ABCA1

Probucol (DH-581), an anti-hyperlipidemic drug, can lower the level of cholesterol in the bloodstream by increasing the LDL catabolic rate.

Isosilybin A is a partial PPARγ agonist, it significantly induced ABCA1 protein expression, it inhibited both monophenolase (IC50=1.7-7.6μM) and diphenolase (IC50=12.1-44.9μM) of tyrosinase. Isosilybin A shows anti-angiogenic efficacy, it has anti-prostate cancer (PCA) activity that is mediated via cell cycle arrest and apoptosis induction.

ABCA1 inducer 1, a non-lipid inducer of ABCA1, enhances ABCA1 expression in E3 4FAD mice expressing human APOE 3 4, augments the lipidation of apolipoprotein (APOE), and reverses various Alzheimer's disease (AD) phenotypes without increasing triglycerides.

Campesterol ((24R)-5-Ergosten-3β-ol) is a plant sterol with cholesterol lowering and anticarcinogenic effects, it and other plant sterols often decrease LDL cholesterol levels overall. Campesterol has anti-inflammatory effect, it inhibits several pro-inflammatory and matrix degradation mediators typically involved in osteoarthritis- induced cartilage degradation, also sometimes used to treat some specific prostate conditions.

IMM-H007 is a novel lipid-lowering agent, increasing abca1 protein expression

Elodeoidileon A acts as an agonist to RXRα, exhibiting a dissociation constant (Kd) of 5.85 μM when interacting with the RXRα-LBD protein. It enhances the expression of ATP Binding Cassette Transporter A1 (ABCA1). Furthermore, Elodeoidileon A holds potential in Alzheimer's disease research.

E17241 functions as an inducer of ABCA1 gene expression, effectively increasing its expression with an EC50 value of 280 nM. It also acts as an agonist for peroxisome proliferator-activated receptors (PPARs), inducing PPAR-mediated gene expression in HepG2 cells expressing PPARγ, PPARα, or PPARδ, with respective EC50 values of 290, 3,900, and 879 nM. In RAW 264.7 macrophage cells, E17241 enhances ACBA1 protein levels, although this effect is absent when siRNA targeting PKCζ mRNA is present. Treatment with E17241 (0.4, 2, or 10 µM) increases cholesterol efflux in RAW 264.7 cells. In an atherosclerosis model using ApoE- - mice administered with a dose of 25 mg kg, E17241 reduces levels of plasma cholesterol, alanine transaminase (ALT), aspartate transaminase (AST), and liver cholesterol and triglycerides, and also decreases the area of aortic lesions. Additionally, daily administration of E17241 (50 mg kg) lowers blood glucose levels and body weight in KKAy diabetic mice on a high-fat, high-glucose (HFHG) diet.

PFM046 is an antagonist of the liver X receptor (LXR), effectively inhibiting the activation of LXRα and LXRβ, with IC50 values of 2.04 μM and 1.58 μM respectively. It reduces the expression of SCD1 and FASN while increasing ABCA1 expression, and demonstrates antitumor activity in mouse models.

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.

IMB-808 is an LXRα β dual agonist that promotes ABCA1 expression and cholesterol efflux without inducing lipidogenesis in HepG2 cells. IMB-808 can be used in atherosclerosis research.

GSK3987 is an LXR ligand. GSK3987 recruits the steroid receptor coactivator-1 to human LXRalpha and LXRbeta with EC50s of 40 nM.

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.

DMHCA is a selective LXR agonist with anti-inflammatory activity, which induces ABCA1 expression and upregulates FASN and SREBP-1alpha gene expression.

1. Pseudoprotodioscin has moderate cytotoxicity.

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.

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.

Falcarindiol, an orally active polyacetylenic oxylipin, activates PPARγ, enhancing ABCA1 expression [a cholesterol transporter], and induces apoptosis and autophagy, exhibiting anti-inflammatory, antifungal, anticancer, and antidiabetic properties.

Erythrodiol, an olive oil component, promotes Cholesterol efflux (ChE) by selectively inhibiting the degradation of ABCA1 protein.

st-Ht31, a cell-permeable stearated peptide derived from the amphipathic helix domain of A-kinase anchoring proteins (AKAPs), effectively binds protein kinase A (PKA), impacting PKA's cellular interactions without altering its activity. Specifically, at a 50 µM concentration, it reduces PKA's membrane anchoring in BHK-21 fibroblast reporter assays. Moreover, st-Ht31 at concentrations of 1 and 3 µM decreases both capacitance and hyperactivation in mouse sperm, thereby inhibiting in vitro fertilization. Additionally, at 50 µM, this compound facilitates cholesterol export in BHK-21 cells and RAW 264.7 macrophages expressing ATP-binding cassette transporter 1 (ABCA1), showcasing its multifaceted cellular impacts.

C2 Dihydro Ceramide (d18:0 2:0) (C2 Dihydroceramide) is a short-chain ceramide that is a precursor of ceramide synthesis and stimulates ABCA1-mediated cholesterol efflux.

CS-6253TFA is the TFA salt form of CS-6253. This compound serves as an activator for the ATP Binding Cassette 1 (ABCA1). It effectively modulates the amyloid-beta Aβ42 40 ratio and influences the metabolism of lipoproteins in plasma. Additionally, CS-6253TFA facilitates the production of cholesterol-rich high-density lipoprotein (HDL) particles and induces the release of microparticles.

CS-6253 is an agonist of ATP Binding Cassette 1 (ABCA 1). It modulates the amyloid beta Aβ42 40 ratio, influencing lipoprotein metabolism in the plasma. Additionally, CS-6253 promotes the production of cholesterol-rich high-density lipoprotein (HDL) particles and induces the release of microparticles.

E1231 is an activator of SIRT1 . E1231 protects from experimental atherosclerosis and lowers plasma cholesterol and triglycerides by enhancing ABCA1 expression.

OSBPL7-IN-1 is an orally active inhibitor of oxysterol binding protein like 7 (OSBPL7) that promotes an increase of ABCA1 at the plasma membrane without affecting mRNA expression[1].