Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
IC50: 8.7 μM (LasB)[1]
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ln Vitro |
LasB-IN-1 (5-10 μM, 10 h) dose-dependently inhibits the expression of LasB (IC50 = 8.7 μM), elastase biosynthesis (IC50 = 7.3 μM) and biosynthesis in Pseudomonas aeruginosa PAO1 strain. Film formation (IC50 = 7.4 μM) [1]. LasB-IN-1 (1.25-20 μM, 24 h) has no cytotoxic effect on RAW264.7 cells and Vero cells. LasB-IN-1 (50-100 μM, 24 h) exhibits mild cytotoxicity. LasB-IN-1 (0.625-10 μM, 4 h) has negligible hemolytic effects on mouse and human erythrocytes [1]. LasB-IN-1 (10 μM, 4, 6 h) can effectively inhibit the migration of zebrafish larval macrophages to the injury site [1]. LasB-IN-1 (0.625-10 μM, 27 h) inhibits the production of IL-1β, TNF-α, and IL-6 in RAW264.7 cells treated with LPS (1 μg/mL, 24 h). LasB-IN-1 (1.25-10 μM, 27 h) can also inhibit 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 inhibited the phosphorylation of NF-κB p65, i-κB α, JNK and ERK in RAW264.7 cells treated with LPS (1 μg/mL, 24 h). And it is concentration-dependent [1].
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ln Vivo |
LasB-IN-1 (1, 2 mg/kg, gavage, 4 h) inhibited neutrophil infiltration in mouse lung tissue[1]. LasB-IN-1 (1, 2 mg/kg, gavage, 4 h) significantly downregulated the expression levels of IL-1β, TNF-α and IL-6 in mice, and reduced the expression of COX-2, iNOS, IL-1β, TNF-α and IL-6 mRNA[1]. LasB-IN-1 (2, 4 mg/kg, gavage, once a day for 7 days) had no obvious adverse reactions[1].
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Cell Assay |
Cell Viability Assay[1]
Cell Types: RAW264.7 cell and Vero cell Tested Concentrations: 1.25, 2.5, 5, 10 , 20, 50, 100 μM Incubation Duration: 24 h Experimental Results: 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 . |
Animal Protocol |
Animal/Disease Models: eight-week-old BALB/c wild-type mice (male, 18–22 g ), established a ALI model by using LPS (P. aeruginosa)[1]
Doses: 1 and 2 mg/kg Route of 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 Experimental Results: 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. Animal/Disease Models: eight-week-old BALB/c wild-type mice (male, 18–22 g )[1] Doses: 2 and 4 mg/kg Route of Administration: intragastric (i.g.) for 7 days Experimental Results: 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. |
References |
Molecular Formula |
C20H22F3NO2
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Molecular Weight |
365.39
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
Typically soluble in DMSO (e.g. 10 mM)
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.7368 mL | 13.6840 mL | 27.3680 mL | |
5 mM | 0.5474 mL | 2.7368 mL | 5.4736 mL | |
10 mM | 0.2737 mL | 1.3684 mL | 2.7368 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.