Table 1. Potency of NaV Channel Subtype Inhibition of Compounds.
XPC-7724 |
XPC-5462 |
phenytoin |
carbamazepine |
|||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|
IC50 | 95% CI | N (cells) | IC50 | 95% CI | N (cells) | IC50 | 95% CI | N (cells) | IC50 | 95% CI | N (cells) | |
hNaV1.1 | 294 | 255–354 | 71 | 8.75 | 7.53–10.2 | 62 | 13.8 | 9.59–20.1 | 26 | 39.3 | 33.3–46.7 | 41 |
hNaV1.2 | 14.3 | 12.2–16.9 | 32 | 0.0109 | 0.00968–0.0122 | 49 | 35.2 | 2.1–44.3 | 26 | 67.4 | 57.3–79.6 | 35 |
hNaV1.3 | 167 | 117–268 | 45 | 206 | 1.85–2.30 | 63 | ||||||
hNaV1.4 | 153 | 123–197 | 41 | 20.8 | 19.1–22.7 | 42 | ||||||
hNaV1.5 | 138 | 103–197 | 15 | 11.9 | 10.4–13.5 | 27 | 23.8 | 19.2–29.6 | 23 | 41.1 | 35.3–47.8 | 39 |
hNaV1.6 | 0.078 | 0.0718–0.0848 | 70 | 0.0103 | 0.000921–0.0115 | 50 | 13 | 10.1–16.9 | 29 | 25.6 | 21.1–30.8 | 45 |
hNaV1.7 | 27.7 | 20.4–40.1 | 45 | 0.192 | 0.175–0.211 | 54 | ||||||
mNaV1.6 | 0.13 | 0.103–0.164 | 30 | 0.0137 | 0.0112–0.0169 | 30 |