Ion Channel Modulators

AaHI is a neurotoxin that can be obtained from the venom of the North African scorpion Androctonus australis hector. AaHI can be used as a tool for the development of active substances with toxin-neutralizing capabilities.

ω-Grammotoxin SIA (GrTx) is P/Q and N-type voltage-gated Calcium channels inhibitor. ω-Grammotoxin SIA is also a protein toxin that can be obtained from spider venom. ω-Grammotoxin SIA has the potential to study neurological diseases as well as cardiovascular diseases.

GpTx-1 is a peptide-based Na_V1.7 sodium channel antagonist isolated from the venom of the Chilean spider Grammostola porter. GpTx-1 demonstrates potent inhibitory activity against the Na_V1.7 channel with an IC₅₀ value of 10 nM, while exhibiting excellent selectivity for Na_V1.4 (IC₅₀ = 0.301 μM) and Na_V1.5 (IC₅₀ = 4.20 μM), showing >20-fold and >950-fold selectivity respectively.

Tertiapin LQ is a specific and reversible renal outer medullary potassium ROMK1 (Kir1.1) channel inhibitor.

Conantokin R (Con-R) is an NMDA receptor peptide antagonist with an IC₅₀ of 93 nM. Conantokin R binds Zn²⁺ and Mg²⁺ with K_ds of 0.15 μM and 6.5 μM, respectively. Conantokin R shows anticonvulsant activity.

Dendrotoxin-I (DTX-I) is a potent K⁺ channels blocker with IC₅₀s of 0.13-50 nM for voltage-gated potassium channel subunits K_V1.1, K_V1.2 and K_V1.6, respectively. Dendrotoxin-I, a neurotoxin, has the potential for cancer research.

Margatoxin TFA, an alpha-KTx scorpion toxin, is a high affinity inhibitor of Kv1.3 (K_d=11.7 pM). Margatoxin TFA inhibits the Kv1.2 (K_d=6.4 pM) and Kv1.1 (K_d=4.2 nM). Margatoxin TFA, a 39 amino-acid-long peptide, is isolated from the venom of the scorpion Centruroides margaritatus and widely used in ion channel research.

Hm1a is a venom peptide and a selective hNaV1.1 activator with an EC₅₀ of 7.5 nM. Hm1a enhances hNaV1.1 and hNaV1.3 channel currents via delayed inactivation. Hm1a restores action potential firing in Dravet syndrome GABAergic inhibitory interneurons, reduces interictal epileptiform discharges and whole-brain hyperexcitability, lowers seizure frequency, and rescues premature death in Dravet syndrome mice. Hm1a can be used for the research of neurological disease, such as Dravet syndrome.

GsAF-1 is a peptide toxin containing three disulfide bonds. GsAF-1 can be isolated from the venom of the Chilean pink tarantula. GsAF-1 can be used for research of moderate-to-severe pain.

Maurotoxin is a 34-residue and four disulde-bridged toxin that can be isolated from the chactoid scorpion (Scorpio maurus). Maurotoxin inhibits the Shaker potassium channels (ShB) K⁺ current with an IC₅₀ of 2 nM.

Dc1a potently promotes opening of the German cockroach Na_v channel (BgNa_v1). Dc1a is a toxin can be isolated from the desert bush spider Diguetia canities.

BmP02 is a selective Kv1.3 channel blocker and a highly-selective Kv4.2 modulator, which can be isolated from Chinese scorpion (Buthus martensi Karsch) venom. BmP02 also delays the inactivation of Kv4.2 in HEK293T cells, with an EC₅₀ value of ~850 nM. BmP02 inhibits the transient outward potassium currents (Ito) in ventricular muscle cells.

BDS-I known as blood depressing substance, is a marine toxin which can be extracted from Anemonia sulcata. BDS-I is a specific inhibitor of Potassium Channel, targeting to Kv3.4. BDS-I inhibits Aβ1-42-induced enhancement of KV3.4 activity, caspase-3 activation, and abnormal nuclear morphology of NGF-differentiated PC-12 cells. BDS-I reverts the Aβ peptide-induced cell death.

Stromatoxin 1 is an inhibitor of Potassium Channel, a peptide which can be isolated from tarantulas. Stromatoxin 1 selectively inhibits K(V)2.1, K(V)2.2, K(V)4.2, and K(V)2.1/9.3 channels. K(V)2.1 and K(V)2.2, but not K(V)4.2, channel subunits play a key role in opposing both myogenic and neurogenic urinary bladder smooth muscle (UBSM) contractions in rats.

Scorpion toxin Tf2 is a selective human voltage-gated sodium channel Nav1.3 (hNav1.3) activator. Scorpion toxin Tf2 selectively shifts the channel's activation voltage to more negative values, enabling channel opening at resting membrane potentials. Scorpion toxin Tf2 can be used for the research of epilepsy, nociception (after spinal cord injury).

LiTx3 is a lethal and cysteine-rich peptide. LiTx3 can be isolated from L. intermedia crude venom. LiTx3 induces flaccid paralysis in Spodoptera frugiperda larvae.

Tamapin is a venom peptide, targeting to small conductance Ca(2+)-activated K(+) (SK) channels. Tamapin is a selctive blocker of SK2 (Potassium Channel). Tamapin inhibits SK channel-mediated currents in pyramidal neurons of the hippocampus. Tamapin can be isolated from the Indian red scorpion (Mesobuthus tamulus).

Phlotoxin-1 (PhlTx1) is a 34-amino acid and 3-disulfide bridge peptide. Phlotoxin-1 can be isolated from Phlogiellus genus spider. Phlotoxin-1 is an antinociceptive agent by inhibiting NaV1.7 channel.

Aah II is a sodium channel modulator. Aah II is a toxin that can be isolated from the venom of scorpion Androctonus australis.

ω-Tbo-IT1 is a peptide toxin that can be isolated from the venom of Tibellus oblongus.ω-Tbo-IT1 is an inhibitor of insect calcium channel.