2. Metabolic Enzyme/Protease NF-κB Immunology/Inflammation Apoptosis
  3. Fatty Acid Synthase (FASN) Stearoyl-CoA Desaturase (SCD) Reactive Oxygen Species (ROS) Interleukin Related TNF Receptor SOD LDLR Glutathione Peroxidase
  4. FASN/SCD-IN-1

FASN/SCD-IN-1 是 Silybin (HY-N0779A) 衍生物，是脂肪酸合酶 (FASN)/硬脂酰辅酶 A 去饱和酶 (SCD) 的口服活性抑制剂。FASN/SCD-IN-1 在体外实验中表现出抑制脂质沉积、降低 FASN 和 SCD 的转录水平、抗氧化、抗炎和抗纤维化的活性。FASN/SCD-IN-1 在急性肝损伤大鼠模型中，表现出显著的保肝作用。FASN/SCD-IN-1 在骨髓增生性脂肪性肝炎 (MASH) 小鼠模型中，改善了 MASH 肝脏的病理特征，包括脂肪变性、炎症和纤维化。FASN/SCD-IN-1 可用于研究 MASH。

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FASN/SCD-IN-1

FASN/SCD-IN-1 Chemical Structure

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FASN/SCD-IN-1 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FASN/SCD-IN-1 is a Silybin (HY-N0779A) derivative, an orally active inhibitor of Fatty Acid Synthase (FASN)/Stearoyl-CoA Desaturase (SCD). FASN/SCD-IN-1 has shown in vitro activity in inhibiting lipid deposition, reducing FASN and SCD transcriptional levels, and exhibiting antioxidant, anti-inflammatory, and anti-fibrotic activities. FASN/SCD-IN-1 has demonstrated significant hepatoprotective effects in a rat model of acute liver injury. FASN/SCD-IN-1 ameliorates the pathological features of MASH liver, including steatosis, inflammation, and fibrosis in a mouse model of myeloproliferative steatohepatitis (MASH). FASN/SCD-IN-1 can be used to study MASH[1].

体外研究
(In Vitro)

FASN/SCD-IN-1 (Compound A2) (100-200 μM，20-30 分钟) 对 DPPH 和 O2•– 具有清除作用，清除率分别为 92.9% 和 82.9%，IC50 分别为 33.4 和 28.1 μM。在脂质过氧化抑制能力 (LPIC) 测定中，LPIC 的抑制率为 67.0%，IC50 为 41.7 μM[1]。
FASN/SCD-IN-1 (10-40 μM，24 小时) 在 Palmitic acid (HY-N0830)/Oleic acid (HY-N1446) (PO) 刺激的 LO2 细胞和小鼠原代肝细胞中可降低甘油三酯 (TG) 水平，抑制脂质积累，在 PO 刺激的 LO2 细胞中降低脂肪酸合酶 (FASN) 和硬脂酰辅酶 A 去饱和酶 (SCD) 的转录水平，在 PO 刺激的小鼠原代肝细胞中降低 ACACA (编码乙酰辅酶A羧化酶) 和 FASN 的表达[1]。
FASN/SCD-IN-1 (1-10 μM, 24 小时) 可降低 Carbon tetrachloride (CCl4) (HY-Y0298) 刺激的 LO2 细胞和小鼠原代肝细胞中过量的 ROS 以及 IL-6、TNF-α mRNA 水平[1]。
FASN/SCD-IN-1 (10-40 μM, 48 小时) 可抑制 TGF-β 刺激的 LX2 细胞中的胶原蛋白 I 和纤维连接蛋白(FN) 水平[1]。

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

FASN/SCD-IN-1 相关抗体:

Western Blot AnalysisTGF-β-stimulated LX2 cells

Cell Line: TGF-β-stimulated LX2 cells
Concentration: 10 μM, 20 μM, 40 μM
Incubation Time: 48 h
Result: Suppressed collagen I and FN levels.
体内研究
(In Vivo)

FASN/SCD-IN-1 (Compound A2) (100 mg/kg，灌胃，每日一次，7 天) 在 CCl4 诱发的急性肝损伤大鼠模型中可通过恢复肝功能、减少脂质蓄积和改善氧化应激，保护大鼠免受急性肝损伤，从而减轻肝功能损伤[1]。
FASN/SCD-IN-1 (150 mg/kg，口服，每日一次，4 周) 在 HFD + CCl4 诱发的 MASH 小鼠中可减少脂肪变性，减轻氧化应激、炎症反应和肝纤维化，因此可显著改善 MASH 小鼠的进展[1]。

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

Animal Model: CCl4 (1 mg/kg, i.p.)-induced acute liver injury SD rat (male, 6 weeks) model[1]
Dosage: 100 mg/kg
Administration: i.g. once a day, 7 days
Result: Alleviated typical features of fatty liver disease, such as partial yellowing, darkening of the liver margins, white fat granules, and a rough surface.
Reduced the hepatopancreatic somatic index (HSI) and liver-to-body weight ratio.
Reduced serum AST, ALT, and LDH levels.
Reduced liver vacuoles, acute fat deposition, elevation of the MDA level and and restored SOD activity.
Animal Model: HFD + CCl4 (0.2 mg/kg, i.p., once a week)-induced MASH C57BL/6 mice (male, 6 weeks) model[1]
Dosage: 150 mg/kg
Administration: p.o., once a day, 4 weeks
Result: Protected body weight and counteracts CCl4 toxicity.
Reduced hepatopancreatic somatic index (HSI) and alleviates liver swelling.
Alleviated liver damage and reverses CCl4-induced liver enlargement, pale color, and mottled texture.
Reduced serum AST and ALT levels.
Improved liver structural distortion and reverses CCl4-induced hepatocellular ballooning, inflammation, and steatosis.
Ameliorated the dyslipidemia, reduced the elevated serum TG, cholesterol (CHO), and low-density lipoprotein cholesterol (LDL-c) levels and increased the lowered high-density lipoprotein cholesterol (HDL-c) levels.
Reduced the hepatic TG and CHO levels.
Restored the decreased liver GSH level and decrease the elevated MDA level, restore the decreased levels of both SOD and GSH-Px.
Reduced IL-6 and TNF-α levels, reduced collagen deposition, levels of α-SMA and collagen I in the liver tissue.
分子量

498.50

Formula

C25H22O9S
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

FASN/SCD-IN-1 相关分类

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  • 稀释计算器

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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:

FASN/SCD-IN-1Fatty Acid Synthase (FASN)Stearoyl-CoA Desaturase (SCD)Reactive Oxygen Species (ROS)Interleukin RelatedTNF ReceptorSODLDLRGlutathione PeroxidaseILTumor Necrosis Factor ReceptorTNFRSuperoxide DismutaseLow-density lipoprotein receptorInhibitorLO2 cellsprimary mouse hepatocytesLX2 cellsacute liver injurySD ratMASHinhibitorinhibit

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