1. Membrane Transporter/Ion Channel
  2. ATP-binding cassette (ABC) transporters
  3. ABCA1 inducer 3

ABCA1 inducer 3 (Compound 85) is an orally active ABCA1 inducer and lipid-modulating agent. ABCA1 inducer 3 increases ABCA1 expression. ABCA1 inducer 3 upregulates hepatic Abcg5 and Abcg8 mRNA expression. ABCA1 inducer 3 promotes cholesterol efflux. ABCA1 inducer 3 improves hyperlipidemia.

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ABCA1 inducer 3

ABCA1 inducer 3 Chemical Structure

CAS No. : 2681270-30-2

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Description

ABCA1 inducer 3 (Compound 85) is an orally active ABCA1 inducer and lipid-modulating agent. ABCA1 inducer 3 increases ABCA1 expression. ABCA1 inducer 3 upregulates hepatic Abcg5 and Abcg8 mRNA expression. ABCA1 inducer 3 promotes cholesterol efflux. ABCA1 inducer 3 improves hyperlipidemia[1].

IC50 & Target[1]

ABCA1

 

In Vitro

ABCA1 inducer 3 (10 μM; 24 h) potently upregulates ABCA1 in ABCA1p-LUC HepG2 cells, achieving a 578% upregulation rate and an EC50 of 0.15 μM[1].
ABCA1 inducer 3 (2.5-10 μM; 24 h) induces moderate, dose-dependent upregulation of Abca1 mRNA expression in RAW264.7 macrophages[1].
ABCA1 inducer 3 (10 μM; 18 h co-treated with 22-NBD cholesterol, 6 h with ApoA-I) promotes cholesterol efflux from RAW264.7 macrophages, as shown by reduced intracellular 22-NBD cholesterol fluorescence[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

ABCA1 inducer 3 (Compound 85) (50 mg/day; p.o.; 8 weeks) reduces plasma TG and TC levels by 33% and 22% respectively, decreases hepatic lipid accumulation by over 40%, and upregulates hepatic cholesterol transporter expression in hyperlipidemic golden Syrian hamsters without hepatic toxicity[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Golden Syrian hamsters[1]
Dosage: 50 mg/day
Administration: p.o.; daily; 8 weeks
Result: Reduced plasma triglyceride (TG) levels by 33% and plasma total cholesterol (TC) levels by 22% compared to the high-fat diet model group, with no significant impact on low-density lipoprotein cholesterol (LDL-C) or high-density lipoprotein cholesterol (HDL-C) levels.
Decreased Oil Red O-positive lipid areas by over 40% compared to the model group.
Upregulated hepatic Abca1 mRNA expression to approximately 1.9-fold that of the normal control group, and restored ABCA1 protein expression to levels significantly higher than the model group.
Significantly upregulated hepatic Abcg5 and Abcg8 mRNA expression.
Showed no significant effects on aspartate aminotransferase (AST), alanine aminotransferase (ALT), plasma glucose, bile acids, or direct bilirubin levels versus the model group.
Molecular Weight

551.26

Formula

C18H14BrCl2N3O4S2

CAS No.
SMILES

O=C(C1=CC(Br)=C2N=C(SC2=C1)N3CCN(CC3)S(=O)(C4=CC=CC(Cl)=C4Cl)=O)O

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ABCA1 inducer 3
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HY-181520
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