FASN/SCD-IN-1
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.
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- CAS 番号: 3063509-61-2
- 分子式: C25H22O9S
- 分子量:498.50
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
FASN/SCD-IN-1 (Compound A2) (100-200 μM, 20-30 min) shows scavenging ability for DPPH and O2•–, with scavenging rates of 92.9% and 82.9% respectively, with IC50s of 33.4, 28.1 μM, in terms of lipid peroxidation inhibition capacity (LPIC) assay, the inhibition rate of LPIC is 67.0%, with an IC50 of 41.7 μM[1].
FASN/SCD-IN-1 (10-40 μM, 24 h) reduces triglyceride (TG) levels and inhibits lipid accumulation in Palmitic acid (HY-N0830)/Oleic acid (HY-N1446) (PO)-stimulated LO2 cells and primary mouse hepatocytes, decreases fatty acid synthase (FASN) and stearoyl-CoA desaturase (SCD) transcript levels in PO-stimulated LO2 cells, decreases ACACA (encoding acetyl-CoA carboxylase) and FASN in PO-stimulated primary mouse hepatocytes[1].
FASN/SCD-IN-1 (1-10 μM, 24 h) reduces the excessive ROS and IL-6, TNF-α mRNA levels in Carbon tetrachloride CCl4 (HY-Y0298)-stimulated LO2 cells and primary mouse hepatocytes[1].
FASN/SCD-IN-1 (10-40 μM, 48 h) suppresses collagen I and fibronectin (FN) levels in TGF-β-stimulated LX2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:TGF-β-stimulated LX2 cells
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Concentration:10 μM, 20 μM, 40 μM
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Incubation Time:48 h
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Result:Suppressed collagen I and FN levels.
| Species | Dose | Route | AUC0-∞ | MRT0-∞ | T1/2 | Tmax | Cmax | Vz |
|---|---|---|---|---|---|---|---|---|
| Rat[1] | 150 mg/kg | p.o. | 11599.6 ng·h/mL | 3.51 h | 1.55 h | 1.99 h | 4081.01 ng/mL | 6.91 L |
FASN/SCD-IN-1 (150 mg/kg, p.o., once a day, 4 weeks) reduces steatosis, attenuates oxidative stress, inflammatory response, and liver fibrosis, and therefore markedly ameliorates the progression in HFD + CCl4-induced MASH mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CCl4 (1 mg/kg, i.p.)-induced acute liver injury SD rat (male, 6 weeks) model[1]
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Dosage:100 mg/kg
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Administration:i.g. once a day, 7 days
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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.
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Animal Model:HFD + CCl4 (0.2 mg/kg, i.p., once a week)-induced MASH C57BL/6 mice (male, 6 weeks) model[1]
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Dosage:150 mg/kg
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Administration:p.o., once a day, 4 weeks
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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.
化学情報
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CAS 番号 3063509-61-2
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分子量 498.50
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分子式 C25H22O9S
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SMILES
OC1=C2C([C@@H]([C@H](OC2=CC(O)=C1)C3=CC4=C(C=C3)OC(CS)C(C5=CC=C(C(OC)=C5)O)O4)O)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
FASN/SCD-IN-1 関連分類
HY-176274 関連分類
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