cardiomyocytes

NS3623 is an activator of human ether-a-go-go-related gene (hERG) potassium channels with a dual mode of action, also acting as an inhibitor of hERG1 channels. It activates the IKr and Ito currents and exhibits an antiarrhythmic effect.

DCPIB, a known specific and potent inhibitor of volume-regulated anion channels (VRAC),DCPIB displayed superior selectivity toward TRESK with an IC50 of 0.14 μM, demonstrating at least 100-fold higher affinity over TREK1/TRAAK channels.

Squalane is a lipid found in some fish oils (especially shark liver oil) and some vegetable oils. It has anticancer and antioxidant properties and is used as a skin moisturizer and emollient.

SB 202190 (FHPI) is a p38 MAPK inhibitor that inhibits p38α and p38β2 (IC50=50/100 nM) selectively and cell-permeably. SB 202190 has antitumor activity and also induces the differentiation of human embryonic stem cells into cardiomyocytes.

R 56865 is a weak potential-operated channel inhibitor that inhibits the late sodium current in human isolated cardiomyocytes.

Gue1654 is a selective OXE-R inhibitor that attenuates coronary artery ligation-induced ischemic myocardial injury and cardiomyocyte oxygen/glucose deprivation-induced injury in mice through activation of BCAT1.Gue1654 inhibits OXE-R-inhibited protein kinase C-ε (PKC-ε)/nuclear factor κB (NF-κB) signaling and apoptosis in cardiomyocytes. Gue1654 can be used to study cardiovascular disease.

AZD-1305 is a novel anti-arrhythmic compound that primarily blocks the fast component of IKr, l-type calcium currents and intra-ward sodium currents in mammalian cells and ventricular cardiomyocytes and can be used in studies to reverse arrhythmias.

GSK 2833503A is a potent and selective TRPC6 and TRPC3 antagonist (IC50 = 3-16 nM and 21-100 nM, respectively). GSK 2833503A exhibits >63-fold selectivity over other ion channels, including other TRP channels, CaV1.2, hERG and NaV1.5. GSK 2833503A suppresses angiotensin II or endothelin-1-induced cardiac hypertrophy signaling in HEK293 cellsin vitroand in cardiomyocytes.

NLRP3-IN-2 (5-Chloro-N-(p-sulfamoylphenethyl)-o-anisamide), an intermediate capable of synthesizing glibenclamide, exerts an inhibitory effect on the formation of NLRP3 inflammatory vesicles in cardiomyocytes, limiting infarct size after myocardial ischemia/reperfusion in mice and has no effect on metabolism.

Temocapril is an inhibitor of tyrosine kinase.

P-1075 opens mitochondrial K(ATP) channels and generates reactive oxygen species causing cardioprotection of rabbit hearts. P-1075 is an effective activator of sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-KIR6) (EC50: 45 nM fo

VUT-MK142 is a new cardiomyogenic small molecule promoting the differentiation of pre-cardiac mesoderm into cardiomyocytes,which may be useful to differentiate stem cells into cardiomyocytes for cardiac repair.

Bisandrographolide C is identified from Andrographis paniculata. Bisandrographolide C activates TRPV1 and TRPV3 channels (Kds: 289 and 341 μM) and protects cardiomyocytes from hypoxia-reoxygenation injury.

(+)-ITD-1 is an inhibitor of TGF-β, effectively inhibiting TGF-β2 with an IC50 of 0.46 μM. It promotes the degradation of the TGF-β type II receptor (TGFBR2) and the differentiation of cardiomyocytes. Additionally, it suppresses the formation of the mesoderm during the early differentiation of mouse embryonic stem cells (mESCs).

KY02111 facilitates differentiation of hPSCs to cardiomyocytes by inhibiting Wnt signaling, maybe affect downstream of GSK3β and APC.

Nrf2 HO-1 Activator 3 (Compound C3a) is an activator of the Nrf2 signaling pathway that facilitates the translocation of Nrf2 into the nucleus and enhances the expression of heme oxygenase-1 (HO-1). In H9c2 cardiomyocytes subjected to H2O2 or high glucose stimulation, Nrf2 HO-1 Activator 3 inhibits the excessive expression of ROS and MDA, suppressing cell viability and colony formation, thereby exhibiting antioxidant activity.

Magnesium Lithospermate B is a natural product activates eNOS and ameliorates endothelial dysfunction in diabetes by enhancing vasodilation in addition to reducing oxidative stress, it can protecte cardiomyocytes from ischemic injury through specific inhibition of TAB1-p38 apoptosis signaling.improves renal failure.

Cardiogenol C is a cardiomyogenesis inducer in embryonic stem cells.

MMPSI (Caspase-3/7 Inhibitor I) is a novel, non-peptide small molecule caspase 3 and caspase 7 inhibitor that reduces ischemic injury in isolated rabbit heart or cardiomyocytes and inhibits apoptosis of H16c2 cells in a concentration-dependent manner.MMPSI can be used to study cardioprotection and myocardial injury.

CP-312 (Cardioprotectant 312) is an antioxidant defense response activator that protects hiPSC-CM viability by acting through induction of heme oxygenase-1 and targeting the antioxidant response network by inducing HMOX1 expression.CP-312 protects human iPSC-derived cardiomyocytes from oxidative stress.

ADR-925, an active chelated iron metabolite of dexrazoxane, has the ability to protect neonatal rat cardiomyocytes from doxorubicin-induced injury.

Cipepofol (HSK3486) is a GABAA receptor agonist with sedative properties and protective effects in a variety of cardiovascular diseases.Cipepofol activates the Sirtuin1 (Sirt1)/Nrf2 pathway and induces apoptosis in cardiomyocytes, and can be used to study myocardial infarction, myocardial ischemia/reperfusion injury, and octopus pot syndrome.

SB 202190 hydrochloride is the salt form of SB 202190.SB 202190 (FHPI) is a p38 MAPK inhibitor that inhibits p38α and p38β2 with selective, cell-permeable, and antitumor activity, and also induces differentiation of human embryonic stem cells to cardiomyocytes.

N-Desbutyl dronedarone is an active metabolite of the antiarrhythmic agent dronedarone .1,2,3It is formed from dronedarone by cytochrome P450s (CYPs) and monoamine oxidase (MAO) in human hepatocyte preparations.4N-Desbutyl dronedarone inhibits the binding of 3,3',5-triiodo-L-thyronine to the thyroid hormone receptors TRα1and TRβ1(IC50s = 59 and 280 μM for the chicken and human receptors, respectively).1It inhibits CYP2J2-mediated formation of 14,15-EET from arachidonic acid and soluble epoxide hydrolase-mediated formation of 14,15-DHET from 14,15-EET (IC50s = 1.59 and 2.73 μM, respectively, in cell-free assays).2N-Desbutyl dronedarone decreases intracellular ATP levels in H9c2 rat cardiomyocytes (IC50= 1.07 μM) and inhibits mitochondrial complex I, also known as NADH dehydrogenase, and mitochondrial complex II, also known as succinate dehydrogenase, activities in isolated rat heart mitochondria (IC50s = 11.94 and 24.54 μM, respectively).3 1.Van Beeren, H.C., Jong, W.M.C., Kaptein, E., et al.Dronerarone acts as a selective inhibitor of 3,5,3'-triiodothyronine binding to thyroid hormone receptor-α1: in vitro and in vivo evidenceEndocrinology144(2)552-558(2003) 2.Karkhanis, A., Tram, N.D.T., and Chan, E.C.Y.Effects of dronedarone, amiodarone and their active metabolites on sequential metabolism of arachidonic acid to epoxyeicosatrienoic and dihydroxyeicosatrienoic acidsBiochem. Pharmacol.146188-198(2017) 3.Karkhanis, A., Leow, J.W.H., Hagen, T., et al.Dronedarone-induced cardiac mitochondrial dysfunction and its mitigation by epoxyeicosatrienoic acidsToxicol. Sci.163(1)79-91(2018) 4.Klieber, S., Arabeyre-Fabre, C., Moliner, P., et al.Identification of metabolic pathways and enzyme systems involved in the in vitro human hepatic metabolism of dronedarone, a potent new oral antiarrhythmic drugPharmacol. Res. Perspec.2(3)e00044(2014)