Ion Channel Modulators

Transdermal Peptide Disulfide (TD 1 Disulfide(peptide)) is a 11-amino acid peptide, binds toNa⁺/K⁺-ATPase beta-subunit (ATP1B1), and mainly interacts with the C-terminus of ATP1B1. Transdermal Peptide Disulfide can enhance the transdermal delivery of many macromolecules.

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

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

CALP2 is a calmodulin (CaM) antagonist ( (K_d of 7.9 µM)) with high affinity for binding to the CaM EF-hand/Ca²⁺-binding site. CALP2 inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca²⁺ concentrations. CALP2 potently inhibits of adhesion and degranulation. CALP2 is also a strong activator of alveolar macrophages.

Calciseptine TFA, a polypeptide found in black mamba venom, is a selcetive Cav1.2 L-type calcium channel inhibitor with an IC₅₀ of 92 nM. Calciseptine TFA binds to the pore domain shoulder at repeats III and IV of Cav1.2, stabilizing an inactivated conformation. Calciseptine TFA 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 TFA can be used for the research of cardiovascular diseases.

JNJ63955918 is a potent, highly selective, blocked-state Nav1.7 blocking peptide with an IC₅₀ of 8.0 nM. JNJ63955918 can be used in pain research.

Leualacin, a calcium channel blocker, can be isolated from the fungus Hapsidospora irregularis.

ShK-Dap22 is a potent Kv1.3-specific immunosuppressive Polypeptide. ShK-Dap22 is a selective Kv1.3 channel blocker with IC₅₀s of 23 pM, 1.8 nM, 10.5 nM, 37 nM, and 39 nM for mKv1.3, mKv1.1, hKv1.6, mKv1.4, and rKv1.2 channels, respectively.

Icrocaptide (ITF1697) is a stable Lys-Pro-containing peptide that inhibits the intracellular Ca²⁺-dependent fusion of Weibel-Palade bodies with the plasma membrane. Icrocaptide exerts its activity at the early stages of endothelial activation and inhibits P-selectin and von Willebrand factor secretion. Icrocaptide can be used for the study of a variety of microvascular disorders.

HG1 Toxin is a peptide found in the venom of the scorpion Heterometrus fulvipes, which has the activity of inhibiting potassium channel Kv1.3. HG1 Toxin also has the activity of inhibiting trypsin (K_i=107 nM) and can be used in the study of autoimmune diseases.

Tertiapin (reduced) is a kind of synthesis of melittin, its Cys3-Cys14 and Cys5-Cys18 between containing a disulfide bond. Tertiapin (reduced) is a kind of inward rectifier potassium channels blockers, can block the activity of calcium activates large conductance potassium channels. Tertiapin (reduced) can be used for research in diseases such as rheumatoid arthritis and multiple sclerosis.

α-Dendrotoxin (α-DTX) is a voltage-gated K⁺ channel blocker and an acid-sensing ion channel (ASIC) inhibitor. α-Dendrotoxin blocks K_v1.1, K_v1.2, K_v1.6 and D-type (I_D) voltage-gated K⁺ channels, and reversibly inhibits slowly inactivating potassium currents. α-Dendrotoxin induces epilepsy-related behaviors in mice. α-Dendrotoxin can be used in studies related to tonic-clonic seizures.

Poneratoxin is the modulator for voltage-gated sodium channel (NaV, EC₅₀ for NaV1.6 and NaV1.7 is 97 nM and 2.3 µM), that lowers the voltage threshold for activation and inhibits the inactivation of channels, enhances the excitability of neurons, and leads to the transmission of pain signals.

Anthopleurin-A is a soidum channel toxin. Anthopleurin-A is selective for cardiac channels and has cardiotonic effect. Anthopleurin-A can be isolated from the sea anemone.

wt hMLN is a microprotein that inhibits of SR Ca²⁺ pump (SERCA). wt hMLN plays an important role in skeletal muscle calcium homeostasis.

Myoregulin (MLN peptide) TFA is a member of the regulin family. Myoregulin TFA regulates muscle performance by modulating intracellular calcium handling. Myoregulin TFA interactes directly with sarcoplasmic reticulum Ca²⁺-ATPase (SERCA) and impedinf Ca²⁺ uptake into the sarcoplasmic reticulum.

Myoregulin (MLN peptide) is a member of the regulin family. Myoregulin regulates muscle performance by modulating intracellular calcium handling. Myoregulin interactes directly with sarcoplasmic reticulum Ca²⁺-ATPase (SERCA) and impedinf Ca²⁺ uptake into the sarcoplasmic reticulum.

AmmTX3 TFA is a peptide toxin identified from the venom of the scorpion Androctonus mauretanicus. AmmTX3 TFA is a highly specific blocker of K_v4 channels, which selectively and almost completely blocks transient A-type K⁺ currents with a K_i of 131 nM. AmmTX3 TFA induces epileptiform behaviors and causes death in mice receiving intracerebroventricular injection. AmmTX3 TFA increases the excitability of dentate gyrus granule cells, reduces GABAergic inhibition, enhances and stabilizes the EPSP-spike component of long-term potentiation, and impairs reference memory. AmmTX3 TFA can be used in research related to pain, epilepsy, and autism spectrum disorder.

MitTx-alpha is a subunit of MitTx. MitTx is a potent, persistent, and selective agonist for acid-sensing ion channels (ASICs). MitTx is highly selective for the ASIC1 subtype at neutral pH; under more acidic conditions (pH<6.5), MitTx massively potentiates (>100-fold) proton-evoked activation of ASIC2a channels.