cardiac function

Enrasentan (sb-217242) is a mixed antagonist of ET(A) and ET(B) receptors that reduces blood pressure, prevents cardiac hypertrophy, and protects myocardial function.

CBS-1114 HCl (N-Phenylbenzamidrazone hydrochloride) is a 5-lipoxygenase inhibitor and an anti-inflammatory compound in a good eye-permeable model.CBS-1114 HCl maintains and improves cardiac function, attenuates cardiac dysfunction, as well as reduces epicardial adipose tissue and/or pericardial adipose tissue in subjects with cardiovascular disease.

AM-8123 is an orally available nonpeptide APJ agonist.AM-8123 reduces collagen load and improves cardiac function. AM-8123 ameliorates myocardial infarction in rats and can be used to study cardiovascular diseases such as heart failure.

Cyclic AMP (cAMP) (Adenosine 3',5'-cyclophosphate) combined with vitamin C treatment of children with viral myocarditis has exact curative effect, and it can improve cardiac function of patients and improve immune function.

RFRP-1 (human) acetate is a potent endogenous NPFF receptor agonist (EC50 values are 0.0011 and 29 nM for NPFF2 and NPFF1, respectively). Attenuates contractile function of isolated rat and rabbit cardiac myocytes. Reduces heart rate, stroke volume, eject

Catestatin acetate is a non-competitive antagonist of nAChR and inhibits catecholamine release. Catestatin acetate regulates cardiac function and blood pressure.

NKH477 is a novel water-soluble forskolin derivative that improves cardiac failure mainly through its beneficial effects on diastolic cardiac function. NKH477 shows an antiproliferative effect in vivo with an altered cytokine profile to inhibit the acute

Dapansutrile is a potent, selective and orally active NLRP3 inflammasome inhibitor, with Anti-inflammatory and analgesic activity.

Danicamtiv (MYK-491) is an inotropic agent and it also is a selective allosteric activator of cardiac myosin. Danicamtiv increases cardiac systolic function and preserves mechanical efficiency.

Mitochondrial fusion promoter M1, a modulator of mitochondrial dynamics, enhances mitochondrial function and cellular respiration, and has shown efficacy in reducing brain and cardiac damage in rats suffering from cardiac ischemia/reperfusion injury.

3-Iodothyronamine is derived from the deiodination and decarboxylation of endogenous thyroxine. It activates the G protein-coupled receptor known as trace amine-associated receptor 1 at nanomolar concentrations whereupon it rapidly influences thyroid hormone actions including body temperature, heart rate, and cardiac output. It has also been reported to function in controlling lipid and glucose utilization, hormonal secretion, and neuronal function, and has been considered for use in chemically-induced hibernation for medical purposes.

Acts as a cardiac hormone with a variety of biological actions including natriuresis, diuresis, vasorelaxation, and inhibition of renin and aldosterone secretion. It is thought to play a key role in cardiovascular homeostasis. Helps restore the body\'s sa

KR-32568 is a sodium hydrogen exchanger 1 (NHE-1) inhibitor (IC50: 230 nM) with potent cardioprotective effects. At a concentration of 10 μM, it restored cardiac systolic function in an isolated ischemic rat heart model. Additionally, KR-32568 (0.3 mg kg) reduced myocardial infarction size in a rat model of ischemia and reperfusion injury.

SAR296968 is a novel selective NCX inhibitor, improving cardiac function and restoring sympathovagal balance in heart failure.

2-APQC acts as a SIRT3 agonist with a dissociation constant (Kd) of 2.756 μM. It enhances cardiac function in both in vivo and in vitro settings, thereby mitigating heart failure.

F 15845 is a blocker of the persistent sodium current prevents consequences of hypoxia in rat femoral artery. F15845 has been shown to selectively inhibit the persistent sodium current of Nav1.5[1] exerting cardioprotective effects following ischemia. In vitro testing showed minimal effects of F15845 on other important ion channels of the heart, including major Ca2+ and K+ channels.[1] This characteristic is thought to account for the limited effect of F15845 to change other heart parameters such as basal cardiac function, hemodynamic functions and ventricular fibrillation. F15845 was also shown to exert improved effects when the membrane potential was depolarized,[1] by acting on the extracellular side of the channel.

[Sar1,Thr8]-Angiotensin II is a potent antagonist of angiotensin II. It does not alter cardiac function and may be safe for patients with heart conditions.

CXL-1020, a nitroxyl (HNO) prodrug, enhances cardiac inotropy/lusitropy and Ca 2+ cycling in rats exhibiting abnormal relaxation, induces vasorelaxation, and augments cardiac function in canine models. It has been investigated for its potential in treating systolic and stable heart failure [1].

BAY2413555 is a muscarinic acetylcholine M2 receptor modulator that can be used in cardioprotection and improvement of cardiac function research.

CU06-1004 (Sac-1004) is an orally active compound that mitigates endothelial dysfunction by inhibiting hyperpermeability and inflammation. It reduces vascular leakage and inflammation in multiple animal models, including diabetic retinopathy, stroke, cancer, and inflammatory bowel disease. CU06-1004 also improves conditions in a CDAA-induced mouse model of NASH and enhances cardiac function [1] [2] [3].

KR-39038 is an orally active GRK5 (G protein-coupled receptor kinase 5) inhibitor (IC50: 0.02 μM) that inhibits the HDAC5 pathway in neonatal cardiomyocytes and significantly reduces angiotensin II-induced hypertrophy, leading to notable anti-myocardial hypertrophy effects and improved cardiac function. KR-39038 is applicable for heart failure research.

APJ receptor agonist 5 (compound 3) is a potent and orally active apelin receptor (APJ) agonist (EC 50: 0.4 nM) with excellent pharmacokinetic profiles in rodent heart failure (HF) models and an acceptable safety profile in preclinical toxicology studies, improving cardiac function and useful for HF disease research.

RFRP-1(human) TFA, an endogenous NPFF receptor agonist, exhibits potent activity with EC50 values of 0.0011 nM for NPFF2 and 29 nM for NPFF1. It significantly diminishes the contractile function of isolated rat and rabbit cardiac myocytes. Moreover, it decreases heart rate, stroke volume, ejection fraction, and cardiac output, while elevating plasma prolactin levels in rats.

Catestatin TFA, a 21-amino acid residue peptide, exhibits both cationic and hydrophobic properties. This endogenous peptide plays a crucial role in regulating cardiac function and blood pressure. It functions as a non-competitive nicotinic antagonist by interacting with nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release.

Cardioexcitatory peptide 1, a potent neuropeptide derived from Achatina atria, exerts significant excitatory effects on cardiac function, additionally influencing the motility of muscular tissues and neural activities [1].

Neuronostatin-13 human acetate is a 13-amino acid peptide hormone, which plays an important role in the regulation of hormonal and cardiac function.

Ginkgolide C (BN-52022), a natural product, can enhance the cardiac function of rats in the body.

MCaE12A, a potent modulator of RyR2, enhances the channel's sensitivity to cytoplasmic calcium concentrations, facilitating its opening. This compound serves as a critical instrument for examining RyR2 structure-to-function relationships and for modulating Ca2+ homeostasis and dynamics in cardiac cells [1].

Epothilone F is a derivative or analogue of Epothilone D. Epothilone F is also an active metabolite of Epothilone D. In molecule of Epothilone F, a hydroxymethyl group is on the thiazole ring. Like taxanes, Epothilone F prevents cancer cells from dividing

Wnt signaling is required for direct multiple biological processes and also plays key roles in the pathogenesis of various diseases. Cyclic AMP response element-binding protein (CREB) is a transcription factor that is a member of the leucine zipper family of DNA binding proteins. This protein binds as a homodimer to the cAMP-responsive element, an octameric palindrome. The protein is phosphorylated by several protein kinases, and induces transcription of genes in response to hormonal stimulation of the cAMP pathway. Via generating a transcriptionally active complex with β-catenin, CREB acts as a mediator of Wnt signaling.ICG-001 is an inhibitor of β-catenin/CREB mediated transcription. The direct cellular target of ICG-001 is CREB. the inhibitory IC50of ICG-001 against β-catenin/CREB mediated transcription was 3 μM. ICG-001 treatment at the concentration of 25 μM for 24h significantly increased caspase activity in both colon cancer cell lines SW480 and HCT116 cell lines but not in normal colonic epithelial cells CCD-841Co. In a cell growth inhibition assay, the IC50s of ICG-001 against SW480 and HCT116 cells were 4.43 μM and 5.95 μM, respectively.In a SW620 nude mouse xenograft model, an water-soluble analog of ICG-001 given at the dose of 150 mg/kg i.v. once in every 2 days dramatically suppressed tumor growth. In a bleomycin-induced pulmonary fibrosis mice model, ICG-001 given at the dose of 5 mg/kg per day reversed pulmonary fibrosis. In a rat myocardial infarction model, ICG-001 was administrated subcutaneously at the dose of 50 mg/kg/day for 10 days which significantly improved cardiac contractile function after myocardial infarction in the rats.

APJ Receptor Agonist 4 is a potent, orally active apelin receptor (APJ) agonist, demonstrating an EC50 of 0.06 nM and a Ki of 0.07 nM. It exhibits excellent pharmacokinetic profiles in rodent heart failure (HF) models and has shown an acceptable safety profile in preclinical toxicology studies. This compound effectively improves cardiac function, making it valuable for research into HF disease.

Apelin biased agonist; exhibits bias for the G protein pathway. Stimulates endothelial NOS phosphorylation and expression, promotes proliferation, and attenuates apoptosis of human pulmonary arterial endothelial cells in vitro. Shows positive inotropic an

Potent endogenous NPFF receptor agonist (EC50 values are 0.0011 and 29 nM for NPFF2 and NPFF1, respectively). Attenuates contractile function of isolated rat and rabbit cardiac myocytes. Reduces heart rate, stroke volume, ejection fraction and cardiac out

Compound 39 (NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal)) is a potent agonist of the APJ receptor, possessing a K i value of 0.6 nM. It is capable of activating Gαi1, with an EC 50 of 0.8 nM, and of recruiting β-arrestin2, with an EC 50 of 31 nM. Furthermore, this compound demonstrates extended effects on cardiac function [1].

KB-R7785 is a novel ADAM12 and MMP inhibitor, ameliorating cardiac function in a transverse aortic constriction (TAC) model by inhibiting the proteolytic activation of HB-EGF signaling, exerting its antidiabetic effect by ameliorating insulin sensitivity through the inhibition of TNF-alpha production.

ML 7 is an inhibitor of myosin light chain kinase that protects cardiac function from ischemia/reperfusion (I/R) injury.

Elabela(19-32) TFA, an effective fragment of ELABELA (ELA), selectively engages with the apelin receptor (APJ). This compound initiates G αi1 and β-arrestin-2 signaling, demonstrating EC50 values of 8.6 nM and 166 nM, respectively. It facilitates receptor internalization, lowers arterial pressure, and has a positive inotropic impact on cardiac function [1].

Forsythoside B binds to LPS and reduces the biological activity of serum LPS, and inhibits NF-κB activation. Forsythoside B inhibits the inflammatory response and has antioxidant properties. Potent neuroprotective effects with a favorable therapeutic time