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

ABCA1 inducer 3 (Compound 85) 是一种口服有效的 ABCA1 诱导剂和脂质调节剂。ABCA1 inducer 3 可提高 ABCA1 的表达水平。ABCA1 inducer 3 可上调肝脏中 Abcg5Abcg8mRNA 表达。ABCA1 inducer 3 可促进胆固醇外流。ABCA1 inducer 3 可改善高脂血症。

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ABCA1 inducer 3

ABCA1 inducer 3 Chemical Structure

CAS No. : 2681270-30-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

ABCA1 inducer 3 (10 μM; 24 h) 可在 ABCA1p-LUC HepG2 细胞中强效上调 ABCA1,上调率达 578%,EC50 为 0.15 μM[1]
ABCA1 inducer 3 (2.5-10 μM; 24 h) 可在 RAW264.7 巨噬细胞中诱导 Abca1 mRNA 表达呈中度、剂量依赖性上调[1]
ABCA1 inducer 3 (10 μM; 18 h) 可促进胆固醇从 RAW264.7 巨噬细胞中外排[1]

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

体内研究
(In Vivo)

ABCA1 inducer 3 (50 mg/天;口服;8 周) 对高脂血症金黄地鼠具有保护作用[1]

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.
分子量

551.26

Formula

C18H14BrCl2N3O4S2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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ABCA1 inducer 3
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HY-181520
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