Ion Channel Modulators

GsMTx4 is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology.

GsMTx4 TFA is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 TFA also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 TFA is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology.

D-GsMTx4 is a spider peptide and the D enantiomer of GsMTx4 (HY-P1410). D-GsMTx4 inhibits the mechanosensitive ion channel Piezo2. D-GsMTx4 inhibits [Ca²⁺]_i elevation. D-GsMTx4 inhibits mTOR and PI3K-Akt signaling pathways. D-GsMTx4 inhibits mechanical allodynia and thermal hyperalgesia. D-GsMTx4 can be used in researches of mechanical stress, chronic pain and idiopathic pulmonary fibrosis.

Apamin (Apamine) is an 18 amino acid peptide neurotoxin found in apitoxin (bee venom), is known as a specifically selective blocker of Ca²⁺-activated K⁺ (SK) channels and exhibits anti-inflammatory and anti-fibrotic activity.

Ziconotide acetate (SNX-111 acetate), a peptide, is a potent and selective block of N-type calcium channels antagonist. Ziconotide acetate reduces synaptic transmission, and can be used for chronic pain research.

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

D-GsMTx4 TFA is a spider peptide and the D enantiomer of GsMTx4 (HY-P1410). D-GsMTx4 TFA inhibits the mechanosensitive ion channel Piezo2. D-GsMTx4 TFA inhibits [Ca²⁺]_i elevation. D-GsMTx4 TFA inhibits mTOR and PI3K-Akt signaling pathways. D-GsMTx4 TFA inhibits mechanical allodynia and thermal hyperalgesia. D-GsMTx4 TFA can be used in researches of mechanical stress, chronic pain and idiopathic pulmonary fibrosis.

ATX-II TFA is a selective sodium channel modulator toxin. ATX-II TFA enhances late sodium current, prevents full sodium channel inactivation, and generates persistent current fractions. ATX-II TFA has pro-arrhythmic effect. ATX-II TFA slows intrinsic heart rate, prolongs QT interval and sinus node recovery time, and causes sinus pauses and arrests. ATX-II TFA can be used for the research of atrial fibrillation, long QT syndrome, and long QT3 syndrome.

Iberiotoxin is a toxin isolated from Buthus tamulus scorpion venom. Iberiotoxin is a selective high conductance high conductance Ca²⁺-activated K⁺ channel inhibitor with a K_d of ~1 nM. Iberiotoxin does not block other types of voltage-dependent ion channels.

ProTx II TFA is a selective blocker of Nav1.7 sodium channels with an IC₅₀ of 0.3 nM, and is at least 100-fold selective for Nav1.7 over other sodium channel subtypes. ProTx-II inhibits sodium channels by decreasing channel conductance and shifting activation to more positive potentials and blocks action potential propagation in nociceptors.

ω-Agatoxin IVA TFA is a potent, selective P/Q type Ca²⁺ (Cav2.1) channel blocker with IC₅₀ values of 2 nM and 90 nM. ω-Agatoxin IVA TFA inhibits glutamate exocytosis and calcium influx elicited by high potassium. ω-Agatoxin IVA TFA inhibits Capsaicin (HY-10448)-induced CGRP release and vasodilation. ω-Agatoxin IVA TFA can be used for the research of neurological and cardiovascular disease.

Caloxin 2A1 is an extracellular plasma membrane Ca²⁺-ATPase (PMCA) peptide inhibitor. Caloxin 2A1 does not affect basal Mg²⁺-ATPase or Na⁺-K⁺-ATPase.

Dalazatide (ShK-186) is a specific Kv1.3 potassium channel peptide inhibitor. Dalazatide can be used in the study of autoimmune diseases such as multiple sclerosis (MS), lupus erythematosus, psoriasis, rheumatoid arthritis, type 1 diabetes and inflammatory bowel disease.

Dalazatide (ShK-186) TFA is a specific Kv1.3 potassium channel peptide inhibitor. Dalazatide TFA can be used in the study of autoimmune diseases such as multiple sclerosis (MS), lupus erythematosus, psoriasis, rheumatoid arthritis, type 1 diabetes and inflammatory bowel disease.

SNX-482, a peptide, is a potent, high affinity, selective and voltage-dependent R-type Ca_V2.3 channel blocker with an IC₅₀ of 30 nM. SNX-482 has antinociceptive effect.

Caloxin 2A1 TFA is an extracellular plasma membrane Ca²⁺-ATPase (PMCA) peptide inhibitor. Caloxin 2A1 TFA does not affect basal Mg²⁺-ATPase or Na⁺-K⁺-ATPase.

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

Iberiotoxin (TFA) is a selective high conductance high conductance Ca²⁺-activated K⁺ channel inhibitor with a K_d of ~1 nM. Iberiotoxin (TFA) does not block other types of voltage-dependent ion channels.

Psalmotoxin 1 (PcTx1) is a protein toxin that can bind at subunit-subunit interfaces of acid-sensing ion channel 1a (ASIC1a). Psalmotoxin 1 is a potent and slective ASIC1a inhibitor (IC₅₀: 0.9 nM) by increasing the apparent affinity for H⁺ of ASIC1a. Psalmotoxin 1 can induce cell apoptosis, also inhibits cell migration, proferliration and invasion of cancer cells. Psalmotoxin 1 can be used in the research of cancers, or neurological disease.

Chlorotoxin is a 36 amino-acid peptide from the venom of the Israeli scorpion Leiurus quinquestriatus with anticancer activity. Chlorotoxin is a chloride channel blocker.