BAY 11-7085 is an irreversible inhibitor of TNFα-induced IκBα phosphorylation with IC50 of 10 μM.
|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 models||male Lewis rats of Adjuvant Arthritis model|
|Formulation||0.5% methyl cellulose|
|Dosages||5 or 20 mg/kg once a day|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 40 mg/mL|
Novel inhibitors of cytokine-induced IkappaBalpha phosphorylation and endothelial cell adhesion molecule expression show anti-inflammatory effects in vivo.
Pierce JW, et al. J Biol Chem. 1997 Aug 22;272(34):21096-103. PMID: 9261113.
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