NKH477 is a novel water-soluble forskolin derivative that improves cardiac failure mainly through its beneficial effects on diastolic cardiacfunction. NKH477 shows an antiproliferative effect in vivo with an altered cytokine profile to inhibit the acute
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
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 cardiacfunction, 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.
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.
KB-R7785 is a novel ADAM12 and MMP inhibitor, ameliorating cardiacfunction 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.
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 cardiacfunction, making it valuable for research into HF disease.
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
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