hypercholesterolemia

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.

D-Thyroxine (Dextroxin) could lower cholesterol and also increases hepatic lipase which in turn improves utilization of triglycerides, leading to improve apolipoprotein E cholesterol particles.

AZD0780 (EX-A6975, PCSK9-IN-12) is an orally active PCSK9 inhibitor with high affinity for PCSK9 (Kd < 200 nM). It binds to a specific pocket in the C-terminal domain of PCSK9 without affecting the PCSK9–LDLR interaction. AZD0780 blocks the lysosomal trafficking of the PCSK9–LDLR complex and prevents PCSK9-induced LDLR degradation, making it useful for studies related to hypercholesterolemia.

Bococizumab(PF-04950615) is a humanized mAb against PCSK9 and an inhibitor of the synthesis of PCSK9 in the liver that reduces the amount of low-density lipoprotein cholesterol (LDL-C) in the blood.Bococizumab is used to treat hypercholesterolemia.

Crilvastatin (PMD 387) is a novel, non-competitive hydroxymethylglutaryl coenzyme A reductase inhibitor with cholesterol-lowering activity, inhibiting cholesterol uptake in rats with hereditary hypercholesterolemia.

Lifibrol (U-83860) is an inhibitor of cholesterol synthesis.Lifibrol has anticholesterol and hypolipidemic properties and promotes the conversion of LDL Apo B-100 in patients with hypercholesterolemia and mixed hyperlipidemia.

Eldacimibe (WAY-ACA-147) is an ACAT2 inhibitor for the treatment of cardiovascular disease and endocrine and metabolic disorders, study of atherosclerosis and hypercholesterolemia.

Lovastatin (MK-803) is an HMG-CoA reductase inhibitor (IC50=3.4 nM). Lovastatin lowers cholesterol and is commonly used as a lipid-lowering agent in the treatment of hypercholesterolemia.

Hyodeoxycholic acid (NSC 60672) has been used in trials studying the treatment of Hypercholesterolemia.

Inositol nicotinate (Mesotal) has the effect of lowering cholesterol and expanding peripheral blood vessels for hypercholesterolemia and atherosclerosis.

Lapaquistat acetate (TAK-475) is a squalene synthase inhibitor with potential anti-inflammatory activity. It mitigates statin-induced toxicity in human skeletal muscle cells and protects guinea pigs from simvastatin-induced myotoxicity, useful for research on hypercholesterolemia and HMG-CoA reductase deficiency.

Tetrahydrobiopterin (BH4) is a cofactor for aromatic amino acid hydroxylases and an essential cofactor for nitric oxide synthase (NOS), which is used in the study of endothelial dysfunction such as hypertension, hypercholesterolemia, and diabetes.

Colestipol hydrochloride is a bile acid-binding anionic exchange polymer that effectively reduces cholesterol levels, commonly utilized in the study of hypercholesterolemia.

MI-883 is an orally active Constitutive Androstane Receptor (CAR, EC50=73 nM) agonist and a Pregnane X Receptor (PXR, IC50=0.1 μM) antagonist. It enhances CAR LBD assembly (EC50=0.38 µM) and activates the CAR3 variant (EC50=0.074 µM), inducing CYP2B6 mRNA expression in HepaRG and primary human hepatocytes. Additionally, MI-883 inhibits the basal activity of PXR (IC50=2.03 µM) and reduces CYP3A4 mRNA expression in transiently transfected HepG2 cells. It also regulates cholesterol metabolism and bile acid excretion, improving hypercholesterolemia in mouse models.

THR-β agonist 2 diacetate (Compound 3) is a potent THR-β agonist with potential applications in researching metabolic disorders such as obesity, hyperlipidemia, hypercholesterolemia, and diabetes, as well as other conditions like steatosis and non-alcoholic steatohepatitis (NASH), atherosclerosis, and other related diseases and conditions.

PCSK9-IN-33 (Compound 1'f) is a PCSK9 inhibitor with an IC50 of 161 nM, which can be utilized in hypercholesterolemia research.

Ganglioside GM3 is a precursor of a, b, and c series gangliosides and interacts with transmembrane receptors such as epidermal growth factor and insulin receptors, modulating receptor function by creating specialized lipid environments. Synthesized by GM3 synthase, it can be used in studies related to hypercholesterolemia.

Seladelpar lysine, a selective PPAR-δ agonist, is used for the therapy of Homozygous Familial Hypercholesterolemia (HoFH).

Eflucimibe is an ACAT inhibitor. Eflucimibe regulates endogenous hypercholesterolemia in a synergistic manner in New Zealand rabbits fed a casein-enriched diet. In vivo, orally administered Eflucimibe displayed high potency and efficacy as an antihypercholesterolemic compound in different cholesterol-fed animals (guinea-pig, rat, rabbit).

Hyzetimibe, a cholesterol absorption blocker, is used potentially for the treatment of hypercholesterolemia.

PPD 10558, a HMG-CoA reductase inhibitor, is used potentially for treatment of primary hypercholesterolemia.

Clofibrin is a kind of hypolipidemic drug, which can reduce Hypertriglyceride and hypercholesterolemia.

4-Hydroxy Atorvastatin calcium salt is metabolised by cytochrome P450 CYP3A4 and has antimicrobial and anti-microbial activity.Atorvastatin is a lipid-lowering HMG-CoA reductase inhibitor.

Diosgenin glucoside (Trillin) and other synthetic glycosides with similar activities may be of use in the management of hypercholesterolemia and atherosclerosis. Significant inhibition of Diosgenin glucoside synthesis and stimulation of solasodine glucosylation was found only with PC molecular species containing fatty acids with a chain length of 12-18 carbon atoms.