cholesterol transport

Nicanartine is a cholesterol inhibitor that is used to treat cardiovascular disease and can be used to study atherosclerosis.

cholesterol-absorption inhibitor Intermediate 2 is a potent and orally active cholesterol absorption inhibitor that reduces blood cholesterol levels.

GW6340 is a selective LXR agonist with potential anticancer activity that promotes macrophage reverse cholesterol transport (mRCT) and can be used to study atherosclerosis.

Dehydroabiethylamine (NSC-2955) is an inducer of hepatic CYP2B activity. Dehydroabiethylamine inhibits pyruvate dehydrogenase kinases (PDKs) and intracellular cholesterol transport with anti-tumor activity.

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.

Diethylumbelliferyl phosphate (DEUP) is a potent and selective inhibitor of cholesterol esterase that does not inhibit protein kinase A activity in vitro. It disrupts steroidogenesis by blocking cholesterol transport to mitochondria in steroidogenic cells, with an IC50 of 11.6 μM. This compound may also limit the absorption of dietary cholesterol.

TSPO ligand-1 has affinity for peripheral and central benzodiazepine receptors.TSPO ligand-1 is an AUTAC4-binding protein in the transmembrane domain of the outer mitochondrial membrane, which induces mitochondrial autophagy and promotes intracellular mitochondrial regeneration.TSPO ligand-1 is involved in intracellular cholesterol transport, and can be used as a biomarker for brain injury and neurodegeneration. TSPO ligand-1 is involved in intracellular cholesterol transport and can be used as a biomarker for brain damage and neurodegeneration.

Dehydroergosterol (DHE) is a naturally occurring fluorescent sterol analog that is a compound for real-time detection elaboration of the sterol environment and intracellular sterol transport in organisms. Dehydroergosterol is a cholesterol mimetic that binds to cholesterol-binding proteins and can be used for real-time imaging of living cells. Dehydroergosterol is a cholesterol mimetic that binds to cholesterol-binding proteins and can be used for real-time imaging of living cells.

Sch 58053 is an analog of Ezetimibe and a selective inhibitor of lymphatic cholesterol transport in the intestine.

1-Palmitoyl-d9-2-palmitoyl-sn-glycero-3-PE serves as an internal standard for the quantification of 1,2-dipalmitoyl-sn-glycero-3-PE (1,2-DPPE) using GC- or LC-MS. 1,2-DPPE, a prevalent PE (phospholipid), contains C16:0 fatty acids at the sn-1 and sn-2 positions and is essential in the inner plasma membrane leaflet. This compound forms a condensed lipid monolayer with cholesterol through tight hydrogen bonding between 1,2-DPPE headgroups, enhancing membrane fluidity to support transport and signaling.

Bile acids are essential for solubilization and transport of dietary lipids, are the major products of cholesterol catabolism, and are physiological ligands for farnesoid X receptor (FXR), a nuclear receptor that regulates genes involved in lipid metabolism.1They are also inherently cytotoxic, as physiological imbalance contributes to increased oxidative stress.2,3Bile acid-controlled signaling pathways are promising novel targets to treat such metabolic diseases as obesity, type II diabetes, hyperlipidemia, and atherosclerosis.Guggulsterone, derived from resin of the guggul tree, is a competitive antagonist of FXR bothin vitroandin vivo.4Thecisstereoisomer of guggulsterone, (E)-guggulsterone, decreases chenodeoxycholic acid (CDCA)-induced FXR activation with an IC50value of 15 μM.5,6By inhibiting CDCA-induced transactivation of FXR, guggulsterone lowers low-density lipoprotein cholesterol and triglyceride levels in rodents fed a high cholesterol diet.4 1.Makishima, M., Okamoto, A.Y., Repa, J.J., et al.Identification of a nuclear receptor for bile acidsScience2841362-1365(1999) 2.Barbier, O., Torra, I.P., Sirvent, A., et al.FXR induces the UGT2B4 enzyme in hepatocytes: A potential mechanism of negative feedback control of FXR activityGastroenterology1241926-1940(2003) 3.Tan, K.P., Yang, M., and Ito, S.Activation of nuclear factor (erythroid-2 like) factor 2 by toxic bile acids provokes adaptive defense responses to enhance cell survival at the emergence of oxidative stressMol. Pharmacol.72(5)1380-1390(2007) 4.Urizar, N.L., Liverman, A.B., Dodds, D.T., et al.A natural product that lowers cholesterol as an anatagonist ligand for FXRScience296(5573)1703-1706(2002) 5.Cui, J., Huang, L., Zhao, A., et al.Guggulsterone is a farnesoid X receptor antagonist in coactivator association assays but acts to enhance transcription of bile salt export pumpThe Journal of Biological Chemisty278(12)10214-10220(2003) 6.Wu, J., Xia, C., Meier, J., et al.The hypolipidemic natural product guggulsterone acts as an antagonist of the bile acid receptorMolecular Endocrinology16(7)1590-1597(2002)