2. Metabolic Enzyme/Protease
  3. ATP Citrate Lyase
  4. ACLY-IN-3

ACLY-IN-3 是一种 ATP-柠檬酸裂解酶 (ACLY) 抑制剂，其 IC50 为 0.036 μM，靶标 Kd 为 0.54 μM。ACLY-IN-3 与 ACLY 的变构结合位点相互作用以抑制其活性。ACLY-IN-3 展现出优异的降脂效果并缓解肝脏炎症与肝纤维化。ACLY-IN-3 可用于代谢功能障碍相关脂肪性肝炎的研究。

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ACLY-IN-3

ACLY-IN-3 Chemical Structure

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ACLY-IN-3 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ACLY-IN-3 is an ATP-citrate lyase (ACLY) inhibitor with an IC50 of 0.036 μM and a target Kd of 0.54 μM. ACLY-IN-3 interacts with the allosteric binding site of ACLY to inhibit its activity. ACLY-IN-3 exhibits excellent lipid-lowering effects and alleviates hepatic inflammation and liver fibrosis. ACLY-IN-3 can be used for the research of metabolic dysfunction-associated steatohepatitis[1].

体外研究
(In Vitro)

ACLY-IN-3 (Compound B1) (50 μM; 4 h) 可通过依赖 ACLY 的机制有效减少油酸诱导的 shNC HepG2 细胞脂质蓄积，且在最高 50 μM 的浓度下未观察到细胞毒性[1]。
ACLY-IN-3 (50 μM; 24 h) 通过依赖 ACLY 的机制抑制油酸诱导的 shNC HepG2 细胞中脂肪生成基因 FASN、ACC1 和 SREBP-1c 的表达[1]。

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

ACLY-IN-3 相关抗体:

Real Time qPCR[1]

Cell Line: oleic acid (OA)-induced shNC and shACLY HepG2 cells
Concentration: 50 μM
Incubation Time: 24 h (with 1 mM OA)
Result: In OA-induced shNC HepG2 cells, significantly downregulated mRNA expression of fatty acid synthase (FASN), acetyl-CoA carboxylase 1 (ACC1), and sterol regulatory element-binding protein 1c (SREBP-1c).
Abolished effect in shACLY HepG2 cells.
药代动力学
(Parmacokinetics)
Species Dose Route Cmax T1/2 AUCinf CL Bioavailability
Mice[1] 10 mg/kg i.p. 1995 ng/mL 8.23 h 2154 ng·h/mL 87 mL/min/kg 124 %
体内研究
(In Vivo)

ACLY-IN-3 (Compound B1) (10-30 mg/kg；腹腔注射；每日给药；持续 8 周) 可显著降低高脂饮食诱导的小鼠 MASH 模型的体重、改善肝脏脂肪变性，并缓解全身胰岛素抵抗、氧化应激、炎症及纤维化[1]。

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

Animal Model: C57BL/6J (male, 8 weeks old, 18-20 g, high-fat diet-induced MASH)[1]
Dosage: 10 mg/kg; 30 mg/kg
Administration: i.p.; daily; 8 weeks
Result: Reduced average body weight from 49.5 g (HFD group) to 41.7 g (10 mg/kg) and 35.7 g (30 mg/kg).
Significantly lowered elevated serum triglycerides, total cholesterol, alanine aminotransferase, aspartate aminotransferase, and low-density lipoprotein cholesterol, while restoring reduced serum high-density lipoprotein cholesterol to near control levels.
Significantly reduced liver weight, hepatic triglycerides, and hepatic total cholesterol compared to the HFD group.
Achieved near-complete reversal of hepatic lipid accumulation (Oil Red O staining).
Significantly downregulated hepatic mRNA expression of lipogenic markers (FASN, LXR, SREBP-1c, HMGCR, ACC1) and fatty acid uptake marker CD36, while upregulating fatty acid oxidation markers (PPARα, CPT1, PPARγ) and lipid metabolism regulator AMPKα1; confirmed corresponding protein expression changes for FASN, ACC1, and PPARα.
Improved glucose tolerance (reduced OGTT AUC) and insulin sensitivity (reduced ITT AUC) compared to the HFD group.
Significantly reduced hepatic malondialdehyde levels (oxidative stress marker), downregulated mRNA expression of inflammatory markers (CD68, TNF-α, NLRP3, ASC) and pro-fibrotic marker α-SMA, and reduced collagen deposition (Sirius Red staining) in liver tissue.
Restored normal hepatocellular morphology (H&E staining) with no detectable pathological changes in heart, spleen, lung, or kidney tissue.
分子量

284.26

Formula

C16H12O5
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

ACLY-IN-3 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ACLY-IN-3ATP Citrate LyaseACLYATP-citrate lyaseinsulin resistanceFASNHepG2 cellsmetabolic dysfunction-associated steatohepatitisSREBP-1coxidative stressACC1hepatic steatosisInhibitorinhibitorinhibit

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