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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- CAS No.: 2681270-30-2
- Formule: C18H14BrCl2N3O4S2
- Masse moléculaire:551.26
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
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. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Golden Syrian hamsters[1]
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Dosage:50 mg/day
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Administration:p.o.; daily; 8 weeks
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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.
Chemical Information
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CAS No. 2681270-30-2
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Masse moléculaire 551.26
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Formule C18H14BrCl2N3O4S2
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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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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RT-PCR
Reverse transcription technology uses RNA as a template to synthesize DNA. RT-PCR is simple, specific and sensitive, and can be used to detect gene expression levels and expression differences in cells; detect RNA virus content; clone cDNA sequences of specific genes.
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Real Time qPCR (Q-PCR)
Real-time quantitative PCR (qPCR) quantifies an amplifiable nucleic-acid target by monitoring fluorescence during PCR cycling rather than measuring product only after amplification. The increase in fluorescence tracks accumulation of PCR product, and the quantification cycle (Cq; historically also Ct/CP) is related to the initial amount of target: samples containing more starting target generally reach the defined fluorescence threshold in fewer cycles.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)