Ion Channel Modulators

CALP1 is a calmodulin (CaM) agonist (K_d of 88 µM) with binding to the CaM EF-hand/Ca²⁺-binding site. CALP1 blocks calcium influx and apoptosis (IC₅₀ of 44.78 µM) through inhibition of calcium channel opening. CALP1 blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 activates CaM-dependent phosphodiesterase activity.

ProTx-I is a toxin derived from Thrixopelma pruriens and a peptide inhibitor targeting TTX-resistant sodium channels. ProTx-I interacts with voltage sensors of multiple domains such as NaV1.7, reduces neuronal excitability through allosteric modulation of channel gating and alteration of voltage dependence. The IC₅₀ values of ProTx-I against human NaV1.7, NaV1.2, NaV1.6, and NaV1.5 are 95 nM, 104 nM, 21 nM, and 358 nM, respectively; ProTx-I also potently inhibits Ba²⁺ currents of hCav3.1, while its inhibitory potency against hCav3.2 is approximately 160-fold lower. ProTx-I is applicable to the research of chronic pain.

Amlodipine aspartic acid impurity (Amlodipine aspartate) is the impurity of Amlodipine aspartic acid. Amlodipine aspartic acid is a calcium channel blocker with antihypertensive and antianginal properties. Amlodipine aspartic acid impurity can control blood pressure. Amlodipine aspartic acid impurity corrects gut dysbiosis and enhances taurine and hypotaurine metabolism. Amlodipine aspartic acid impurity can be studied in research for NAFLD and hypertension.

6-FAM-AEEAc-Stichodactyla helianthus Neurotoxin (ShK) TFA (6-FAM-AEEAC-SHK TFA) is a peptide neurotoxin conjugated with a fluorescent marker. 6-FAM-AEEAc-Stichodactyla helianthus Neurotoxin (ShK) TFA can block voltage-gated potassium channels (kv1.1 and kv1.2) to prolong the duration of action potentials, thereby affecting the conduction of neural signals. 6-FAM-AEEAc-Stichodactyla helianthus Neurotoxin (ShK) TFA can be used in neuroscience research.

Chlorotoxin(linear) is a linear 36 amino-acid peptide which can be used in Chlorotoxin related research.

Corza6 is a potent and selective human voltage-gated proton channel (hHv1) peptide inhibitor. Corza6 binds to the external voltage sensor domain (VSD) loop in hHv1 with a K_d of ~1 nM at the natural, hyperpolarized resting membrane potential (RMP) of mammalian cells. Corza6 allows capacitation in sperm and permits sustained reactive oxygen species (ROS) production in white blood cells (WBCs).

Corza6 TFA is a potent and selective human voltage-gated proton channel (hHv1) peptide inhibitor. Corza6 TFA binds to the external voltage sensor domain (VSD) loop in hHv1 with a K_d of ~1 nM at the natural, hyperpolarized resting membrane potential (RMP) of mammalian cells. Corza6 TFA allows capacitation in sperm and permits sustained reactive oxygen species (ROS) production in white blood cells (WBCs).

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.

NTPA TFA is a polycarboxylic acid ligand that participates in the coordination reaction with metal ions to form complexes.

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

Wasabi Receptor Toxin is a cell-penetrating scorpion toxin. Wasabi Receptor Toxin is the activator for TRPA1 ion channel with EC₅₀ in nanomolar level, and prolongs the channel open time, but reduces Ca²⁺ permeability. Wasabi Receptor Toxin causes thermal hypersensitivity and mechanical allodynia in rats, without triggering neurogenic inflammation.

Jingzhaotoxin-34, a 35-residue polypeptide, is a neurotoxin. Jingzhaotoxin-34 inhibits tetrodotoxin-sensitive (TTX-S) sodium currents (IC₅₀ of ~85 nM) while having no significant effects on tetrodotoxin-resistant (TTX-R) sodium currents on rat dorsal root ganglion neurons.

Spinoxin isolated from the venom of scorpion Heterometrus spinifer, is a 34-residue peptide neurotoxin cross-linked by four disulfide bridges. Spinoxin is a potent inhibitor of Kv1.3 potassium channel (IC₅₀ = 63 nM), considering to be valid molecular targets in the diagnostics and therapy of various autoimmune disorders and cancers.

Heteropodatoxin-1 (HpTx1), a spider peptide toxin, is a Kv4.2 current inhibitor. Heteropodatoxin-1 also inhibits Nav1.7 and activates Nav1.9 but does not affect Nav1.8.

Phrixotoxin 1, from the venom of the theraphosid spider Phrixotrichus auratus, is a specific peptide inhibitor of Kv4 potassium channel.

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

Hainantoxin-IV is a specific antagonist of Sodium Channel, targeting to tetrodotoxin-sensitive (TTX-S) voltage-gated sodium channels. His28 and Lys32 are the key resiudes of Hainantoxin-IV for binding with target, while Hainantoxin-IV adopts an inhibitor cystine knot motif.

Guangxitoxin 1E is a potent and selective blocker of K_V2.1 and K_V2.2 channels. Guangxitoxin 1E inhibits K_V2 with an IC₅₀ of 1-3 nM. K_V2 channels underlie delayed-rectifier potassium currents in various neurons.

Lei-Dab7 TFA is a high affinity, selective K_Ca2.2 (SK2) channel blocker (K_d=3.8 nM). Lei-Dab7 TFA exhibits >200-fold selectivity for K_Ca2.2 over K_Ca2.1, K_Ca2.3, K_Ca3.1, K_v and Kir2.1. Lei-Dab7 TFA increases theta-burst responses and increases LTP in rat hippocampal slices in vitro.

APETx2, a sea anemone peptide from Anthopleura elegantissima, is a selective and reversible ASIC3 inhibitor, with an IC₅₀ of 63 nM. APETx2 directly inhibits the ASIC3 channel by acting at its external side. APETx2 could reverses acid‐induced and inflammatory pain.