LasB-IN-1
LasB-IN-1 (compound 5f) is a potent and orally active inhibitor of LasB (IC50 = 8.7 μM). LasB-IN-1 effectively attenuates elastase production and biofilm formation by P. aeruginosa while alleviating the inflammatory response through downregulating MAPK and NF-κB pathways. LasB-IN-1 is potential to be a novel anti-infective candidate against drug-resistant infections.
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- 화학식: C20H22F3NO2
- 분자량:365.39
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
제품 설명
IC50 & Target
IC50: 8.7 μM (LasB)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| RAW264.7 | IC50 |
1.44 μM
Compound: 5f
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Inhibition of LPS-induced ROS production in mouse RAW264.7 cells by DCFH-DA staining based fluorescence method
Inhibition of LPS-induced ROS production in mouse RAW264.7 cells by DCFH-DA staining based fluorescence method
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[PMID: 37995562] |
| RAW264.7 | IC50 |
18.22 μM
Compound: 5f
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Antiinflammatory activity in LPS-induced mouse RAW264.7 cells assessed as inhibition of IL-1 beta production pretreated for 3 hrs followed by LPS stimulation and measured after 24 hrs by ELISA method
Antiinflammatory activity in LPS-induced mouse RAW264.7 cells assessed as inhibition of IL-1 beta production pretreated for 3 hrs followed by LPS stimulation and measured after 24 hrs by ELISA method
|
[PMID: 37995562] |
| RAW264.7 | IC50 |
2.61 μM
Compound: 5f
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Antiinflammatory activity in LPS-induced mouse RAW264.7 cells assessed as inhibition of IL-6 production pretreated for 3 hrs followed by LPS stimulation and measured after 24 hrs by ELISA method
Antiinflammatory activity in LPS-induced mouse RAW264.7 cells assessed as inhibition of IL-6 production pretreated for 3 hrs followed by LPS stimulation and measured after 24 hrs by ELISA method
|
[PMID: 37995562] |
| RAW264.7 | IC50 |
6.2 μM
Compound: 5f
|
Antiinflammatory activity in LPS-induced mouse RAW264.7 cells assessed as inhibition of TNF-alpha production pretreated for 3 hrs followed by LPS stimulation and measured after 24 hrs by ELISA method
Antiinflammatory activity in LPS-induced mouse RAW264.7 cells assessed as inhibition of TNF-alpha production pretreated for 3 hrs followed by LPS stimulation and measured after 24 hrs by ELISA method
|
[PMID: 37995562] |
In Vitro
LasB-IN-1 (5-10 μM, 10 h) suppresses the expression of LasB (IC50 = 8.7 μM), the elastase biosynthesis (IC50 = 7.3 μM) and the formation of biofilms (IC50 = 7.4 μM) in a dose-dependent manner in P. aeruginosa PAO1 strains[1].
LasB-IN-1 (1.25-20 μM, 24 h) reveals no cytotoxic effect in RAW264.7 cell and Vero cell. LasB-IN-1 (50-100 μM, 24 h) shows a slight cytotoxic effect. LasB-IN-1 (0.625-10 μM, 4 h) exerts negligible hemolytic effects on mouse and human erythrocytes[1].
LasB-IN-1 (10 μM, 4, 6 h) effectively inhibits the migration of macrophages to the site of injury in zebrafish larvae[1].
LasB-IN-1 (0.625-10 μM, 27 h) inhibits the production of IL-1β, TNF-α, and IL-6 in LPS (1 μg/mL, 24 h) treated RAW264.7 cells. LasB-IN-1 (1.25-10 μM, 27 h) also inhibits the mRNA expression of COX-2, iNOS, IL-1β, TNF-α, and IL-6[1].
LasB-IN-1 (1.25-10 μM, 27 h) significantly inhibits the phosphorylation of NF-κB p65, IκBα, JNK and ERK of LPS (1 μg/mL, 24 h) treated RAW264.7 cells in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:RAW264.7 cell and Vero cell
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Concentration:1.25, 2.5, 5, 10, 20, 50, 100 μM
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Incubation Time:24 h
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Result:Revealed no cytotoxic effect at concentrations of lower than 20 μM, a slight cytotoxic effect was observed at a concentration of 50 μM, indicating the noncytotoxicity at concentrations effective against virulence and biofilm formation.
In Vivo
LasB-IN-1 (1, 2 mg/kg, i.g., 4 h) significantly downregulates expression levels of IL-1β, TNF-α, and IL-6 as well as reduces mRNA expression of COX-2, iNOS, IL-1β, TNF-α, and IL-6 in mice [1].
LasB-IN-1 (2, 4 mg/kg, i.g., once for 7 d) shows no obvious adverse reactions [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:eight-week-old BALB/c wild-type mice (male, 18–22 g ), established a ALI model by using LPS (P. aeruginosa)[1]
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Dosage:1 and 2 mg/kg
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Administration:intragastric (i.g.), after treatment for 4 h, intraperitoneal injection of LPS (20 mg/kg), sacrificed by cervical dislocation after a 6 h treatment
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Result:Reduced myeloperoxidase (MPO) activity in mice compared with that in LPS-only mice, indicating the inhibition of neutrophil infiltration in mouse lung tissues.
Exhibited significantly downregulated expression levels of IL-1β, TNF-α, and IL-6, with a concentration-dependent response while significantly reduced mRNA expression of COX-2, iNOS, IL-1β, TNF-α, and IL-6 in mice compared with LPS-only mice.
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Animal Model:eight-week-old BALB/c wild-type mice (male, 18–22 g )[1]
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Dosage:2 and 4 mg/kg
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Administration:intragastric (i.g.) for 7 days
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Result:Exhibited no adverse effects such as vomiting or diarrhea, had a negligible impact on the body weight of mice, did not induce any significant damage or histopathological alterations in vital organs.
Chemical Information
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분자량 365.39
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화학식 C20H22F3NO2
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SMILES
O=C1N(CC2=CC=C(C(F)(F)F)C=C2)C(O)(CCCC)C3=C1C=CCC3
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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.
Protocol
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
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Fungal Biofilm Culture
Fungal biofilm culture is an in vitro method for growing surface-attached fungal communities, most commonly Candida albicans, on abiotic substrates such as polystyrene wells, silicone elastomer, or polymethylmethacrylate; the assay models adhesion, proliferation, filamentation, extracellular-matrix-associated maturation, and dispersion. Biofilm output can be read by optical density at 600 nm for adherent biomass, XTT reduction for metabolic activity, CFU recovery for viable attached or dispersed cells, and microscopy for architecture.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)