Abciximab (C7E3), a chimeric mouse/human monoclonal antibody, is a glycoprotein (GP) IIb/IIIa inhibitor. Abciximab inhibits platelet aggregation and leucocyte adhesion by binding to the glycoprotein IIb/IIIa, vitronectin and Mac-1 receptors[1].
Fenquizone (MG-13054), a thiazide-like diuretic, exhibits chronic antihypertensive effect. Fenquizone can be used for the research of oedema and hypertension[1].
Icariin is a flavonol glycoside. Icariin inhibits PDE5 and PDE4 activities with IC50s of 432 nM and 73.50 μM, respectively. Icariin also is a PPARα activator.
Cladribine is an adenosine deaminase inhibitor used to treat hairy cell leukemia and multiple sclerosis. Target: Adenosine DeaminaseCladribine possesses concentration-dependent apoptosis-inducing potential in the HSB2 cells. Cladribine inhibits growth of primary mast cell (MC) and the MC line HMC-1 in a dose-dependent manner, with lower IC50 values recorded in HMC-1.2 cells harboring KIT D816V compared to HMC-1.1 cells lacking KIT D816V. Cladribine (0.7-3.5 mM) and/or diltiazem (2.4 mM), is injected intraperitoneally into adult zebrafish and red blood cell (RBC) lysates are assayed by HPLC for levels of purine nucleotides (e.g. ATP), potential biomarkers of cardiovascular health. Diltiazem increased RBC ATP concentrations, which are inhibited by co-injection of cladribine.
Pexelizumab (h5G1. 1-SC) is a humanized scFv monoclonal antibody directed against the C5 complement component. Pexelizumab inhibits apoptosis and leukocyte infiltration. Pexelizumab can be used for the research of cerebral IR injury and myocardial infarction[1][2].
SCH79797 dihydrochloride is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 dihydrochloride inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 dihydrochloride also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes[1][2][3][4].
LDL-IN-3 is an anti-atherosclerotic compound extracted from patent WO/2005/039596A1, example C25 and patent US 6133467, example 3.
KRN4884 is a K+ channel opener. In the presence of intracellular ATP (1 mM), KRN4884 (0.1-3 μM) activates KATP channels in a concentration-dependent manner (EC50=0.55 μM).
Eptifibatide acetate is a cyclic heptapeptide, acts as a competitive antagonist for the activated platelet glycoprotein IIb/IIIa receptor, with anti-platelet activity[1].
RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 (HY-108566). RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell apoptosis[1][2].
Cangrelor tetrasodium, an adenosine triphosphate analogue, is a reversible and selective platelet P2Y12 antagonist, with prompt and potent antiplatelet effects. Cangrelor tetrasodium directly blocks adenosine diphosphate (ADP)-induced activation and aggregation of platelets. Cangrelor tetrasodium is also a nonspecific GPR17 antagonist[1][2].
MRS1845 is a Ca2+ channel blocker with relative specificity for store-operated calcium entry (SOCE) channels[1].
Zifaxaban is a novel, potent, selective, direct and oral factor Xa inhibitor with IC50 of 11.1 nM (human FXa), displays > 10,000-fold selectivity than other serine proteases; also deoes not impair platelet aggregation induced by collagen, adenosine diphosphate (ADP) or arachidonic acid; significantly prolongs clotting time, prothrombin time (PT), and activated partial thromboplastin time (APTT) in the plasma of humans, rabbits, and rats, with a relatively weak effect on thrombin time; strongly suppresses thrombus formation with ED50 values of 3.09 mg/kg in venous thrombosis models in rats.
Macitentan is an orally active, non-peptide endothelin receptor antagonist for the treatment of idiopathic pulmonary fibrosis and pulmonary arterial hypertension.
Vanillylmandelic acid is the endproduct of epinephrine and norepinephrine metabolism. Vanillylmandelic acid can be used as an indication of the disorder in neurotransmitter metabolism as well. Vanillylmandelic acid has antioxidant activity towards DPPH radical with an IC50 value of 33 μM[1].
TM5275 sodium is a plasminogen activator inhibitor (PAI-1) with an IC50 of 6.95 μM.
Captopril disulfide is a metabolite of Captopril with antihypertensive activity[1].
BMS-654457 is a small-molecule, reversible inhibitor of factor XIa (FXIa), binding with human and rabbit FXIa with Kis of 0.2 and 0.42 nM, respectively.
AMG 333 is a potent and highly selective TRPM8 antagonist with an IC50 of 13 nM.
Moricizine Hydrochloride (EN 313) is an orally active Class I antiarrhythmic agent. Moricizine Hydrochloride decreases the maximum rate of phase 0 depolarization; increases rates of phase 2 and 3 repolarization, decreases action potential duration, and decreases effective refractory period[1].
Lomitapide (AEGR-733; BMS-201038) is a potent inhibitor of microsomal triglyceride-transfer protein (MTP) with an IC50 of 8 nM in vitro.
5-Lipoxygenase-In-1 is a 5-Lipoxygenase inhibitor extracted from patent EP 331232 A2, table 4, compound example 4.10.
Pitavastatin lactone is a major metabolite of Pitavastatin in humans. Pitavastatin is a potent competitive inhibitor of HMG-CoA reductase little metabolized in hepatic microsomes[1].
Angiopeptin, a cyclic octapeptide analogue of somatostatin, markedly inhibits myointimal proliferation in response to endothelial cell injury. Angiopeptin is a potent and full agonists to inhibit adenylate cyclase or stimulate extracellular acidification through the sst2 or sst5 receptor. Angiopeptin is a potent inhibitor of growth hormone release and insulin-like growth factor-1 production[1][2].
Prasugrel is a platelet inhibitor with IC50 value of 1.8 μM.IC50 value:Target: P2Y12 receptorPrasugrel is a novel platelet inhibitor used for the reduction of thrombotic cardiovascular events (including stent thrombosis) in patients with acute coronary syndrome who are to be managed with PCI. Prasugrel reduces the aggregation ("clumping") of platelets by irreversibly binding to P2Y12 receptors. In rat platelets, prasugrel AM inhibited in vitro platelet aggregation induced by ADP (10 μm) with an IC50 value of 1.8 μm. From Wikipedia
Nicorandil-d4 (SG-75-d4) is the deuterium labeled Nicorandil. Nicorandil (SG-75) is a potent potassium channel activator and targets vascular nucleoside diphosphate-dependent K+ channels and cardiac ATP-sensitive K+ channels (KATP). Nicorandil is a nicotinamide ester with vasodilatory and cardioprotective effects and has the potential for angina and forischemic heart diseases[1][2][3].
Fulacimstat is an orally available chymase inhibitor, with IC50s of 4, 3 nM for human and hamster chymase enzyme, respectively.
PF-06282999 is a potent and selective myeloperoxidase inhibitor which is potential useful for the treatment of cardiovascular diseases.
Norepinephrine tartrate (Levarterenol tartrate), a naturally occurring chemical in the body that acts as both a stress hormone and neurotransmitter, is a β1-selective adrenergic receptor agonist with EC50 of 5.37 μM.
DL-m-Tyrosine shows effects on Arabidopsis root growth. Carbidopa combination with DL-m-tyrosine shows a potent hypotensive effect[1][2].