Table 2.
EC50 measured for calcium kinetic parameters using hiPSC-derived cardiomyocytes treated with pharmacologicallydiverse drugs.
| Compound | Reported EC50/IC50 |
Rise Time | Decay | FWHM | T75-25 | Reference |
|---|---|---|---|---|---|---|
| Verapamil | 143–246 nM PC-mc; PC-cc |
0.46 µM (−151 ms) |
0.17 µM (−275 ms) |
0.26 µM (−426 ms) |
0.39 µM (−168 ms) |
(Zahradník, Minarovic, & Zahradníková, 2008; Zhang, et al., 1999) |
| Bay K 8644 | 10–100 nM CR-mc |
1.3 µM (+70 ms) |
6.38 nM (+139 ms) |
11.0 nM (+209 ms) |
5.48 nM (+103 ms) |
(Ogawa, et al., 1992) |
| Dofetilide | 12 nM PC-cc |
N.S. |
0.75 nM (+183 ms) |
N.S (+207 ms) |
5.87 nM (+1091 ms) |
(Snyders & Chaudhary, 1996) |
| NS1463 | 10.5µM PC-Xl |
3.89 µM (−114 ms) |
2.54 µM (−239ms) |
7.0 µM (−357ms) |
2.33 µM (−170 ms) |
(Hansen, et al., 2006) |
| Flecainide | 7.4 µM PC-Xl |
9.67 µM (−75 ms) |
1.01 µM (+286 ms) |
N.S. (+244 ms) |
1.13 µM (+1017 ms) |
(Ramos & O'Leary, 2004) |
| Levcromakalim | 1.73 µM TM-ec |
3.72 µM (−150 ms) |
5.28 µM (−446 ms) |
9.16 µM (−597 ms) |
3.07 µM (−356 ms) |
(Houjou, et al., 1996) |
| Sotalol | 268µM PC-cc |
89.1 µM (−150 ms) |
85.7 µM (−375 ms) |
86.3 µM (−515 ms) |
None | (Peng, et al., 2010) |
| Aspirin | N.D. | N.S. | N.S. | N.S. | N.S. | |
| Cisapride | 6.5–240 nM PC-cc |
154 nM (−151 ms) |
147 nM (−404 ms) |
149 nM (−555 ms) |
N.S |
(Mohammad, et al., 1997; Potet, et al., 2001; Toga, et al., 2007) |
| Mosapride | N.D. | N.S. | N.S. | N.S. | N.S. | |
| E-4031 | 11 nM PC-cc |
38.6 nM (−141 ms) |
45.7 nM (−420 ms) |
44.1 nM (−561 ms) |
82.2 nM (−451 ms) |
(Fossa, et al., 2004) |
The specific of reduction (−) or prolongation (+) (in ms) is reported for each kinetic parameter at EC50 (e.g. Verapamil half maximally reduced the rise time by 151 ms). For comparison, the published EC50 or IC50 values for channel inhibition and the utilized methodology are listed. Abbreviations: PC-mc, Whole-Cell Patch Clamp on Mammalian Cardiomyocytes; PC-cc, Whole-Cell Patch Clamp on Transfected Cancer Cell Lines; CR-mc, Contractile Response in mammalian cardiomyocytes; PC-Xl, Patch Clamp Recording in X. laevis Oocytes; TM-ec, Tension Measurement in epithelial cells; N.D., not determined; N.S., not significant. EC50 values are listed when the drug elicited a statistically significant effect on the given parameter compared to control (vehicle alone) treatment for at least the highest concentration by ANOVA followed by the Dunnett's Multiple Comparison Test.