cholesterol transport

Nicanartine是一种胆固醇抑制剂，可用于治疗心血管疾病，可用于研究动脉粥样硬化。

cholesterol-absorption inhibitor Intermediate 2 是一种有效且具有口服活性的胆固醇吸收抑制剂，可降低血液中胆固醇含量。

U18666A 是一种细胞渗透性药物，是一种胆固醇合成和转运抑制剂，抑制埃博拉病毒，登革热病毒和人类丙型肝炎病毒的复制。

GW6340 是一种选择性 LXR 激动剂，具有潜在的抗癌活性，可促进巨噬细胞反向胆固醇转运 (mRCT)，可用于研究动脉粥样硬化。

Dehydroabiethylamine (NSC-2955) 是肝脏 CYP2B 活性的诱导剂。 Dehydroabiethylamine 抑制丙酮酸脱氢酶激酶 (PDK) 和细胞内胆固醇转运，具有抗肿瘤活性。

Diethylumbelliferyl phosphate (DEUP) 作为一种选择性的强效胆固醇酯酶抑制剂，能防止胆固醇被运输到类固醇生成细胞的线粒体，从而有效抑制类固醇的生成。在体外环境中，DEUP不会对蛋白激酶活性A造成抑制。此外，其IC50值为 11.6 μM，表明该化合物能够在一定程度上阻止膳食胆固醇的吸收。

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)

Dehydroergosterol (DHE) 是一种天然存在的荧光甾醇类似物，是实时探测 阐明生物体中甾醇环境和细胞内甾醇运输的化合物。Dehydroergosterol 是一种胆固醇模拟物，可胆固醇结合蛋白结合，可用于活细胞实时成像。

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

TSPO ligand-1 对外周和中枢苯二氮卓受体有亲和力。TSPO ligand-1 是一种线粒体外膜跨膜结构域上与 AUTAC4 结合的蛋白，可诱导线粒体自噬 (autophagy) 促进胞内线粒体更新。TSPO ligand-1 参与胆固醇在胞内的转运，可作为脑损伤和神经变性的生物标志物。

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.