ACLY-IN-4
ACLY-IN-4 is an ATP-citrate lyase (ACLY) inhibitor with an IC50 of 0.022 μM and a Kd of 0.19 μM. ACLY-IN-4 binds to the allosteric binding site of ACLY. ACLY-IN-4 exhibits hypolipidemic, anti-steatotic, insulin sensitivity-improving, anti-oxidative stress, anti-inflammatory and anti-fibrotic activities. ACLY-IN-4 alleviates hepatic steatosis, systemic insulin resistance, oxidative stress, hepatic inflammation and fibrosis. ACLY-IN-4 can be used for the research of metabolic dysfunction-associated steatohepatitis.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C15H10O6
- 分子量:286.24
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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
ACLY-IN-4 (Compound C1) (50 μM; 4 h with 1 mM OA) inhibits Oleic acid (HY-N1446)-induced lipid accumulation in shNC HepG2 cells, but this effect is attenuated in shACLY HepG2 cells, indicating an ACLY-dependent mechanism[1].
ACLY-IN-4 (50 μM; 24 h with 1 mM OA) downregulates lipogenic gene expression (FASN, ACC1, SREBP-1c) in Oleic acid-induced shNC HepG2 cells via an ACLY-dependent mechanism[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:oleic acid (OA)-induced shNC and shACLY HepG2 cells
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Concentration:50 μM
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Incubation Time:24 h (with 1 mM OA)
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Result:Significantly downregulated mRNA expression of FASN, ACC1, and SREBP-1c in OA-induced shNC HepG2 cells.
Abolished the downregulatory effect on mRNA expression of FASN, ACC1, and SREBP-1c in OA-induced shACLY HepG2 cells.
| Species | Dose | Route | Cmax | T1/2 | AUCINF_obs | CL | Bioavailability |
|---|---|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | i.p. | 2062 ng/mL | 0.42 h | 1019 ng·h/mL | 413 mL/min/kg | 255 % |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, 8 weeks old, 18-20 g, HFD-induced MASH)[1]
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Dosage:10 mg/kg; 30 mg/kg
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Administration:i.p.; daily; 8 weeks
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Result:Reduced average body weight to 46.0 g (10 mg/kg) and 32.9 g (vs 49.5 g in HFD control).
Significantly reduced serum triglyceride (TG), total cholesterol (T-CHO), alanine aminotransferase (ALT), aspartate aminotransferase (AST), low-density lipoprotein cholesterol (LDL-C), liver weight, hepatic TG, and hepatic T-CHO at 10 mg/kg.
Restored serum high-density lipoprotein cholesterol (HDL-C) levels at 10 mg/kg.
Significantly reduced hepatic lipid accumulation (confirmed by Oil Red O staining) at 10 mg/kg.
Suppressed hepatic mRNA expression of lipogenic markers (FASN, LXR, SREBP-1c, HMGCR, ACC1, CD36) and pro-inflammatory/fibrotic markers (CD68, TNF-α, NLRP3, ASC, α-SMA) at 10 mg/kg.
Restored mRNA expression of fatty acid oxidation markers (PPARα, CPT1, PPARγ, AMPKα1) at 10 mg/kg.
Reduced hepatic malondialdehyde (MDA) levels at 10 mg/kg.
Reduced liver protein levels of FASN, ACC1, NLRP3, ASC, α-SMA while increasing PPARα levels at 10 mg/kg.
Showed greater reductions in body weight, serum and hepatic lipid parameters, liver weight, and hepatic lipid accumulation than the 10 mg/kg dose at 30 mg/kg.
Produced similar significant effects on gene and protein expression of lipogenic, fatty acid oxidation, inflammatory, and fibrotic markers as the 10 mg/kg dose at 30 mg/kg.
Nearly restored hepatocellular morphology to match the standard diet control group (confirmed by H&E staining) at 30 mg/kg.
化学情報
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分子量 286.24
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分子式 C15H10O6
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SMILES
O=C(C1=CC2=CC(O)=C(C=C2O1)O)C3=CC(O)=C(C=C3)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)
ACLY-IN-4 関連分類
HY-182751 関連分類
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