HD202A
HD202A is an orally active, selective dual inhibitor of MNK1/MNK2 (with IC50 values of 6.09 nM and 8.06 nM, and Kd values of 1.913 μM and 5.244 μM, respectively) that inhibits the MNK-eIF4E signaling pathway. By downregulating perilipin 2 and SCD1, while upregulating adipose triglyceride lipase and PPARγ coactivator 1α, HD202A enhances mitochondrial fatty acid oxidation and redox homeostasis. HD202A effectively suppresses body weight gain, hepatic lipid accumulation and elevation of serum lipids, significantly improves glucose tolerance and insulin sensitivity of the organism, and ameliorates inflammatory features. With these comprehensive pharmacological activities, HD202A exhibits great application potential in studies of metabolic dysfunction-associated steatotic liver disease.
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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。
- CAS 番号: 2930131-74-9
- 分子式: C25H24N6OS
- 分子量:456.56
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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
|
MNK1 6.09 nM (IC50) |
MNK2 8.06 nM (IC50) |
PPARγ1 |
eIF4E |
MNK1 1.913 μM (Kd) |
MNK2 5.244 μM (Kd) |
HD202A (compound 26) (0.1-1 μM) dose-dependently inhibits MNK-mediated eIF4E phosphorylation in A549 cells[1].
HD202A (1 μM) reduces lipid droplet accumulation and downregulates Plin2 in differentiated 3T3-L1 adipocytes without causing cytotoxicity[1].
HD202A (1 μM; 24-36 h) reduces lipid accumulation, restores lipid homeostasis, and improves mitochondrial function in PA-induced HepG2 cells; at 25 μM, it inhibits HepG2 cell proliferation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 cells
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Concentration:25 μM; with or without 400 μM Palmitate
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Incubation Time:24-36 h
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Result:Inhibited HepG2 cell proliferation by ~40%.
HD202A (25-75 mg/kg; p.o.; single dose) exhibits in vivo MNK inhibitory activity in white adipose tissue, liver, and skeletal muscle of mice when measured 24 hours postdose[1].
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, 20 weeks old, mean body weight ~48 g, HFD-induced MASLD)[1]
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Dosage:12.5 mg/kg; 25 mg/kg; 50 mg/kg
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Administration:p.o.; daily; 11 weeks
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Result:Attenuated HFD-induced body weight gain dose-dependently without altering food intake.
Reduced fat mass and increased lean mass.
Decreased liver, epididymal fat, and (at 50 mg/kg only) subcutaneous fat indices.
Improved glucose homeostasis dose-dependently, with faster glucose clearance and reduced AUC in ITT and OGTT at 50 mg/kg.
Reduced fasting glucose, serum TG, TC, LDL-C, NEFA, ALT, AST, and TNF-α levels across relevant doses.
Reduced hepatic triglyceride content and macrovesicular steatosis dose-dependently.
Decreased hepatic iNOS H-scores and increased hepatic CD163 H-scores (without changing F4/80 levels) at 50 mg/kg.
Suppressed hepatic P-eIF4E levels.
Downregulated SCD1 and Plin2 expression.
Upregulated ATGL and PGC-1α expression.
化学情報
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CAS 番号 2930131-74-9
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分子量 456.56
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分子式 C25H24N6OS
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SMILES
O=C(N1CCC(N(C)C)CC1)C2=CC=C(C3=NN4C(S3)=NC=C4C5=CC=C(C#N)C=C5)C=C2
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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)
HD202A 関連分類
HY-182046 関連分類
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