sEH-IN-23
sEH-IN-23 is a soluble epoxide hydrolase inhibitor with a IC50 of 0.8 nM against human sEH and 0.7 nM against murine sEH. sEH-IN-23 inhibits inflammatory factor production mediated by NF-κB activation, reactive oxygen species (ROS) generation, and the release of pro-inflammatory cytokines IL-1β, IL-6 and TNF-α. sEH-IN-23 exhibits anti-inflammatory activity in acute lung injury models. sEH-IN-23 can be used for the research of acute lung injury.
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- Fòrmula: C22H22ClF3N4O5
- Peso molecular:514.88
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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
Descripciòn
IC50 & Target
[1]|
EH1 |
IL-6 |
IL-1β |
In Vitro
sEH-IN-23 (compound 20K) (100 μg/mL; 0-60 min) has a half-life of 189.00 min in in vitro rat liver microsome stability assays[1].
Following incubation for 48 h in the CCK-8 assay, sEH-IN-23 (12.5-100 μM; 48 h) maintains the viability of RAW264.7 macrophages above 75%[1].
sEH-IN-23 (10-20 μM; 1-2 h pre-incubation) dose-dependently inhibits LPS (HY-D1056)-induced M1 polarization, reduces the release of IL-6 and TNF-α, and decreases ROS production in RAW264.7 macrophages[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 macrophages
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Concentration:12.5, 25, 50, 100 μM
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Incubation Time:48 h
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Result:Maintained cell viability higher than 75% at all tested concentrations.
Parmacokinetics
In Vivo
sEH-IN-23 (2 g/kg; p.o.; daily; for 14 consecutive days) is well tolerated in mice, with no toxicity observed in monitoring indicators or histopathology of major organs[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 (male, 20-22 g, intraperitoneal injection of LPS)[1]
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Dosage:15 mg/kg; 30 mg/kg
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Administration:i.p.; once daily; 5 consecutive days
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Result:Reduced lung histopathology scores.
Alleviated alveolar obstruction, alveolar wall thickening, and neutrophil exudation in lung tissue.
Inhibited serum inflammatory cytokines in a dose-dependent manner, reduced levels of IL-1β, IL-6, and TNF-α.
Reduced CD68-positive macrophage infiltration in lung tissue.
Inhibited LPS-induced nuclear translocation of p65 (NF-κB pathway component) in lung tissue and in F4/80-marked lung macrophages.
Reduced lung tissue myeloperoxidase (MPO) activity in a dose-dependent manner.
Reduced reactive oxygen species (ROS) levels in lung tissue.
Chemical Information
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Peso molecular 514.88
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Fòrmula C22H22ClF3N4O5
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SMILES
O=C(O)C1=CC=C(CNC(N2CCC(NC(NC3=CC=C(OC(F)(F)F)C(Cl)=C3)=O)CC2)=O)C=C1
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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)
sEH-IN-23 Related Classifications
HY-182283 Related Classifications
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