Table 1. Potency and selectivity of JzTx-V and peptide analogs.
| Peptide | Peptide Name | NaV1.7 IC50 (nM) | NaV1.4 IC50 (nM) | NaV1.5 IC50 (nM) |
|---|---|---|---|---|
| JzTx-V | JzTx-V(1–29) | 0.6 | 2.2 | 2,350 |
| 1 | [Glu28]JzTx-V(1–29) | 0.6 | 301 | 8,800 |
| 2 (AM-8145) | Pra-[Nle6;Glu28]JzTx-V(1–29) | 0.5 | 145 | 3,000 |
| 3 | Pra-[Nle6]JzTx-V(1–29) | 1.2 | 6.2 | 1,087 |
| 4 | [Pra1;Nle6;Glu28]JzTx-V(1–29) | 0.3 | 89 | 4,600 |
| 5 | [Nle6;Pra11;Glu28]JzTx-V(1–29) | 0.5 | 194 | 6,000 |
| 6 | [Nle6;Pra14;Glu28]JzTx-V(1–29) | 0.5 | 110 | 3,500 |
| 7 | [Nle6;Pra17;Glu28]JzTx-V(1–29) | 3.6 | 130 | 3,100 |
| 8 (AM-0422) | CyA-[Nle6;Pra17;Glu28]JzTx-V(1–29) | 0.8 | 103 | 966 |
| 9 (AM-8394) | Pra-[Nle6;Glu19,28]JzTx-V(1–29) | >1000 | n.d. | n.d. |
IC50 values of JzTx-V analogs on human NaV1.7, NaV1.4 and NaV1.5 as determined on the PX platform. IC50 values were determined from at least ten different cells with two to three data points per peptide concentration as previously described [24]. n.d. = not determined. All peptides contain C-terminal amides.