TABLE 1

Characterization of activation of hNa_v1.7 mutants in the presence of 100 nM ProTx-II

Cells were held at −100 mV. Families of currents were induced by 50-ms depolarizing steps to various potential ranging from −80 to +40 mV. Recording currents from WT and mutant Na_v1.7 started at ∼20 min after establishing whole-cell configuration. All data come from three to four cells. The half-activation potential (V_1/2) and slope factor (k) were determined with Boltzmann fits. The values of IC₅₀, slope factor (n_H), and f_bottom were determined with Hill equation in Figs. 2A, 6B, and 7B.

Channel	Voltage Dependence of Activation
	Control		ProTx-II
	V_1/2	k	V_1/2	k	IC₅₀	n_H	f_bottom
	mV	mV	mV	mV	nM
hNa_v1.7	−41.5 ± 0.8	6.5 ± 0.7	−10.4 ± 0.9	14.5 ± 0.8	0.7 ± 0.2	1.1 ± 0.2	0.05 ± 0.02
L201V/N206D	−42.5 ± 0.4	5.3 ± 0.4	−12.1 ± 1.0	17.1 ± 0.9	1.0 ± 0.3	1.1 ± 0.2	0.03 ± 0.01
F813G	−39.6 ± 0.2	5.5 ± 0.2	−23.0 ± 2.7	18.7 ± 2.8	6.0 ± 2.1	1.0 ± 0.2	0.09 ± 0.04
E818C	−33.0 ± 1.2	8.1 ± 1.1	−0.6 ± 1.2	15.3 ± 1.1	2.9 ± 0.1	1.0 ± 0.1	0.13 ± 0.03
E203K/E818C	−14.2 ± 0.4	9.0 ± 0.4	14.2 ± 1.8	19.2 ± 1.5	4.6 ± 0.7	1.2 ± 0.2	0.16 ± 0.02
F204A/F813G	−41.1 ± 1.3	7.2 ± 1.1	−26.3 ± 1.2	14.9 ± 1.2	8.2 ± 1.1	1.3 ± 0.2	0.08 ± 0.03
F813G/E818C	−34.0 ± 1.2	8.1 ± 1.1	−20.5 ± 1.4	15.3 ± 1.3	29.8 ± 3.6	1.0 ± 0.2	0.10 ± 0.05
D1586A	−33.0 ± 0.8	7.5 ± 0.7	−7.1 ± 1.2	16.6 ± 1.1	1.0 ± 0.1	1.2 ± 0.4	0.08 ± 0.04
D1586E	−40.6 ± 0.7	7.0 ± 0.6	−13.6 ± 1.9	17.5 ± 1.9	0.4 ± 0.03	1.0 ± 0.2	0.09 ± 0.02
E1589Q	−40.0 ± 1.6	8.4 ± 1.4	−11.7 ± 1.9	17.2 ± 1.8	0.5 ± 0.1	1.0 ± 0.1	0.06 ± 0.02
T1590K	−44.2 ± 0.5	5.2 ± 0.4	−16.2 ± 0.8	14.0 ± 0.7	0.9 ± 0.4	1.1 ± 0.3	0.07 ± 0.04
F1592A	−34.1 ± 1.1	8.0 ± 0.9	−5.3 ± 2.1	19.3 ± 2.1	0.7 ± 0.3	1.1 ± 0.4	0.04 ± 0.04
D1586A/T1590K	−40.5 ± 0.3	6.9 ± 0.2	−2.5 ± 0.8	18.5 ± 0.8	0.7 ± 0.4	0.8 ± 0.4	0.04 ± 0.01
T1590K/F1592A	−35.1 ± 0.2	6.9 ± 0.2	−8.3 ± 2.6	25.2 ± 2.9	0.8 ± 0.4	1.1 ± 0.1	0.06 ± 0.01