cholesterol synthesis

TASIN-30 is an EBP inhibitor with EC50 values of 0.097 μM for EBP competition and 50 μM for DHCR7 competition, TASIN-30 is utilized in cholesterol biosynthesis and metabolic research to dissect sterol pathway regulation, evaluate enzyme selectivity, and explore therapeutic strategies targeting dysregulated lipid metabolism in disease models.

Simvastatin (MK 733) is an HMG-CoA reductase inhibitor (Ki=0.2 nM) with oral activity. Simvastatin has hypolipidemic activity, inhibits hepatic production of cholesterol, and is also used for the prevention of cardiovascular disease.

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.

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.

Lathosterol, a molecule akin to cholesterol, serves as a biomarker for the body's total cholesterol synthesis, as indicated by its serum concentration.

Azalanstat (RS 21607) is an orally available selective mammalian lanosterol 14-alpha-demethylase inhibitor with hypocholesterolemic activity that inhibits cholesterol synthesis in HepG2 cells, human fibroblasts, hamster hepatocytes, and hamster livers through inhibition of the cytochrome P450 enzyme, lanosterol 14 alpha demethylase.

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.

Cholestyramine (Cholestyramine resin), a bile acid-binding resin, inhibits intestinal bile acid absorption which results in the increasing bile acid synthesis from cholesterol.

Gemfibrozil (CI-719) interacts with peroxisome proliferator-activated receptors (PPARalpha) resulting in PPARalpha-mediated stimulation of fatty acid oxidation and an increase in lipoprotein lipase (LPL) synthesis. Gemfibrozil is a fibric acid derivative with hypolipidemic effects. This enhances triglyceride-rich lipoprotein clearance and reduces the expression of apolipoprotein C-III (apoC-III). The reduction in hepatic production of apoC-III result in the subsequent reduction of serum levels of very-low-density-lipoprotein cholesterol (VLDL-C). In addition, gemfibrozil-mediated PPARalpha stimulation of apoA-I and apoA-II expression results in an increase in high-density lipoprotein cholesterol (HDL-C).

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.

Butanoic acid is an endogenous human metabolite, an endogenous histone deacetylase (HDAC) inhibitor. The IC50 of HDAC3, HDAC4 and HDAC1 were 2.4 mM, 4.5 mM and 5.3 mM, respectively. 3-Hydroxybutyric acid has the effects of energy metabolism, neuroprotection, anti-inflammatory, and improvement of insulin resistance.

D-Pantothenic acid (vitamin B5) is an essential micronutrient and a precursor to coenzyme A. D-Pantothenic acid participates in the metabolism of the three major nutrients—fat, carbohydrates, and protein—within the body. D-Pantothenic acid also plays a crucial role in skin barrier repair, maintaining hematopoietic function, and synthesizing adrenal hormones.

Cholesteryl Hemisuccinate (Cholesterol hydrogen succinate) is a highly soluble cholesterol analogue often used in polar solutions for its hepatoprotective, anticancer and tumour growth inhibiting properties. Cholesteryl Hemisuccinate inhibits the hepatotoxicity of acetaminophen and prevents AAP-induced apoptosis and necrosis in hepatocytes. Cholesteryl Hemisuccinate inhibits DNA polymerase and DNA topoisomerase, thereby inhibiting DNA replication and repair as well as cell division.

Uridine 5'-monophosphate disodium salt (Disodium UMP) has been used to study the effect of pyrimidine synthesis inhibitor, 5-azacytidine, on cholesterol and lipid metabolism. It has been used to study the effect of nucleotides on growth of specific intestinal bacteria.

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).

Farnesyl Pyrophosphate ammonium salt is an isomer of (E,E)-Farnesyl Pyrophosphate ammonium salt, which is a key metabolic intermediate in the mevalonate (MVA) pathway and an agonist of TRPM2, and is involved in cholesterol synthesis, ubiquinone synthesis, protein farnesylation and other physiological processes.

7α-Hydroxy-4-cholesten-3-one is an intermediate in bile acid synthesis from cholesterol, a PXR agonist, and a biomarker for bile acid loss and diseases related to defective bile acid biosynthesis. It is also the physiological substrate for [CYP8B1].

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.

Mevalonic acid lithium salt (MVA lithium salt) is a precursor of the mevalonic acid pathway, an initiator of cell growth, a key substance in cholesterol synthesis, and stimulates DNA synthesis, morphology transformation, and cell cycling in human lymphocytes from peripheral blood.

CAP2 (Cholesterol-amino-phosphate 2) hydrochloride is a lipid within the cholesterol amino phosphate (CAP) family. It is employed in the synthesis of lipid nanoparticles (LNP) for the delivery of mRNA and other efficacious payloads.

DSP-0390 is an oral inhibitor of emopamil binding protein (EBP). It effectively suppresses the EBP enzyme, which is involved in a critical late-stage step of cholesterol biosynthesis. By inhibiting the synthesis of new cholesterol, DSP-0390 selectively induces cytotoxicity in rapidly proliferating GBM cells. In human GBM xenograft models, DSP-0390 has demonstrated significant antitumor activity.

Cholesteryl n-Valerate is a cholesterol ester widely used in biochemical experiments and drug synthesis research.

Cholesteryl Laurate is a cholesterol ester widely used in biochemical experiments and drug synthesis research.

Squalene synthase-IN-2 (compound isomer A-(1S, 3R)-14i) is an orally active inhibitor of squalene synthase, with IC50 values of 3.4 nM for squalene synthase and 99 nM for cholesterol synthesis enzymes. Squalene synthase-IN-2 effectively reduces plasma cholesterol and triglycerides.