Table 2.
EC50 values shown for the Cl−/NO3 − antiport assay, the NMDG-Cl assay alone, with gramicidin (Gra) and with oleic acid (OA), with the chloride selectivity (SG) and the factor of enhancement (FOA) included.
Perenosin | clog Pa | Cl−/NO3 − at pH 7.2 (by ISE) | NMDG-Cl (by HPTS) | |||||
---|---|---|---|---|---|---|---|---|
EC50 (mol%)b | nc | EC50 (mol%)d | EC50 (Gra) (mol%)e | EC50 (OA) (mol%)f | SG g | FOA h | ||
1d | 5.1 | 0.1220 | 1.2 | 0.01073 | 0.00656 | 0.00925 | 1.6 | 1.2 |
2 | 4.9 | 0.0043 | 1.3 | 0.00062 | 0.00037 | 0.00085 | 1.7 | 0.7 |
3 | 5.7 | n.d.i | n.d.i | 0.01151 | 0.00879 | 0.04912 | 1.3 | 0.2 |
4 | 4.4 | 0.0111 | 1.1 | 0.00069 | 0.00038 | 0.00008 | 1.8 | 8.6 |
5 | 5.3 | 0.0227 | 1.3 | 0.00231 | 0.00095 | 0.00273 | 2.4 | 0.9 |
6 | 6.9 | 0.0852 | 0.3 | 0.00249 | 0.00211 | 0.00208 | 1.2 | 1.2 |
7 | 6.1 | >10j | n/aj | n.d.j | n.d.j | n.d.j | n/aj | n/aj |
8 | 6.2 | >10j | n/aj | n.d.j | n.d.j | n.d.j | n/aj | n/aj |
aaverage clog P values calculated using VCCLab62. bEC50 at 270 s, shown as carrier: lipid molar percent. cHill coefficient reveals the stoichiometry of the complex mediating transport. dEC50 from the NMDG-Cl assay, measuring H+/Cl− symport. eEC50 in the presence of Gra, showing the total H+/Cl− symport possible with no rate limiting H+/OH− transport. Gra concentration has been optimised to 0.1 mol%. fEC50 in the presence of OA, showing changes in transport due to acceleration of the natural proton transport facilitated by fatty acids. OA concentration has been optimised to 2 mol%. gSG > 1 indicates Cl− selectivity and is calculated by dividing EC50 in absence of Gra by EC50 (Gra). hFactor of enhancement in the overall H+/Cl− cotransport rate is calculated by dividing EC50 in absence of Gra or OA by EC50 (OA). FOA > 1 suggests the receptor can assist the flip-flop of OA− increasing pH dissipation. in.d. EC50 not determined by ISE due to poor solubility. jWeak transport ability where EC50 for Cl−/NO3 − by ISE is larger than 10 mol%, hence NMDG-Cl by HPTS assay not determined (n.d.).