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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- Fòrmula: C38H44N6O9S2
- Peso molecular:792.92
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Help & FAQs
Actividad biológica
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.
Chemical Information
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Peso molecular 792.92
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CD-10 Related Classifications
HY-174395 Related Classifications
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