Potency data for probe BI-8668 and control BI-0337
In vitro potency
| Target name | Target information | Species | Assay description | BI-8668 | BI-0337 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| SCNN1A, SCNN1B, SCNN1G | epithelium | Homo sapiens | Inhibition of Na+ current by Ussing Chamber: Measurement of net ion transport across an epithelium using Ussing Chamber- MucilAir™ P0: IC50 were derived form a 5-steps concentration curve (1 nM -> 10,000 nM) | IC50 = 17 nM (n=6) | IC50 > 10 µM (n=6) |
In cell potency
| Target name | Target information | Species | Assay description | BI-8668 | BI-0337 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| SCNN1A, SCNN1B, SCNN1G | M1 cells | Mus musculus | Inhibition of M-1 water resorption: Measurement of ENaC-mediated water permeability through cell monolayers of M-1 cells and the blocking capacity of ENaC-inhibitors. The transported volume is determined with tritiated water. A potent ENaC-inhibitor results in reduced water transport leading to more remaining liquid in the apical (upper) compartment of the cell layer. | Inhibition = 81% |