cholesterol

Cholesterol is the primary sterol in mammals, accounting for approximately 20–25% of the plasma membrane structure. It plays a key role in regulating membrane fluidity, permeability, and protein function. As an endogenous agonist of estrogen-related receptor α (ERRα), cholesterol is widely involved in metabolic regulation and serves as a precursor for the synthesis of hormones and bile acids. It is commonly used in experimental models of hyperlipidemia.

7α-Hydroxycholesterol, a cholesterol oxide formed through both enzymatic and non-enzymatic oxidation, can serve as a biomarker for lipid peroxidation.

Rosuvastatin (ZD4522) is an inhibitor of HMG-CoA reductase (HMGCR) (IC50=11 nM), selective and competitive. Rosuvastatin has hypolipidemic and antiatherosclerotic effects.

Digitonin is a natural product of the glycoside family and is a detergent. Digitonin has antitumor activity, binds to cholesterol molecules to increase the permeability of cell membranes, and is active in the cleavage of cell membranes in a wide range of cells.

AY 9944 is a specific cholesterol biosynthesis inhibitor that targets the 7-dehydrocholesterol Δ7-reductase (DHCR7) enzyme (IC50=13 nM). At high doses, AY 9944 also inhibits sterol Δ7-Δ8 isomerase in cultured embryos, leading to the accumulation of cholest-8-en-3β-ol[1][2][3]. Additionally, AY 9944 causes hypocholesterolemia and accumulation of 7DHC.

Mitotane (NCI-C04933) is a derivative of the insecticide DICHLORODIPHENYLDICHLOROETHANE that specifically inhibits cells of the adrenal cortex and their production of hormones. It is used to treat adrenocortical tumors and causes CNS damage, but no bone marrow depression.

7-Ketolithocholic acid (3α-Hydroxy-7-oxo-5β-cholanic acid) is capable of absorption and suppresses the production of endogenous bile acid and the secretion of biliary cholesterol.

Rosuvastatin calcium (ZD4522) , a selective and competitive inhibitor of hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, has antilipidemic activity.

Methyl Cholate is the methyl ester form of bile acid, which is a major bile acid produced by the liver and synthesized from cholesterol.

Cetilistat (ATL-962) is a novel inhibitor of pancreatic lipase being developed by Alizyme for the treatment of obesity and associated co-morbidities, including type 2 diabetes.

Cetaben, a PPARα-independent peroxisome proliferator, is a non-fibrotic lipid-lowering drug that effectively reduces cholesterol and triglyceride concentrations.

Melinamide is an antilipidemic compound with pharmacological properties similar to gemfibrozil. Melinamide reduces elevated serum lipids primarily by lowering the triglyceride-rich very low-density lipoprotein (VLDL) fraction. In Type III hyperlipoproteinemia, where cholesterol elevation arises from intermediate-density lipoproteins (IDL), melinamide can decrease serum cholesterol levels.

U18666A is a cell-permeable drug and is a cholesterol synthesis and transport inhibitor. It inhibits replication of Ebola virus, dengue virus, and human hepatitis C virus.

YM-750 is a potent inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), with an IC50 value of 0.18 μM. ACAT is an enzyme that catalyzes the conversion of cholesterol and long-chain fatty-acyl-coenzyme A into cholesteryl esters.

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.

BIBB 515 is a selective and potent inhibitor of OSC in vivo with an ED50 value of 0.2-0.5 and 0.36-33.3 mg/kg in rats and mice, respectively. 2, 3-Oxidosqualene cyclase (OSC) is an important enzyme in the biosynthesis of animal, plant, and fungal sterols.

SBC-110736 is an inhibitor of proprotein convertase subtilisin kexin type 9 (PCSK9).

Lanosterol (3β-Hydroxy-8,24-lanostadiene) is a tetracyclic triterpenoid which is the compound from which all steroids are derived.

1. Pseudoprotodioscin has moderate cytotoxicity.

3-chloro-5-hydroxy Benzoic Acid (3-chloro-5-hydroxy BA) is an agonist of GPR81 (EC50 : 16 μM)

glycohyodeoxycholic acid is a major metabolite of the secondary bile acid hyodeoxycholic acid in humans.

Pentacosanoic acid, belongs to the class of organic compounds known as very long-chain fatty acids.

Soticlestat (OV935) is a potent, selective and orally active cholesterol 24-hydroxylase (CYP46A1) inhibitor. It has the potential for epilepsy syndromes research.

Zeaxanthin is a dietary carotenoid that accumulates in the retina (particularly the macula) and has antioxidant activity that may improve obesity, prevent age-related macular degeneration, and protect against nonalcoholic steatohepatitis.