Ion Channel Modulators | Peptides | MedChemExpress

Ion Channel Modulators

Ion Channel Modulators (207)

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Formula: C185H273N49O45S6

Molecular Weight: 4095.84

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.

August 31

Formula: C185H273N49O45S6.xC2HF3O2

Molecular Weight: 4095.84 (free base)

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.

Formula: C79H131N31O24S4

Molecular Weight: 2027.34

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.

Formula: C102H172N36O32S7.xC2H4O2

Molecular Weight: 2639.13 (free base)

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.

Formula: C169H274N54O48S7·xC2HF3O2

Molecular Weight: 4054.80 (free base)

ShK toxin TFA (Stichodactyla helianthus neurotoxin TFA) is a neurotoxin. ShK toxin TFA blocks voltage-dependent potassium channel (Kv1.3 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.

Formula: C213H323N63O61S6.xC2HF3O2

Molecular Weight: 4934.62 (free acid)

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.

Formula: C179H274N50O55S7

Molecular Weight: 4230.85

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 Kd of ~1 nM. Iberiotoxin does not block other types of voltage-dependent ion channels.

Formula: C168H250N46O41S8.xC2HF3O2

Molecular Weight: 3826.59 (free base)

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.

Formula: C217H360N68O60S10.C2HF3O2

Molecular Weight: 5316.27

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.

Formula: C64H91N19O22

Molecular Weight: 1478.52

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

Formula: C184H296N57O55PS7

Molecular Weight: 4442.10

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.

Formula: C184H296N57O55PS7.xC2HF3O2

Molecular Weight: 4442.10 (free acid)

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.

Formula: C192H274N52O60S7

Molecular Weight: 4495.00

SNX-482, a peptide, is a potent, high affinity, selective and voltage-dependent R-type CaV2.3 channel blocker with an IC50 of 30 nM. SNX-482 has antinociceptive effect.

Formula: C66H92F3N19O24

Molecular Weight: 1592.54

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.

Formula: C178H286N52O50S7

Molecular Weight: 4178.95

Margatoxin, an alpha-KTx scorpion toxin, is a high affinity inhibitor of Kv1.3 (Kd=11.7 pM). Margatoxin inhibits the Kv1.2 (Kd=6.4 pM) and Kv1.1 (Kd=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.

Formula: C179H274N50O55S7.xC2HF3O2

Molecular Weight: 4230.85 (free base)

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

Formula: C200H312N62O57S6

Molecular Weight: 4689.39

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.

Formula: C158H249N53O47S11

Molecular Weight: 3995.71

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.

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