IMB-808 is an effective partial dual agonist of liver X receptor α and β (LXRα/β) that promotes the expression of genes related to reverse cholesterol transport (including ABCA1 and ABCG1).
AZ-2 is an inducer of ABCA1 and apoE. It enhances ABCA1 activity and decreases P2X7 receptor activity. AZ-2 activates endogenous LXR signaling but shows no direct LXRα or LXRβ agonist activity.
AZ-1 is an inducer of ABCA1 and apoE. It enhances ABCA1 activity and decreases P2X7 receptor activity. AZ-1 activates endogenous LXR signaling but shows no direct LXRα or LXRβ agonist activity.
C2 L-threo Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. It stimulates cholesterol efflux in CHO cells expressing the human ABCA1 receptor when used at a concentration of 10 μM, however, this efflux is 50% less than that stimulated by C2 ceramide . C2 L-threo Ceramide inhibits IL-4 production by 17% in EL4 T cells stimulated with phorbol 12-myristate 13-acetate when used at a concentration of 10 μM. It also induces cell cycle arrest in the G0/G1 phase and a 7-fold increase in sphingosine accumulation as well as inhibits growth of HL-60 leukemia cells.
E17110 is an LXRβ agonist. E17110 exhibited a significant activation effect on LXRβ (EC50: 0.72 μmol/L). E17110 also increased the expression of ABCA1 and ABCG1 in RAW264.7 macrophages. E17110 significantly decreased cellular lipid accumulation and promoted cholesterol efflux in RAW264.7 macrophages.
Cajanin has potential hypolipidemic effects,possibly via up-regulating the ABCA1 protein expression,subsequently resulting in increased macrophage cholesterol efflux and RCT, it can significantly improve basal glucose uptake in HepG2 cells, its improving effect is concentration dependent, it exhibits effects stronger than that of rosiglitazone, which has been used as an antidiabetic drug.
Tanshindiol C protects macrophages from oxLDL induced foam cell formation via activation of Prdx1/ABCA1 signaling and that Prdx1 may be a novel target for therapeutic intervention of atherosclerosis.It possesses a unique anti-cancer activity whose mechani