucose uptake via activation of the IRS-1/PI3K/Akt signaling pathway. Chiisanogenin binds to MLKL and inhibits its phosphorylation and oligomerization, maintains lysosomal integrity, restores autophagic flux, and suppresses NLRP3 inflammasome activation and pyroptosis. Chiisanogenin inhibits xanthine oxidase activity and regulates oxidative stress and ion pump activity. Chiisanogenin binds to or inhibits PKA, H⁺/K⁺-ATPase and β-glucuronidase. Chiisanogenin possesses multiple pharmacological activities, including broad-spectrum antibacterial activity, anticancer, anti-inflammatory, antirheumatic, renoprotective, cardioprotective and antiarrhythmic effects. Chiisanogenin can be used in research related to type 2 diabetes, rheumatoid arthritis, myocardial injury, hepatocellular carcinoma and ventricular arrhythmia^.

ERG-IN-7 is a Nav1.5, Cav1.2 and Kv11.1 inhibitor with IC₅₀ values of 10.34 μM, 21.01 μM, and 16.385 μM for human Nav1.5, Cav1.2, and Kv11.1, respectively. ERG-IN-7 prolongs action potentials, reduces conduction velocity, and restores cardiac function. ERG-IN-7 can be used for the research of ventricular arrhythmia.

Zinc13732787 is an inhibitor of the KCNQ1/KCNE1 potassium channel complex, with no activity against the KCNQ2/KCNQ3 channel. Zinc13732787 reduces axonal growth in human neural stem cells, while exerting no effect on KCNQ1-knockout neural stem cells. Zinc13732787 can be used for research on arrhythmia, epilepsy, and neuropsychiatric disorders.

NE-10133 is a I_SK and I_KS potassium channel (Potassium Channel) inhibitor. NE-10133 inhibits voltage-dependent and slowly activated delayed rectifier potassium currents. NE-10133 exhibits class III antiarrhythmic activity. NE-10133 is applicable for research related to arrhythmias.

azo-Q2a is a photoswitchable Na_V1.5 inhibitor. azo-Q2a exists as the trans isomer with low activity in the dark or under 480 nm illumination, and exists as the cis isomer with higher inhibitory potency under 365 nm illumination. azo-Q2a reduces the heart rate of living zebrafish larvae in a light-dependent manner. azo-Q2a can be used for the study of arrhythmias.

Asocainol hydrochloride (Goe 4704 hydrochloride) is an antiarrhythmic agent. Asocainol hydrochloride reduces the maximum rate of action potential rise and action potential amplitude. Asocainol hydrochloride is applicable for the research of arrhythmias.