Ion Channel Modulators

Huwentoxin-IV is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC₅₀s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV has analgesic effects on animal models of inflammatory and neuropathic pain.

Agitoxin-2 is a K+ channel inhibitor, with IC₅₀ values of 201 pM and 144 pM for mK_V1.3 and mK_V1.1, respectively).

β-Pompilidotoxin TFA (β-PMTX TFA), a wasp venom, can slow sodium channel inactivation and increases steady-state sodium current in cells.

Huwentoxin XVI, an analgesic, is a highly reversible and selective mammalian N-type calcium channel (IC₅₀ of ~60 nM) antagonist from Chinese tarantula Ornithoctonus huwena. Huwentoxin XVI has no effect on voltagegated T-type calcium channels, potassium channels or sodium channels.

Huwentoxin XVI TFA, an analgesic, is a highly reversible and selective mammalian N-type calcium channel (IC₅₀ of ~60 nM) antagonist from Chinese tarantula Ornithoctonus huwena. Huwentoxin XVI TFA has no effect on voltagegated T-type calcium channels, potassium channels or sodium channels.

Calciseptine is a natural polypeptide toxin found in the venom of the black mamba snake (Dendroaspis p. polylepis). Calciseptine is a highly effective and selective blocker of the L-type channel of the Cav1.2 subtype, with an IC₅₀ value of 92 nM. Calciseptine has no effect on Cav3.1, Cav2.2, Cav2.1, Cav1.1, voltage-sensitive sodium channels and potassium channels. Calciseptine exhibits negative inotropic and negative relaxant effects on mice, and does not affect heart rate or the action potential of sinoatrial node pacemaker cells. Calciseptine can be used for research on cardiovascular diseases_[1].

ShK toxin blocks voltage-dependent potassium channel (K_v1.3 channel). ShK toxin can be isolated from the whole body extract of the Caribbean sea anemone (Stichodactylu helianthus). ShK toxin competes with dendrotoxin I and α-dendrotoxin for binding to synaptosomal membranes of rat brain, facilitates acetylcholine release. ShK toxin suppresses K+ currents in cultured rat dorsal root ganglion neurons. ShK toxin also inhibits T lymphocyte proliferation.

ADWX 1 is a new peptide inhibitor that is potent and selective for Kv1.3 with an IC₅₀ value of 1.89 pM. ADWX 1 inhibits Kv1.3 channel activity specifically to inhibit both the initial calcium signaling and NF-κB activation. ADWX 1 ameliorates the disease in rats of experimental autoimmune encephalomyelitis (EAE) models. ADWX 1 can be used to study T cell-mediated autoimmune diseases.