artery

Bumetanide (PF 1593) is a potent sulfamoylanthranilic acid derivative belonging to the class of loop diuretics. In the brain, bumetanide may prevent seizures in neonates by blocking the bumetanide-sensitive sodium-potassium-chloride cotransporter (NKCC1), thereby inhibiting chloride uptake thus, decreasing the internal chloride concentration in neurons and may block the excitatory effect of GABA in neonates.

Pramipexole dihydrochloride hydrate (Mirapex) is the hydrochloride salt of pramipexole, a benzothiazole derivative. As a nonergot dopamine agonist, pramipexole binds to D2 and D3 dopamine receptors in the striatum and substantia nigra of the brain.

The quinuclidine PHA 568487 free base is an agonist of the alpha 7 nicotinic acetylcholine receptor that was designed to mitigate the bioactivation associated with the core scaffold and subsequently remove associated liabilities with in vivo tolerability.

Zotarolimus (ABT-578), an analogue of rapamycin, inhibits FKBP-12 (IC50= 2.8 nM).

BQ-123 is a selective endothelin A receptor (ETA) antagonist with IC50 of 7.3 nM. Phase 2.

Atuliflapon (AZD5718) is a novel 5-Lipoxygenase Activating Protein(FLAP) inhibitor for Treatment of Coronary Artery Disease.

Taurocholic acid (N-Choloyltaurine) is a bile acid involved in fat emulsification, possessing notable biological and immunomodulatory activities. It can inhibit bile duct injury induced by hepatic artery ligation by upregulating VEGF-A expression and protect cholangiocytes from TNF-α-induced damage via a PI3K-mediated pathway, and is commonly used to induce pancreatitis models.

Arbutamine (GP 21213) is a novel potent non-selective beta-adrenoceptor agonist with alpha-1-sympathomimetic activity.Arbutamine promotes cardiac stress and increases heart rate, cardiac contractility.Arbutamine can be used to study cardiac stress and coronary artery disease

BQ-788 is a selective and potent ETB receptor antagonist with potential hypertensive activity.BQ-788 inhibits ET-1 binding to ETB receptors and inhibits exogenous ET-1-induced elevation of coronary artery perfusion pressure.

(2R,3S)-N-(4-(2,6-dimethoxyphenyl)-5-(5-methylpyridin-3-yl)-4H-1,2,4-triazol-3-yl)-3-(5-methylpyrimidin-2-yl)butane-2-sulfonamide is an Apelin receptor agonist with an EC50 for Apelin receptors of 0.012 µM.(2R,3S)-N-(4-(2,6-dimethoxyphenyl)-5-(5-methylpyridin-3-yl)-4H-1,2,4-triazol-3-yl)-3-(5- methylpyrimidin-2-yl)butane-2-sulfonamide is used in the treatment of heart failure, atherosclerosis, obesity, diabetes mellitus, amyotrophic lateral sclerosis, coronary artery disease, hypertension, stroke and myocardial infarction.

GP2-114 is a catecholamine motility mimetic that produces current-dependent cardiovascular effects when administered via transdermal iontophoresis and can be used to study coronary artery disease (CAD).

Atopaxar (E5555), a reversible PAR-1 thrombin receptor antagonist, interferes with platelet signaling. Atopaxar has been investigated for the treatment of Coronary Artery Disease and Acute Coronary Syndrome.

FPL 55712 is a leukotriene receptor and SRS-A antagonist that inhibits bronchoconstriction and can be used in studies of asthma and coronary artery thrombosis.

Talibegron hydrochloride (ZD2079 hydrochloride) is a β3 adrenergic receptor agonist with a pD2 of 3.72 on phenylephrine-preconstricted rat mesenteric artery. It relaxes rat mesenteric artery and isolated aorta in vitro, and inhibits ob gene expression and circulating leptin levels in lean mice in vivo.

TGX-115 is a cell-permeable and potent inhibitor of the PI 3-K isoform p110β p110δ (IC50 values of 0.13 μM for p110β and 0.63 μM for p110δ), an enzyme that regulates platelet adhesion and inhibits phosphoinositide (PI) 3-kinase, and can be used to treat coronary artery occlusion, stroke, acute coronary artery It can be used to treat cardiovascular diseases such as coronary occlusion, stroke, acute coronary syndrome, acute myocardial infarction, restenosis, atherosclerosis and unstable angina.

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.

Iroxanadine (BRX-005) is a Novel small molecule MAPK p38 inhibitor that induces phosphorylation of p38 SAPK and induces concentration-dependent relaxation in guinea pig pulmonary artery preparations precontracted with phenylephrine.13480-84-5

KT-362 fumarate is a novel compound that acts as an antagonist of calcium channels, potassium channels and sodium channels.KT-362 fumarate causes vasodilation by affecting intracellular calcium mobilization in atrial muscle cells.KT-362 fumarate has a relaxing effect on femoral and basilar artery strips in rabbits.

(Rac)-Modipafantis an orally available and selective platelet-activating factor receptor (PAFR) antagonist that inhibits PAF-induced aggregation of washed platelets in rabbits, and can be used to study arthritis and ischemia reperfusion (I R) in the superior mesenteric artery (SMA) of the rat.

Piclozotan (anhydrous), a 5-HT1A receptor agonist, demonstrated significant neuroprotective activity in a transient middle cerebral artery occlusion (t-MCAO) model, ameliorating motor complications in patients with advanced Parkinson's disease.

Granotapide is a microsomal triglyceride transfer protein (MTP) inhibitor that treats and rather prevents atherosclerosis, coronary artery disease, metabolic syndrome, obesity, diabetes mellitus, prediabetes mellitus, and hypertension.

Indecainide (Ricainid) is a novel antiarrhythmic compound that is carcinogenic and can be used to study chronic stable ventricular arrhythmias secondary to coronary artery disease or cardiomyopathy.

Pinokalant (LOE-908) is a novel non-selective cation channel inhibitor.Pinokalant significantly reduces cortical infarct volume in in vivo experiments, improves the metabolic and electrophysiological status of the ischemic penumbra region, and reduces the size of the lesion on magnetic resonance images in the acute phase after middle cerebral artery occlusion in rats.Pinokalant is a potential SARS-CoV-2 protease inhibitor for the study of stroke.

BMS-593214 is an active site-directed factor (F) VIIa inhibitor that exhibits antithrombotic and antihaemostatic properties. It acts as a direct competitive inhibitor of human FVIIa and a non-competitive inhibitor of FVIIa-activated substrate FX. Additionally, BMS-593214 effectively prevents electroinduced carotid artery thrombosis (AT) and wire-induced vena cava thrombosis (VT).