Nrf2/HO-1 activator 4
Nrf2/HO-1 activator 4 is a Nrf2/HO-1 activator. Nrf2/HO-1 activator 4 inhibits nitric oxide production and the expression of pro-inflammatory cytokines IL-1β, IL-6, TNF-α, as well as upstream inflammatory enzymes COX-2 and iNOS. Nrf2/HO-1 activator 4 reduces ROS accumulation, and restores GSH levels and SOD activity. Nrf2/HO-1 activator 4 ameliorates depression-like behaviors in mice. Nrf2/HO-1 activator 4 can be used for research on major depressive disorder.
For research use only. We do not sell to patients.
- CAS No.: 3072761-08-8
- Formula: C27H27FN6O2S
- Molecular Weight:518.61
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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HO-1 |
IL-1β |
IL-6 |
iNOS |
COX-2 |
Nrf2/HO-1 activator 4 (Compound 6j) (1-10 μM; 26 h) potently inhibits LPS (HY-D1056)-induced NO production in BV-2 microglia with an IC50 of 3.45 μM, and shows no cytotoxicity at concentrations up to 10 μM[1].
Nrf2/HO-1 activator 4 (5-10 μM; 8-26 h) reduces LPS-induced mRNA and protein expression of COX-2 and iNOS in BV-2 microglial cells in a concentration-dependent manner[1].
Nrf2/HO-1 activator 4 (5-10 μM; 8 h) concentration-dependently inhibits the LPS-induced upregulation of IL-1β, IL-6 and TNF-α mRNA expression in BV-2 microglia[1].
Nrf2/HO-1 activator 4 (10 μM; 26 h) alleviates LPS-induced oxidative stress in BV-2 microglial cells by reducing ROS accumulation, restoring GSH levels, and increasing SOD activity[1].
Nrf2/HO-1 activator 4 (5-10 μM; 26 h) activates the Nrf2-HO-1 pathway in LPS-stimulated BV-2 microglia by increasing nuclear accumulation of Nrf2 and upregulating HO-1 protein expression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BV-2 microglial cells
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Concentration:5 μM, 10 μM
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Incubation Time:2 h pretreatment, followed by 6 h LPS stimulation
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Result:Significantly attenuated LPS-induced upregulation of IL-1β, IL-6, and TNF-α mRNA at 5 μM.
Enhanced the inhibitory effect on LPS-induced IL-1β, IL-6, and TNF-α mRNA upregulation in a concentration-dependent manner at 10 μM.
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Cell Line:BV-2 microglial cells
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Concentration:5 μM, 10 μM
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Incubation Time:2 h pretreatment, followed by 24 h LPS stimulation
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Result:Increased the levels of the iNOS and COX-2.
Significantly promoted the nuclear translocation of Nrf2 and the expression of protective proteins such as HO-1.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 J (8-week-old male, LPS-induced depressive model)[1]
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Dosage:10 mg/kg
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Administration:i.p.; daily; 2 days
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Result:Reduced LPS-induced immobility time in the tail suspension test from 160.6 s to 131.3 s.
Decreased the number of Iba1+ microglia, total area of Iba1+ staining, number of GFAP+ astrocytes, and total area of GFAP+ staining in the hippocampus compared to the LPS group.
Significantly attenuated LPS-induced upregulation of IL-1β and TNF-α mRNA expression in hippocampal tissue.
Chemical Information
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CAS No. 3072761-08-8
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Molecular Weight 518.61
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Formula C27H27FN6O2S
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SMILES
CC(C)COC1=CC=C(C2=NC(C)=C(C(NC(C)(C3=CN(C4=CC=C(F)C=C4)N=N3)C)=O)S2)C=C1C#N
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)