atherosclerosis

Eplerenone (CGP 30083) is an aldosterone receptor antagonist and potassium-sparing diuretic used in the therapy of hypertension. Eplerenone therapy has been associated with transient elevations in serum aminotransferase levels, but has yet to be linked to cases of clinically apparent drug induced liver disease.

Loxoprofen (Koloxo) is an anti-inflammatory non-steroidal medicine.

Lacidipine (SN-305) is a lipophilic dihydropyridine calcium antagonist with an intrinsically slow onset of activity. Due to its long duration of action, lacidipine does not lead to reflex tachycardia. It displays specificity in the vascular smooth muscle, where it acts as an antihypertensive agent to dilate peripheral arterioles and reduce blood pressure.

Anagliptin (SK-0403) is a potent inhibitor of DPP-4 (IC50 of 3.8 nM) used in the treatment of type 2 diabetes mellitus.

Ethyl linoleate is a natural product.

SMS1-IN-1 is a potent inhibitor of sphingomyelin synthase 1 (SMS1, IC50 = 2.1 μM), and can be used in the atherosclerosis studies.

LY518674 (LY-674) decreases triglycerides and increases HDL-C and is used for the treatment of atherosclerosis. LY518674 is an effective and selective PPARα agonist (EC50: 42 nM for human PPARα).

PHPS1 is an inhibitor of Shp2. PHPS1 efficiently inhibits activation of Erk1/2 by the leukemia-associated Shp2 mutant, Shp2-E76K, and blocks the anchorage-independent growth of a variety of human tumor cell lines.

2-Hydroxybenzylamine, a potent small molecule scavenger of IsoLGs, sequesters the reactive species as inert adducts. 2-Hydroxybenzylamine may be used to decrease early recurrence of atrial fibrillation and other atrial arrhythmias following atrial fibrillation ablation by decreasing IsoLG adducts with native biomolecules.

T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of ~50 nM and 5 μM, respectively; it inhibits nuclear factor/κB (NF/κB).

1. Loganic acid (Loganate) and geniposide exhibit both sides effect on superoxide generation.

IMM-H007 is a novel lipid-lowering agent, increasing abca1 protein expression

BI-0115 is a selective small molecule inhibitor of LOX-1 that blocks cellular uptake of oxLDL. It binding triggers receptor inhibition by formation of dimers of the homodimeric ligand binding domain. The structure of LOX-1 bound to BI-0115 shows that inte

Clematichinenoside AR exerts anti-inflammatory and immunosuppressive properties, it has anti-arthritic effects on PI3K/Akt signaling pathway and TNF-α± associated with collagen-induced arthritis.

N-(p-Coumaroyl) Serotonin, a polyphenol isolated from the seeds of safflower, exhibits antioxidant, cardioprotective effects after ischemia, and antitumor activity. It may improve vascular distensibility and reduce cardiovascular risk. N-(p-Coumaroyl) Serotonin ameliorates atherosclerosis and distensibility of the aortic wall in vivo, and is commonly used in atherosclerosis research.

Emodin 6-O-β-D-glucoside (Glucoemodin) can protect barrier integrity and inhibit HMGB1-mediated inflammatory responses, which suggests a potential use as a therapy for sepsis or septic shock. Emodin 6-O-beta-D-glucoside has anti-inflammatory activities and also may have significant therapeutic benefits against diabetic complications and atherosclerosis.

Vulpinic Acid (Pulvinic acid methyl ester) is a lichen metabolite with anti-inflammatory, antibacteria, properties, plant growth inhibitor.

Rhamnocitrin can enhance the immune function, improve the formation of spleen cells of mice serum hemolysin of chicken red blood cell immune.

LDL-IN-3 belongs to synthetic compounds and is an antioxidant and anti-atherosclerotic agent with good cell permeability and cardiovascular protective properties. This compound is used for the treatment of atherosclerosis-related diseases, effectively inhibiting oxidative stress and lipid deposition, and reducing arterial plaque formation.

GW9662 (TIMTEC-BB SBB006523) is a PPARγ antagonist (IC50=3.3 nM) with selectivity. GW9662 can be used to study the pathogenesis of metabolic diseases, such as obesity and diabetes, by inhibiting the activity of PPARγ. GW9662 can be used to study the pathogenesis of inflammatory diseases, such as atherosclerosis and rheumatoid arthritis. GW9662 has anti-tumor effect.

(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.

Icosabutate (NST-4016) is an orally active derivative of eicosapentaenoic acid that inhibits hepatic inflammation and fibrosis in NASH, improves cardiovascular risk profiles in statin-treated patients with residual hypertriglyceridemia, lowers triglycerides, and may be useful in studies of liver fibrosis and atherosclerosis.

PSI-697 (P-Selectin Inhibitor) is an orally active P-selectin inhibitor with anti-inflammatory and anti-thrombotic effects, useful for studying cardiovascular diseases such as atherosclerosis.

Octimibate (Octimibato) is a non-prostaglandin platelet aggregation inhibitor and cyclic prostaglandin agonist.Octimibate is used in the treatment of cardiovascular disease and can be used to study atherosclerosis and thrombosis.