nav1.7 inhibitor-1

NaV1.7 inhibitor-1, an efficacious inhibitor of voltage-gated sodium channel (NaV) 1.7 (IC50 of 0.6 nM for hNaV1.7).

1-(2,4-difluorophenyl)guanidine hydrochloride is a compound that is a potent and selective inhibitor of the voltage-gated sodium channel Nav1.7, a key player in pain signaling. It is therefore able to reduce pain signaling, resulting in an analgesic effect.

Ancistrotecine B (Compound 2), a Nav1.7 channel inhibitor (IC50: 0.73 μM), has been shown to alleviate inflammatory pain in mice [1].

ProTx-III, a spider venom peptide derived from the Peruvian green velvet tarantula, functions as a selective and potent inhibitor of the voltage-gated sodium channel Na v 1.7, exhibiting an IC 50 of 2.1 nM. Characterized by its inhibitor cystine knot motif (ICK), ProTx-III can attenuate the pain response and is applicable in research on chronic pain, epilepsy, and arrhythmia [1].

Heteropodatoxin-1 (HpTx1), a spider peptide toxin, inhibits Kv4.2 and Nav1.7 currents while activating Nav1.9 channels, with no effect on Nav1.8 channels [1].

GTx1-15, an inhibitor cystine knot (ICK) peptide, antagonizes the voltage-dependent calcium channel Cav3.1, as well as voltage-dependent sodium channels Nav1.3 and Nav1.7 [1].

Phlo1a (μ-TrTx-Phlo1a), a 35-amino acid peptide toxin, demonstrates a weak inhibitory effect on Nav1.2 and Nav1.5 channels [1]. Meanwhile, Phlo1b acts as a selective inhibitor of the Nav1.7 channel.

Pe1b (μ-TrTx-Pe1b) is a selective NaV1.7 channel inhibitor with an inhibitory concentration 50 (IC50) value of 167 nanomolar (nM) [1].

Theraphotoxin-Tap1a (Tap1a) is a spider venom-derived peptide that acts as an inhibitor of sodium channels, displaying IC50 values of 80 nM for Na v 1.7 and 301 nM for Na v 1.1. It demonstrates analgesic effects [1].

m3-Huwentoxin IV (m3-HwTx-IV) is a potent inhibitor of sodium channels (NaV), with half-maximal inhibitory concentrations (IC50s) of 3.3 nM for hNaV1.7, 6.8 nM for hNaV1.6, 7.2 nM for hNaV1.3, 8.4 nM for hNaV1.1, 11.9 nM for hNaV1.2, and 369 nM for hNaV1.4 in the QPatch assay. It also alleviates spontaneous pain in a rodent model induced by the NaV1.7 activator OD1 in a dose-dependent manner [1].

DS43260857 is a potent NaV1.7 inhibitor with high inhibitory effects on both human and mouse NaV1.7, exhibiting IC50 values of 6.6 μM for hNaV1.1, 14 μM for hNaV1.5, 0.015 μM for hNaV1.7, and 0.061 μM for mNaV1.7 [1].