| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
NF-κB-IN-20 (Compound M11) (0.01–100 μM, 5 h) showed good in vitro safety (half-lethal concentration CC50 > 100 μM) in LPS-induced Raw264.7 cells. It was able to reduce the mRNA expression levels of inflammatory and oxidative stress markers IL-6 (IC50 = 6.55 μM), IL-1β, TNF-α and SOD in a dose-dependent manner, and inhibit the expression of reactive oxygen species (ROS), enhance mitochondrial membrane potential, thereby alleviating LPS-induced cell damage [1].
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|---|---|
| ln Vivo |
NF-κB-IN-20 (Compound M11) (15-60 mg/kg, ig, once daily for 7 days) can reduce inflammatory damage and local oxidation caused by acute lung injury, and inhibit collagen formation and ischemia of M1 macrophages[1]. NF-κB-IN-20 (15-60 mg/kg, ig, once daily for 7 days) can increase sputum in mice and reduce cough symptoms, thus contributing to the treatment of lung diseases[1]. NF-κB-IN-20 (500 mg/kg, ig, single death) showed good in vivo safety profile in SD mice over a 14-day observation period[1].
|
| Cell Assay |
RT-PCR[1]
Cell Types: Raw264.7 cells Tested Concentrations: 25, 50 and 100 μM Incubation Duration: 1 h and stimulated with LPS for 4 h. Experimental Results: Reduced the mRNA expressions of IL-6, IL-1β, and TNF-α and increased the mRNA expression of SOD. |
| Animal Protocol |
Animal/Disease Models: LPS induced ALI model established in five-to six-week-old male BALB/c mice[1]
Doses: 15, 30 and 60 mg/kg Route of Administration: Oral gavage (i.g.), once daily for 7 days Experimental Results: 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). Animal/Disease Models: Cecal puncture induced ALI model established in five-to six-week-old male BALB/c mice[1] Doses: 15, 30 and 60 mg/kg Route of Administration: Oral gavage (i.g.), once daily for 7 days Experimental Results: 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. Animal/Disease Models: 5 % ammonia-induced cough assay established in five-to six-week-old male BALB/c mice[1] Doses: 15, 30 and 60 mg/kg Route of Administration: Oral gavage (i.g.), once daily for 7 days Experimental Results: Demonstrated a significant increase in phenol red secretion in the BALF. Led to a prolonged cough latency period and a decreased frequency of coughs. |
| References |
| Molecular Formula |
C21H23NO4
|
|---|---|
| Molecular Weight |
353.41
|
| Appearance |
Typically exists as solids 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.8296 mL | 14.1479 mL | 28.2957 mL | |
| 5 mM | 0.5659 mL | 2.8296 mL | 5.6591 mL | |
| 10 mM | 0.2830 mL | 1.4148 mL | 2.8296 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.
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