lipoprotein ldl

Torcetrapib (CP-529414) is a cholesteryl ester transfer protein (CETP) inhibitor designed to reduce the heterotypic transfer of cholesteryl ester from HDL to LDL and or VLDL. It failed in phase III trials due to an excess of deaths.

Tirzepatide (LY-3298176) is a dual agonist of glucose-dependent polypeptide (GIP) (EC50=0.042 nM) and glucagon-like peptide-1 (GLP-1) (EC50=0.086 nM) receptors, and it has neuroprotective activity. It can improve blood pressure and lower low-density lipoprotein (LDL) cholesterol and triglycerides, and can be used to study diabetes and obesity.

Atorvastatin Sodium (Lipitor) is a competitive inhibitor of HMG-CoA reductase and increases the expression of low density lipoprotein (LDL) receptors on hepatocytes. Atorvastatin Sodium treatment inhibits aquaporin 4 to reduce ischaemic brain oedema.

Ro 48-8071 fumarate, an inhibitor of OSC (Oxidosqualene cyclase; IC50=6.5 nM), exhibits LDL (low-density lipoprotein) cholesterol-lowering activity.

Gemcabene calcium , a first-in-class lipid-lowering agent, lowers low-density lipoprotein cholesterol (LDL-C), decreases triglycerides, and raises high-density lipoprotein cholesterol (HDL-C) andexerting anti-inflammatory activity, lowers pro-inflammatory acute-phase protein, C-reactive protein (CRP).

PCSK9-IN-29 serves as a lipid-lowering agent that enhances the expression of low-density lipoprotein receptor (LDLR) protein and reduces PCSK9 protein expression in hepG2 cells. Additionally, in crab-eating macaques on a high-fat diet, it lowers serum LDL-C, TC, and liver enzyme ALT levels, reduces body weight and fat, and boosts bone mineral content. PCSK9-IN-29 is useful for studies involving non-alcoholic fatty liver disease and obesity.

PCSK9-IN-30 (Compound 3f), a PCSK9 inhibitor, effectively targets a cryptic binding groove on PCSK9, thereby preventing PCSK9 from associating with the low-density lipoprotein receptor (LDLR) (IC 50 = 537 nM). This inhibition aids in the restoration of low-density lipoprotein (LDL) uptake by liver cells and significantly reduces plasma cholesterol levels. Demonstrating good bioavailability in mice, PCSK9-IN-30 holds potential for research within cardiovascular disease contexts.

Oxidized low density lipoprotein (Human) (Human ox-LDL) plays a crucial role in atherogenesis and contributes to endothelial dysfunction through the cytoplasmic adapter protein TRAF3IP2. This compound also promotes endothelial cell activation, leads to increased production of adhesion molecules, and reduces eNOS activity and NO production. Additionally, Human ox-LDL activates the NLRP3 inflammasome in macrophages.

MD-700 is an innovative isobenzofuranone that increases LDL receptor expression in HepG2 cells within 4 hours at a concentration of 0.03 microg ml. MD-700 selectively reduces levels of LDL and very low-density lipoprotein cholesterol.

GI-Y2 is a GSDMD inhibitor that suppresses macrophage pyroptosis induced by oxidized low-density lipoprotein (ox-LDL). In vivo, GI-Y2 dose-dependently reduces atherosclerotic plaques and decreases lesion size and fibrosis in the aortic root of ApoE-/- mice. GI-Y2 holds potential for research in pyroptosis and cardiovascular diseases, such as atherosclerosis.

KYLO-0603 is an orally active and selective THR-β agonist with an EC50 of 31.07 nM. It effectively reduces serum cholesterol and low-density lipoprotein cholesterol levels. By activating THR-β receptors, KYLO-0603 enhances the expression of THR-regulated genes like iodothyronine deiodinase 1 (Dio1), malic enzyme 1 (Me1), and thyroid hormone-responsive (Thrsp) gene, while it inhibits the expression of inflammatory and fibrosis-related genes, including low-density lipoprotein receptor (LDL-R) gene. This compound is applicable for the study of metabolic associated steatohepatitis (MASH) and liver fibrosis.

Peroxisome proliferator-activated receptors (PPARs) α, δ, γ are ligand-activated nuclear transcription factors involved in the regulation of energy homeostasis as well as insulin sensitivity and glucose metabolism. Pharmacologies of PPARδ receptor agonists, though relatively obscure, have recently been reported to elevate high-density lipoprotein (HDL) cholesterol and lower plasma triglyceride (TG) levels in obese insulin resistant rhesus monkeys. CAY10592 is a full PPARδ agonist (EC50 = 30 nM) in a fatty acid oxidation assay of rat L6 muscle cells with desirable oral pharmacokinetic properties. In a transactivation assay using human PPAR receptors, CAY10592 acts as a selective partial PPARδ agonist (EC50 = 53 nM) with no effect on PPARα or PPARγ activity up to 30 μM. Chronic treatment of high fat fed ApoB100/CETP-transgenic mice with CAY10592 at a dose of 20 mg/kg increases HDL levels, decreases LDL and TG levels, and improves insulin sensitivity.

MK-8262, an orally active and potent cholesteryl ester transfer protein (CETP) inhibitor (IC 50 = 53 nM, log D = 5.3), is a bistrifluoromethyl analogue that shows promise in research related to high-density lipoprotein (HDL) and low-density lipoprotein (LDL) with potential implications for coronary heart disease (CHD).

PCSK9 modulator-2 (Compound 1) is a potent PCSK9 modulator (EC 50 = 202 nM) with potential applications in hyperlipidemia research. Proprotein convertase subtilisin kexin type 9 (PCSK9) is a recently validated therapeutic target for lowering low-density lipoprotein cholesterol (LDL-C) [1].

PCSK9 modulator-3 (Compound 13) is a potent PCSK9 modulator with an EC50 value of 2.46 nM, showing potential in hyperlipidemia research. PCSK9 is a newly established target for lowering low-density lipoprotein cholesterol (LDL-C) [1].

PCSK9 modulator-4 (Compound 21) is a potent PCSK9 modulator (EC50 = 0.15 nM) utilized in hyperlipidemia research, targeting the recently validated low-density lipoprotein cholesterol (LDL-C) lowering mechanism [1].

AMPK activator 6 (Compound GC) activates the AMPK pathway and reduces lipid content in HepG2 and 3T3-L1 cells. It significantly suppresses increases in total cholesterol (TC), low-density lipoprotein-C (LDL-C), triglyceride (TG), and other biochemical indices in blood serum, holding research value in non-alcoholic fatty liver disease (NAFLD) and metabolic syndrome.

Pitavastatin (NK-104) sodium is a potent inhibitor of hydroxymethylglutaryl-CoA (HMG-CoA) reductase and an inducer of the hepatocyte low-density lipoprotein cholesterol (LDL-C) receptor. It inhibits acetate synthesis of cholesterol in HepG2 cells and exhibits anti-atherogenic, anti-osteoarthritic, anti-asthmatic, anti-tumour, neuroprotective, hepatoprotective, and nephroprotective effects.

Bambuterol is a prodrug of β2-agonist commonly used for the treatment of asthma and chronic obstructive pulmonary disease (COPD) with the advantage of once daily dosing and favorable side effect profile. Administration of a single-dose of R-bambuterol resulted in dose-dependent reductions in the levels of plasma LDL-C, high-density lipoprotein cholesterol (HDL-C), total cholesterol (TC), apolipoprotein B (ApoB) and apolipoprotein A1 (ApoA1) at Tmax. R-bambuterol can lower the plasma levels of LDL-C, and marginally raise the ratio of ApoA1 ApoB (indicator of HDL-C LDL-C) with both a single dose and multiple doses. R-bambuterol was more potent in LDL-C lowering than rac-bambutero

6,8-Diprenyleriodictyol is an antioxidant, which inhibits Cu(2+)-mediated oxidation of human low density lipoprotein (LDL).

Azalanstat HCl is an anti-obesity drug acting as a lanosterol 14α-demethylase inhibitor. Azalanstat HCl has been shown to inhibit cholesterol synthesis in HepG2 cells, human fibroblasts, hamster hepatocytes and hamster liver, by inhibiting the cytochrome P450 enzyme lanosterol 14 alpha-demethylase. When administered orally to hamsters fed regular chow, RS-21607 (50 mg kg day) lowered serum cholesterol in a dose-dependent manner (ED50 = 62 mg kg) in a period of 1 week. It preferentially lowered low density lipoprotein (LDL) cholesterol and apo B relative to high density lipoprotein (HDL) cholesterol and apo A-1.

Azalanstat mesylate is an anti-obesity drug acting as a lanosterol 14α-demethylase inhibitor. Azalanstat mesylate has been shown to inhibit cholesterol synthesis in HepG2 cells, human fibroblasts, hamster hepatocytes and hamster liver, by inhibiting the cytochrome P450 enzyme lanosterol 14 alpha-demethylase. When administered orally to hamsters fed regular chow, RS-21607 (50 mg kg day) lowered serum cholesterol in a dose-dependent manner (ED50 = 62 mg kg) in a period of 1 week. It preferentially lowered low density lipoprotein (LDL) cholesterol and apo B relative to high density lipoprotein (HDL) cholesterol and apo A-1.

Pitavastatin (NK-104) is a potent inhibitor of hydroxymethylglutaryl-CoA (HMG-CoA) reductase, effectively inhibiting cholesterol synthesis from acetic acid in HepG2 cells with an IC50 of 5.8 nM. It also induces hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptors and exhibits therapeutic activities such as anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective, and reno-protective effects.

PCSK9-IN-13 is a potent inhibitor of PCSK9, effectively preventing the binding of PCSK9 to low-density lipoprotein (LDL) receptors through its mechanism of action. It exhibits this inhibitory activity with an IC 50 value of 537 nM.