atherosclerotic

Orlistat (Tetrahydrolipstatin) is a lipase inhibitor and a fatty acid synthase (FASN) inhibitor. Orlistat has been shown to promote weight loss.

Limaprost (17α,20-dimethyl-δ2-PGE1) is an analog of PGE1 with structural modifications intended to give it a prolonged half-life and greater potency.It is a potent and orally active vasodilator. Limaprost increases blood flow and inhibits platelet aggregation. Limaprost (17α,20-dimethyl-δ2-PGE1) can be used for pain relief, has antianginal effects, and has potential for ischaemic symptoms treatment.

LDL-IN-3 shows anti-atherosclerotic and antioxidant activities.

Evolocumab is an inhibitor of the humanized monoclonal antibody PCSK9. It binds to circulating PCSK9 protein, resulting in inhibition of PCSK9 binding to LDLR. It can be used in studies of hypercholesterolemia and atherosclerotic cardiovascular disease.

BMS-212122 (UNII-0Z473OO6GB) is a potent inhibitor of microsomal triglyceride transfer protein (MTP) and has shown hypolipidemic effects in animal studies.BMS-212122 significantly reduced lipid content and monocyte-derived (CD68+) cells in atherosclerotic plaques.

Benzyl isothiocyanate (Benzoylthiocarbimide) (BITC) is an isothiocyanate originally found in cruciferous vegetables. It shows immunomodulatory, anti-parasitic, antibiotic, antioxidative, anti-atherosclerotic, anti-angiogenic, anti-metastatic, anticancer chemotherapeutic, and chemopreventive activities.

Daidzin (Daidzoside) is an isoflavone isolated from soya bean with anti-oxidant, anti-carcinogenic, and anti-atherosclerotic activities.

Patchouli alcohol (Patchoulol) is a naturally occurring tricyclic sesquiterpenoid found in patchouli oil. It is a key bioactive component known for its immunomodulatory, anti-inflammatory, antioxidant, antitumor, antibacterial, anti-atherosclerotic, antiemetic, and sedative properties.

L-Arginine (L-Arg) is a substrate of endothelial nitric oxide synthase (eNOS). L-Arginine is transported to vascular smooth muscle cells via a family of cationic amino acid transporters and is metabolized to nitric oxide, polyamines, or L-proline. L-Arginine is a potent vasodilator and can be used to induce experimental acute pancreatitis.

Squalene (AddaVax) is an intermediate in cholesterol synthesis. Squalene has a variety of pharmacological properties, such as antilipemic, hepatoprotective, anti-atherosclerotic, cardioprotective, antioxidant, antitumor and antifungal.

Cholesteryl linoleate is the major cholesteryl ester in LDL and atherosclerotic lesions. It is present in LDL as a cholesteryl ester that is oxidized to form cholesteryl linoleate hydroperoxides using LDL receptor-associated proteins that are transferred to the plasma membranes of macrophages and CHO cells expressing 15-lipoxygenase.

3-Chloro-L-Tyrosine (Chlorotyrosine), a specific marker of myeloperoxidase-catalyzed oxidation, is markedly elevated in low-density lipoprotein isolated from human atherosclerotic intima. In particular, myeloperoxidase halogenates tyrosine residues in plasma proteins and generates 3-chlorotyrosine (CY). The detection of free chlorotyrosine in blood or urine arises from the degradation of these chlorinated proteins. CY concentrations may be useful for monitoring the activation of neutrophils in asthmatic patients.

Undecanedioic acid has been found in parts of human aortas with advanced atherosclerotic lesions associated with intercellular matrix macromolecules and specifically with elastin.

Ethyl linoleate is a natural product.

Beauveriolide III, a cyclodepsipeptide found in Beauveria fungi, inhibits lipid droplet formation (at 3-10 μM) and cholesterol synthesis (IC50=0.41 μM). This compound also suppresses acyl-coenzyme A:cholesterol acyltransferase (ACAT) activity (IC50=5.5 μM) and reduces atherosclerotic lesion size in Ldlr-/- and ApoE-/- mouse models (25-50 mg/kg).

GW9508(GW 9508) is a potent and selective agonist for FFA1 (GPR40), stimulates insulin secretion in a glucose-sensitive manner.

Bovinic acid ((9Z,11E)-Octadecadienoic acid) is a conjugated linoleic acid with anticancer and anti-atherosclerotic activity and can be used to study coronary heart disease and obesity in the elderly.

SB-657510 is a urotensin II (UII) receptor (UT) antagonist. The Ki values of UT for human, monkey, cat, rat and mouse were 61, 17, 30, 65 and 56 nM, respectively. SB-657510 plays an anti-inflammatory role by inhibiting UII-induced inflammatory mediators, such as adhesion molecules, in human vascular endothelial cells and upregulation of cytokines and tissue factors. SB 657510 has a therapeutic effect on diabetes-related atherosclerotic disease in diabetic mouse models.

SP-8356 is a potent, orally active inhibitor of cluster of differentiation 147 (CD147),and is an anti-inflammatory synthetic verbenone derivative, with anti-atherosclerotic effects.

Triacsin C (WS 1228A) from Streptomyces aureofaciens is a differential inhibitor of arachidonic acid coenzyme A synthetase and non-specific long-chain acyl-coenzyme A synthetase, with anti-atherosclerotic activity, inhibition of ACSL activity, and inhibition of the accumulation of TAGs into lipid droplets (LDs).Triacsin C has been used to study rotavirus infection and Alzheimer;s disease. Triacsin C is used to study rotavirus infection and Alzheimer;s disease.

Glyparamide is a hypoglycemic compound that reduces platelet aggregation, resulting in less atherosclerotic plaque formation.

DG-041 is an antagonist of high-affinity EP3 receptor (IC50s: 4.6 nM and 8.1 nM in the binding and FLIPR assay, respectively). DG-041 inhibits PGE2 facilitation of platelet aggregation and has the blood-brain barrier permeability.

TRAF-STOP inhibitor 6877002 (CD40-TRAF6 inhibitor), is a selective inhibitor of CD40-TRAF6 interaction. TRAF-STOP 6877002 reduces leukocyte recruitment, and reduces macrophage activation; reduces macrophage proliferation in atherosclerotic plaques.

Timofibrate, a thiazolidine derivative patented by Italchemi S.p.A.-Istituto Chimico Farmaceutico, possesses anti-atherosclerotic, cholesterol-lowering, and liver-protective properties.