CD-10
CD-10 is an orally active and BBB-penatrable Keap1-Nrf2 protein-protein interaction (PPI) inhibitor. CD-10 binds to Keap1 with a KD value of 193 nM. CD-10 exhibits potent anti-oxidative and anti-inflammatory effects through Keap1-Nrf2 pathway activation, evidenced by reduced levels of MDA, IL-4, IL-10 and increased expression of HO-1. CD-10 effectively alleviated anxiety and depressive behaviors and restored serum neurotransmitter levels by promoting Nrf2 nuclear translocation in the chronic unpredictable mild stress (CUMS) mouse model. CD-10 can be used for the study of depression.
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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。
- 分子式: C38H44N6O9S2
- 分子量:792.92
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
CD-10 (10 μM, 24 h) restores the level of Glutathione (GSH) and reduces the concentration of IL-1β significantly in the LPS (HY-D1056)-stimulated BV2 cells[1].
CD-10 (10 μM, 24 h) activates the Keap1-Nrf2 pathway by reducing the level of Malondialdehyde (MDA), IL-4, and IL-10 and increases the level of HO-1 in the LPS-stimulated BV2 cell model[1].
CD-10 (10 μM, 24 h) induces Nrf2 nuclear translocation and activates Nrf2-targeted genes in the LPS-stimulated BV2 cell model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LPS (100 ng/ml)-stimulated BV2 cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Increased the expression level of HO-1.
Didn’t change the protein level of Nrf2 in the cytoplasm and elevated the ratio of the nuclear Nrf2 level to the cytoplasmic Nrf2 level.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:8-week male C57BL/6J CUMS mouse model [1]
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Dosage:20 mg/kg
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Administration:i.g. 2 weeks
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Result:Increased the total movement distance, activity time in the central area, the total entries, percentage of time spent in opened arms and opened arm entries.
Decreased percentage of duration of total immobility in TST and immobility time in FST.
Restored the pleasure derived from sweet foods and the appetite.
Elevated the levels of SOD and GSH, reduced the level of MDA.
Reduced the levels of IL-1β and TNF-α, as well as the increased level of IL-4.
Increased the expression levels of total Nrf2, HO-1and decreased iNOS levels in the hippocampus and cortex.
Increased the nucleus protein levels of Nrf2 and the ratio of nuclear to cytoplasm Nrf2 level.
Increased the binding of Nrf2 to the ARE response element.
化学情報
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分子量 792.92
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分子式 C38H44N6O9S2
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SMILES
COC1=CC=C(C=C1)S(=O)(N(C2=CC=C(C3=CC=CC=C32)N(S(=O)(C4=CC=C(C=C4)NC(CCN5CCC6(CC5)CCOC6)=O)=O)CC(N)=O)CC(N)=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)