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. 2021 Sep 21;8:742457. doi: 10.3389/fmolb.2021.742457

TABLE 3.

Kinetic properties of Tap1a-WT and Tap1a-OPT1 at hNaV1.1 and hNaV1.7 determined via patch-clamp electrophysiology. Kinetic data were determined using peptide concentrations equivalent to 10× IC50, and k obs and k off are given as the mean ± SEM from 4–7 independent experiments.

Kon observed (s−1) Kon (nM−1s−1) Koff (s−1) Kd (nM)
hNaV1.1
 Tap1a-WT 2.01 ± 0.1 × 10−2 6.53 × 10–6 6.56 ± 0.32 × 10−4 3.16 × 10–2
 Tap1a-OPT1 8.75 ± 0.8 × 10−2 * , # ndb irreversiblea ndb
hNaV1.7
 Tap1a-WT 7.07 ± 1.2 × 10−3 6.52 × 10–6 8.46 ± 0.6 × 10–4 1.2 × 10–1
 Tap1a-OPT1 8.60 ± 1.7 × 10−3 ndb irreversiblea ndb

Kon observed = 1/τon; kon = [(1/τon)–koff]/(ligand); koff = 1/τoff; Kd = koff /kon.

*

Statistically significant compared to Tap1a-WT Kon observed for NaV1.1, p = 0.0121.

Statistically significant compared to Tap1a-WT Kon observed for NaV1.7, p = 0.0061.

#

Statistically significant compared to Tap1a-OPT1 Kon observed for NaV1.7, p = 0.0012.

a

Koff is less than the lowest valid measurement under the experimental conditions.

b

nd = not determined.