| In Vitro | In vitro activity: Evans Blue is found to be inhibiting DNA binding of NF-κB at a low concentration of 100 μM. It has proven over the years to be a dependable stain for microscopic determination of cell death. Evans Blue is also a known blocker of a subset of a-amino-3-hydroxy-5-methyl-isoxazole/kainate receptors (IC50=355 nM) for the subunit combination GluR1,2. Evans blue is the first known δ-subunit-specific antagonist of ENaC and activates large-conductance Ca2+-activated K+ channels in sheep bladder myocytes and cultured endothelial cells of human umbilical veins.
Kinase Assay:
Cell Assay: |
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| In Vivo | Evans blue pretreatment could inhibit the mast cells degranulation and that may be the main mechanism for prevent animals from C48/80-triggered anaphylaxis and systemic inflammation. Evans blue modulates the non-N-methyl-d-aspartate receptor in rat thalamic neurons, blocks the P2X-purinergic receptor in rat vas deferens, and inhibits the glutamate transporter in rat brain synaptic vesicles. |
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| Animal model | CD hairless rats |
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| Formulation & Dosage | Dissolved in saline; 100 mg/kg; i.p. |
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| References | Bioorg Med Chem Lett. 2004 Dec 20;14(24):6123-7; J Pharmacol Exp Ther. 2005 Nov;315(2):965-9. |
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