Ion Channel Modulators

m3-Huwentoxin IV (m3-HwTx-IV) is a potent Na_V inhibitor with IC₅₀s of 3.3, 6.8, 7.2, 8.4, 11.9 and 369 nM against hNa_V1.7, hNa_V1.6, hNa_V1.3, hNa_V1.1, hNa_V1.2 and hNa_V1.4, respectively in QPatch assay. m3-Huwentoxin IV dose-dependently suppresses spontaneous pain induced by the Na_V1.7 activator OD1 in a rodent pain model.

Mambalgin-3 is an acid-sensitive ion channel 1 (ASIC1) inhibitor. Mambalgin-3 can be used in the study of analgesia.

Tertiapin-RQ is an inward rectifier K⁺ channel blocker peptide with antidepressive effect.

Jingzhaotoxin-X (JZTX-X) is a selective Kv4.2 and Kv4.3 potassium channels inhibitor. Jingzhaotoxin-X causes long-lasting mechanical hyperalgesia.

Jingzhaotoxin XI (JZTX-XI) is a sodium conductance inhibitor with an IC₅₀ of 124 nM. Jingzhaotoxin XI slows the fast inactivation (EC₅₀=1.18±0.2 μM) of Na_v1.5 expressed in Chinese hamster ovary (CHO-K1) cells.

Jingzhaotoxin-XII (JzTx-XII) is a specific Kv4.1 channel inhibitor with an IC₅₀ of 0.363 μM. Jingzhaotoxin-XII interacts with the channels by modifying the gating behavior.

KTX-Sp2 is a potassium channel toxin. KTX-Sp2 effectively blocks three types of exogenous voltage-gated potassium channels: Kv1.1, Kv1.2 and Kv1.3. Ktx-Sp2 inhibits endogenous Kv1.3 and suppresses Ca²⁺ signaling in Jurkat T cells. Ktx-Sp2 inhibits IL-2 secretion from activated Jurkat T cells.

Kurtoxin is a selective Cav3 (T-type) voltage-gated Ca²⁺ channel gating inhibitor with a K_d of 15 nM for Cav3.1 (α1G T-type) Ca²⁺ channel. Kurtoxin can interact with high affinity with native neuronal high-threshold L-type, N-type, and P-type Ca²⁺ channels in central and peripheral neurons. Kurtoxin also shows cross-reactivity with voltage-gated Na⁺ channel.

mHuwentoxin-IV is a naturally modified Huwentoxin-IV (HY-P1220). mHuwentoxin-IV inhibits tetrodotoxin-sensitive (TTX-S) voltage-gated sodium channels of dorsal root ganglion neurons with an IC₅₀ of 54.16 nM. mHuwentoxin-IV inhibition of tetrodotoxin-sensitive sodium channels is not reversed by strong depolarization voltages.

Tap1a (Theraphotoxin-Tap1a) is a spider venom peptide that inhibits sodium channels with IC₅₀s of 80 nM and 301 nM against Na_v1.7 and Na_v1.1, respectively. Tap1a shows analgesic effects.

Aa1 toxin, a neurotoxic peptide that can be obtained from the venom of Androctonus australis Garzoni, is a specific potassium channel blocker. Aa1 toxin can be used in the study of neurological diseases.

Aam-KTX is a K_v channel inhibitor with IC₅₀ values of 1.1 nM and >750 nM for K_v1.3 and K_v1.1, respectively. Aam-KTX is a toxic peptide obtained from the venom of the scorpion Mesobuthus eupeus. Aam-KTX has potential in autoimmune diseases research.

δ-Dendrotoxin is a K⁺ channel blocker that can be obtained from the venom of the black mamba snake. δ-Dendrotoxin can be used in the study of neurological diseases.

Ceratotoxin-2 (CcoTx2) is a voltage-gated sodium channel blocker with IC₅₀s of 8 nM and 88 nM against Na_v1.2/β₁ and Na_v1.3/β₁, respectively.

Pe1b (μ-TrTx-Pe1b) is a selective Na_v1.7 inhibitor with an IC₅₀ of 167 nM.

FS-2 is a potent and specific L-type Ca_V channel inhibitor. FS-2 inhibits high K⁺ or glucose induced L-type Ca²⁺ influx in RIN beta cells.

GsAF-I is a potent Na_v and hERG1 channels blocker with IC₅₀s of 0.36, 0.6, 1.28, 0.33, 1.2, 0.04 and 4.8 μM against Na_v1.1, Na_v1.2, Na_v1.3, Na_v1.4, Na_v1.6, Na_v1.7 and hERG1, respectively.

Haplotoxin-2 is a peptide toxin that can be isolated from Haplopelma lividum.

δ-Theraphotoxin-Hm1a toxin is a selective Na_v1.1 activator. δ-Theraphotoxin-Hm1a toxin elicits pain and touch sensitivity. δ-Theraphotoxin-Hm1a toxin can be used for the research of irritable bowel syndrome.

Mambalgin-2 (Mamb-2) is an acid-sensitive ion channels (ASICs) inhibitor and a venom peptide. Mambalgin-2 can be obtained from the venom of the African black mamba. Mambalgin-2 can be used in the study of pain and neurological diseases.