TABLE 4

Estimated IC50 values (nM) for NaV1 blockers at human NaV1 channels

TTXaCmpd 801bCmpd 13cICA121431d
NaV1.168nd23
NaV1.2126900240
NaV1.34460>30,00013
NaV1.61.68690013,000
NaV1.761212,000
NaV1.7 (GP)2.74.416.9>10,000
  • a All values are for human NaV1 channels, except for the guinea pig (GP) NaV1.7 values. The values for TTX were obtained from (Catterall et al., 2005), except for the the NaV1.7, which were obtained here, as described in Materials and Methods.

  • b The values for compound 801 were obtained, as described in Materials and Methods.

  • c The values for compound 13 were obtained by Ion Works and provided by Dr. Silvia Fonquerna at Almirall Laboratories.

  • d The values for ICA121431 were obtained from (McCormack et al., 2013).

  • nd - not determined

  • GP- guinea pig