NF-κB-IN-20
NF-κB-IN-20 is an orally active NF-κB inhibitor. NF-κB-IN-20 directly binds to the Keap1 protein, activating the Keap1/Nrf2/HO-1 antioxidant pathway, and simultaneously inhibiting the NF-κB inflammatory pathway, thereby synergistically reducing oxidative stress and inflammatory responses. NF-κB-IN-20 M11 inhibits the expression of IL-6, IL-1β, and TNF-α, significantly reduces the level of ROS, and restores the mitochondrial membrane potential. NF-κB-IN-20 can be used for the study of acute lung injury (ALI).
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- 화학식: C21H23NO4
- 분자량:353.41
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보관:
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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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
NF-κB |
IL-6 |
IL-1β |
HO-1 |
In Vitro
NF-κB-IN-20 (Compound M11) (0.01‑100 μM, 5 h) exhibits good in vitro safety (CC50 > 100 μM) in LPS (HY-D1056)-induced Raw264.7 cells, attenuates the mRNA expression levels of the inflammatory and oxidative stress markers IL-6 (IC50 = 6.55 μM), IL-1β, TNF-α, and SOD in a dose-dependent manner and inhibits ROS expression, enhances mitochondrial membrane potential, therefore mitigating LPS-induced cellular damage[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Raw264.7 cells
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Concentration:25, 50 and 100 μM
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Incubation Time:1 h and stimulated with LPS for 4 h.
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Result:Reduced the mRNA expressions of IL-6, IL-1β, and TNF-α and increased the mRNA expression of SOD.
Parmacokinetics
In Vivo
NF-κB-IN-20 (15-60 mg/kg, i.g., once daily for 7 days) enhances sputum secretion and mitigated coughing in mice, thereby contributing to the management of pulmonary diseases[1].
NF-κB-IN-20 (500 mg/kg, i.g., single dose) exhibits good in vivo safety profile in SD rats during the 14-day During the 14-day observation period[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:LPS induced ALI model established in five-to six-week-old male BALB/c mice[1]
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Dosage:15, 30 and 60 mg/kg
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Administration:Oral gavage (i.g.), once daily for 7 days
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Result:Significantly reduced the total number of inflammatory cells in BALF. Enhanced the activities of SOD and GSH-Px in lung tissue, while reducing the level of ROS, effectively reversing the oxidative stress caused by LPS. Improved the pathological phenomena such as inflammatory cell infiltration, destruction of alveolar structure, and thickening of alveolar septa.
Inhibited the expression of M1-type macrophage markers (iNOS, CD86), while promoting the expression of M2-type markers (Arg-1, CD163).
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Animal Model:Cecal puncture induced ALI model established in five-to six-week-old male BALB/c mice[1]
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Dosage:15, 30 and 60 mg/kg
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Administration:Oral gavage (i.g.), once daily for 7 days
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Result:Alleviated lung injury caused by sepsis infection.
Ameliorated inflammatory cell infiltration, alleviated alveolar atrophy, and inhibited collagen formation and fibrosis.
Reversed the expression of inflammatory cytokine and oxidative stress related factors.
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Animal Model:5 % ammonia-induced cough assay established in five-to six-week-old male BALB/c mice[1]
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Dosage:15, 30 and 60 mg/kg
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Administration:Oral gavage (i.g.), once daily for 7 days
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Result:Demonstrated a significant increase in phenol red secretion in the BALF. Led to a prolonged cough latency period and a decreased frequency of coughs.
- RNA extraction experimental
- Mitochondrial membrane-potential fluorescent assay
- ROS/oxidative-stress fluorescent staining
- Fluorescent plasma-membrane potential dye assay
- Mitochondrial membrane-potential and mitochondrial mass staining
- Research Protocol for Inflammation-related Diseases
- Inhalation Toxicity Study
- Pyroptosis Solutions
Chemical Information
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분자량 353.41
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화학식 C21H23NO4
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SMILES
O=C(N(C)/C=C\C1=CC=CC=C1)/C=C/C2=CC(OC)=C(OC)C(OC)=C2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NF-κB-IN-20 Related Classifications
HY-175833 Related Classifications
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Keywords
- NF-κB-IN-20
- NF-κB
- Keap1-Nrf2
- Heme Oxygenase (HO)
- Interleukin Related
- TNF Receptor
- Reactive Oxygen Species (ROS)
- SOD
- Nuclear factor-κB
- Nuclear factor-kappaB
- Heme Oxygenase
- IL
- Tumor Necrosis Factor Receptor
- TNFR
- Superoxide Dismutase
- Acute lung injury
- Anti-inflammation
- Lansiummaide B analogues
- Oxidative stress
- Inhibitor
- inhibitor
- inhibit