BAY 11-7085 is an irreversible inhibitor of TNFα-induced IκBα phosphorylation with IC50 of 10 μM.
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Source | Clin Exp Otorhinolaryngol (2018). Figure 3. Bay 11-7085 |
| Method | RT-PCR | |
| Cell Lines | B cells | |
| Concentrations | 10 μM | |
| Incubation Time | 1 h | |
| Results | Results of RT-PCR and ELISA showed that BAY 11-7085 significantly attenuated recombinant nCLU-induced MUC5AC mRNA expression and protein production |
| Cell Experiment | |
|---|---|
| Cell lines | HUVEC |
| Preparation method | Human umbilical vein endothelial cells (HUVEC) were isolated and maintained in culture using previously described procedures. For experiments on cytokine induction, cells were exposed to recombinant human TNFα at a final concentration of 100 units/ml in complete media for the times indicated. The proteosomal inhibitor carbobenzoxyl-leucinyl-leucinyl-leucinal-H (MG115) was prepared as a 40 mM stock solution in Me2SO and added to complete medium to a final concentration of 40 μM. Cell toxicity was assessed by morphology and by 3-(4,5-dimethyl thiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. |
| Concentrations | 0, 1.25, 2.5, 5, 10 and 20 μM |
| Incubation time | 16 h |
| Animal Experiment | |
|---|---|
| Animal models | male Lewis rats of Adjuvant Arthritis model |
| Formulation | 0.5% methyl cellulose |
| Dosages | 5 or 20 mg/kg once a day |
| Administration | intraperitoneal injection |
| Molecular Weight | 249.33 |
| Formula | C13H15NO2S |
| CAS Number | 196309-76-9 |
| Solubility (25°C) | DMSO 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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