cardioprotective

Nicorandil (SG-75)(Ikorel) acts by relaxing the smooth muscle of the blood vessels, especially those of the venous system. It undertakes this through two methods. Firstly, by activating potassium channels, and secondly by donating nitric oxide to activate the enzyme guanylate cyclase. Guanylate cyclase causes activation of cGMP leading to both arterial and venous vasodilatation by de-phosphorylation of the myosin light chain.

Pinacidil (P 1134) is a guanidine that opens potassium channels and directly dilates peripheral blood vessels in small arteries, lowering blood pressure and peripheral resistance and producing fluid retention.

Danegaptide Hydrochloride (GAP-134 (Hydrochloride)) (GAP-134 Hydrochloride) is a selective modifier of the gap junction protein.

BTB06584 is an IF1-dependent, selective inhibitor of the mitochondrial F1 Fo-ATPase. BTB06584 is a novel acetohydroxyacid synthase(AHAS) inhibitor, a promising drug target against Mycobacterium tuberculosis (MTB).

(±)-Talinolol is a selective β1 adrenoceptor antagonist well known for its cardioprotective and antihypertensive activity.

UCF 101 is a specific inhibitor of HtrA2 and reduces apoptosis in PC12 cells.

Liriope muscari baily saponins C has an anti-thrombotic activity due to down-regulation of the increased mRNA expression levels of TF and IL-6.

Atpenin A5 is a potent and highly specific complex II inhibitor (IC50 ~10 nM), as well as an effective mKATP channel agonist and cardioprotective agent [1].

Resveratroloside has cardioprotective effect, it exhibits α±-glucosidase inhibitory activity, it also can inhibit hydroxylation of testosterone by CYP3A4.

GSK329 is an effective and selective inhibitor of TNNI3 Interacting Kinase (TNNI3K). GSK329 exhibits positive cardioprotective outcomes in the model of ischemia/reperfusion cardiac injury.

Panaxadiol (20(R)-Panaxadiol) is a novel antitumor agent extracted from the Chinese medicinal herb Panax ginseng.

Semaglutide is a long-acting, selective, competitive GLP-1R agonist and a long-acting analog of human glucagon-like peptide-1, exhibiting potent hypoglycemic, weight-loss, cardioprotective, and neuroprotective effects. Upon activation of the GLP-1R, semaglutide promotes insulin secretion, inhibits gastric emptying and appetite, while also enhancing autophagy and suppressing oxidative stress and apoptosis. Semaglutide also plays a role in regulating mitochondrial function and lipid metabolism. Semaglutide is being investigated for use in type 2 diabetes, obesity, Parkinson’s disease, metabolic and fatty liver diseases (MASLD), and other neurodegenerative and liver diseases, as well as in cancer research.

Necrostatin-7 (Necrostatin 7) is an inhibitor of necrotic apoptosis with cardioprotective effects, inhibits RANK-NFATc1 signaling, and attenuates macrophage differentiation into osteoblasts.

CMF019 (CMF-019) is a potent, G-protein-biased small-molecule agonist of the Apelin receptor (APJ/APLNR). CMF019 exhibits pKi values of 8.58, 8.49, and 8.71 for binding to APJ in humans, rats, and mice, respectively. CMF-019 exhibits cardioprotective effects in rodents. CMF019 can be utilized in mechanism and drug development for heart failure and pulmonary arterial hypertension.

CP-060 is a potent Ca2+ antagonist and inhibits Ca2+ overload with antioxidant and cardioprotective activities.

JTV-519 Formate is a Ca2+-dependent blocker of sarcoplasmic reticulum Ca2+-stimulated ATPase (SERCA). JTV-519 Formate is also a partial agonist of ryanodine receptors in striated muscle. JTV-519 Formate exhibits antiarrhythmic and cardioprotective properties.

BAY 60-6583 is a potent, high-affinity adenosine A2B receptor agonist (EC50 = 3 nM) with affinity for A2B receptors that exceeds that for A1, A2A, and A3 receptors.BAY 60-6583 is cardioprotective in a model of myocardial ischemia.The Ki values for BAY 60-6583 binding to mouse, rabbit, and dog A2BAR were 750 nM, 340 nM, and 330 nM, respectively. The Ki values of BAY 60-6583 binding to A2BAR in mice, rabbits and dogs were 750 nM, 340 nM and 330 nM respectively.

CERM-11956 is a beprudil derivative and an anti-ischemic agent with Ca2+ cardioprotective effects and induces negative inotropic effects.

YT 146 is a selective adenosine receptor A2 agonist with cardioprotective and vasodilatory effects that inhibits neointimal thickening after endothelial injury in rat femoral arteries.

Protectin D1 (Neuroprotectin D1) is a neuroprotectin produced by neuronal cells and is a potential cardioprotective agent.Protectin D1 attenuates myocardial ischemia/reperfusion injury and inhibits imiquimod-induced psoriasis-like skin inflammation by modulating the PI3K/AKT signaling pathway.

Furnidipine significantly reduced AoD and AF and had antiarrhythmic and cardioprotective effects at low doses in a rat model.

BIIB 722 Mesylate is a selective sodium-hydrogen exchange inhibitor with cardioprotective properties and can be used to study myocardial ischemia and myocardial infarction.

Scutellarin (Breviscapin) is a natural flavonoid isolated from Scutellaria baicalensis that exhibits antioxidant, anti-inflammatory, antithrombotic, neuroprotective, and cardioprotective and neuroprotective activities. Scutellarin demonstrates antiviral activity against HIV-1 IIIB, HIV-1 (74V), and HIV-1 KM018. Scutellarin inhibits the RANKL-mediated MAPK/NF-κB pathway (IC₅₀ = 10 μM) and activates the Nrf2/HO-1 antioxidant pathway (EC₅₀ = 5 μM). Scutellarin can be used in natural product development and basic research on cardiovascular and cerebrovascular diseases.

Tetrahydrocurcumin (HZIV 81-2), a major metabolite of curcumin, has strong antioxidant and cardioprotective properties.