cardiac function

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

Angiotensin II is a major biologically active vasoconstrictor peptide that regulates blood pressure by binding to AT1R and AT2R receptors. It stimulates the sympathetic nervous system, promotes aldosterone synthesis, and enhances renal function. Additionally, it induces vascular smooth muscle cell proliferation and increases collagen synthesis, leading to vascular and myocardial hypertrophy and fibrosis. It also promotes apoptosis and endothelial capillary formation. Angiotensin II is commonly used to induce hypertension and cardiac hypertrophy animal models.

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.

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.

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.

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.

CBM-301940 (compound 5) is a potent and orally active MCD (Malonyl-CoA Decarboxylase) inhibitor with IC50=23 nM that improves cardiac efficiency and function with cardioprotective properties in a rat cardiac ischemia/reperfusion model.

CLT-28643 is a potent and specific α5β1-Integrin inhibitor that prevents fibrosis in glaucoma filtration surgery (GFS), inhibits tumor growth and angiogenesis, suppresses fibrosis and inflammation in a bleomycin-induced lung fibrosis model, and improves insulin sensitivity and cardiac function in H9C2 cells from obese mice.

AZD0233 is an orally active CX3CR1 antagonist that immunomodulates the CX3CR1/CX3CL1 signaling axis. It improves cardiac function in dilated cardiomyopathy mouse models while reducing macrophage infiltration and fibrotic scarring.

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.

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

Butin, the major bioactive flavonoid isolated from Dalbergia odorifera heartwood, possesses oral activity with notable antioxidant, antiplatelet, and anti-inflammatory effects. This compound effectively alleviates myocardial infarction, improves cardiac function, and prevents diabetes-induced cardiac oxidative damage in rats.

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.

Pyrocatechol sulfate, a phenolic metabolite found in human plasma, is associated with the intake of specific foods such as berries and the state of the gut microbiome. It serves as a potential urinary biomarker for kidney function, dialysis clearance rates, whole grain consumption, and regular coffee intake. Additionally, in conjunction with other phenolic sulfates, pyrocatechol sulfate plays a role in regulating various biological functions, including those related to brain health and the rhythmic beating of cardiac cells.

Ulacamten, also known as CK-4021586 or CK-586, is an orally bioavailable and highly selective cardiac myosin inhibitor that enhances the transition of myosin into a force-generating state without altering calcium handling, demonstrating sub-micromolar biochemical potency and improving left ventricular systolic function in preclinical models while maintaining myocardial energetic efficiency and minimizing off-target activity against skeletal and smooth muscle myosin.

Enrasentan (also known as SB-217242) is a dual receptor endothelin antagonist with a higher affinity for the ET(A) receptor. In animal models of hypertension and cardiac hypertrophy, this compound reduces blood pressure, prevents cardiac hypertrophy, and preserves myocardial function. Enrasentan enhances survival rates, limits left ventricular remodeling, and maintains myocardial performance in hypertensive cardiac hypertrophy and dysfunction.

TR-100 is a small-molecule inhibitor that targets tumor-associated tropomyosin; it specifically binds to the C-terminus of tropomyosin 3.1, thereby disrupting its interaction with actin filaments and compromising cytoskeletal stability. TR-100 selectively affects Tpm3.1-dependent actin filament function in cancer cells while having minimal impact on normal tissues (such as cardiac muscle). It is primarily used to study mechanisms related to tumor cell proliferation, migration, and survival. Additionally, TR-100 inhibits Dynamin-1 with an IC50 value of 10.8 µM.

ALDH2activator 1 (Compound Z17) is an allosteric activator of aldehyde dehydrogenase 2 (ALDH2). This compound improves cardiac function and reduces myocardial necrosis in a mouse model of ischemia-reperfusion. ALDH2activator 1 holds potential for research in cardiovascular diseases, such as myocardial infarction (MI).

SKLB-11A is a potent allosteric agonist of SIRT3 (sirtuin 3). It activates signaling pathways associated with autophagy (autophagy), helps prevent mitochondrial dysfunction, and improves cardiac function in models of Doxorubicin-induced cardiotoxicity as well as myocardial ischemia/reperfusion.

SGLT2-IN-2 (Compound E9) is an inhibitor of SGLT2 and significantly enhances the inhibition of SGLT2, NHE1, and SOD enzyme activities. It provides protection against myocardial cell damage induced by glucose-free DMEM. Additionally, SGLT2-IN-2 markedly improves cardiac function in TAC-induced heart failure (HF) mice, suppressing myocardial cell hypertrophy and collagen deposition. It reduces myocardial tissue damage and boosts autophagy in damaged myocardial cells, increasing the survival rate of HF mice.

IS20 is an agonist of prokineticin receptor 1 (PKR1). It reduces Doxorubicin-induced apoptosis and ROS production by activating the Akt or MAPK pathways. In mouse models, IS20 protects the heart from cardiovascular toxicity caused by Doxorubicin, improving survival rates and cardiac function. It does not alter the cytotoxicity and anti-tumor effects of acute Doxorubicin treatment on breast cancer cells and the MDA-MB-231 xenograft mouse model. IS20 is applicable in cancer research.

EL244 is an inhibitor of Autotaxin (ATX) with an IC50 of 50 nM and an agonist of PPARγ with an IC50 of 1.3 μM and a Kd of 1.3 μM. In human HepG2 cells, EL244 exhibits low cytotoxicity with an EC50 of 81.2 μM and minimal inhibition of cardiac hERG potassium channels (12% at 25 μM). In vivo, EL244 significantly reduces pulmonary lysophosphatidic acid levels, alleviates fibrosis, restores respiratory function, and has limited systemic absorption. EL244 is suitable for research on idiopathic pulmonary fibrosis.

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

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