L-R4W2 TFA is a potent antagonist of vanilloid receptor 1 (VR1, TRPV1), with an IC50 of 0.1 μM. L-R4W2 TFA may act as a potent analgesic.

L-R4W2 is a potent antagonist of vanilloid receptor 1 (VR1, TRPV1), with an IC50 of 0.1 μM. L-R4W2 may act as a potent analgesic.

K41498 TFA is a potent and highly selective CRF2?receptor antagonist with Ki?values of 0.66 nM, 0.62 nM and 425 nM for human CRF2α, CRF2β?and CRF1 receptors respectively. K41498 TFA is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF2α- and hCRF2β-expressing cells. K41498 TFA can be used for hypotension?study.

β-Pompilidotoxin TFA (β-PMTX TFA), a wasp venom, can slow sodium channel inactivation and increases steady-state sodium current in cells.

β-Pompilidotoxin (β-PMTX), a wasp venom, can slow sodium channel inactivation and increases steady-state sodium current in cells.

ω-Agatoxin IVA is a potent, selective P/Q type Ca2+ channel blocker with IC50s of 2 nM and 90 nM for P-type and Q-type Ca2+ channels, respectively. ω-Agatoxin IVA (IC50, 30-225 nM) inhibits glutamate exocytosis and calcium influx elicited by high potassium. ω-Agatoxin IVA also blocks the high potassium-induced release of serotonin and norepinephrine. ω-Agatoxin IVA has no effect on L-type or N-type calcium channels.

ω-Agatoxin TK, a peptidyl toxin of the venom of Agelenopsis aperta, is a potent and selective P/Q type Ca2+ channel blocker. ω-Agatoxin TK inhibits the high K+ depolarisation-induced rise in internal Ca2+ in cerebral isolated nerve endings with an IC50 of of 60 nM. ω-Agatoxin TK has no effect on L-type, N-type, or T-type calcium channels.

Huwentoxin XVI TFA, an analgesic, is a highly reversible and selective mammalian N-type calcium channel (IC50 of ~60 nM) antagonist from Chinese tarantula Ornithoctonus huwena. Huwentoxin XVI TFA has no effect on voltagegated T-type calcium channels, potassium channels or sodium channels.

Huwentoxin XVI, an analgesic, is a highly reversible and selective mammalian N-type calcium channel (IC50 of ~60 nM) antagonist from Chinese tarantula Ornithoctonus huwena. Huwentoxin XVI has no effect on voltagegated T-type calcium channels, potassium channels or sodium channels.

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

CALP1 is a calmodulin (CaM) agonist (Kd 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.

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

CALP2 is a calmodulin (CaM) antagonist ( (Kd 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.

SNX-482, a peptidyl toxin of the spider Hysterocrates gigas, 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.

ProTx-I, a venom toxin of the tarantula Thrixopelma pruriens, is a potent, selective CaV3.1 channel blocker with IC50 values of 0.2 μM and 31.8 μM for hCaV3.1 and hCaV3.2 respectively. ProTx-I is also a potent blocker for voltage-gated Na+ channels and inhibits KV 2.1 channels.

COG 133 TFA is a fragment of Apolipoprotein E (APOE) peptide. COG 133 TFA competes with the ApoE holoprotein for binding the LDL receptor, with potent anti-inflammatory and neuroprotective effects. COG 133 TFA is also a nAChR antagonist with an IC50 of 445 nM.

Charybdotoxin TFA, a 37-amino acid peptide isolated from venom of the scorpion Leiurus quinquestriatus var. hebraeus, is a K+ channel blocker.

ω-Conotoxin GVIA TFA is an inhibitor of the N-type Ca2+ channel.

ω-Conotoxin GVIA is an inhibitor of the N-type Ca2+ channel.

ω-Conotoxin MVIIC TFA is a N- and P/Q-type Ca2+ channel blocker, significantly suppresses the 11-keto-βboswellic acid-mediated inhibition of glutamate release.

ω-Conotoxin MVIIC is a N- and P/Q-type Ca2+ channel blocker, significantly suppresses the 11-keto-βboswellic acid-mediated inhibition of glutamate release.

O-Nornuciferine, an aporphine-type alkaloid from lotus leaf, is a potent hERG channel inhibitor.

4,6-O-ethylidene-α-D-glucose (Ethylidene-glucose), a glucose derivative, is a competitive exofacial binding-site inhibitor on glucose transporter 1 (GLUT1) with a Ki of 12 mM for wild-type 2-deoxy-D-glucose transport.

Ferulamide is a Ferulic acid derivative isolated from Portulaca oleracea L. with anticholinesterase activities.

Isopimaric acid is a potent opener of large conductance calcium activated K+ (BK) channels.

Phellamurin is a plant flavonone glycoside from the leaves of Phellodendron amurense and inhibits intestinal P-glycoprotein. Phellamurin also inhibits egg laying by Papilio protenor. Phellamurin induces cells apoptosis and has anti-tumor activity.

(±)-Anatoxin A fumarate is a natural alkaloid isolated from freshwater cyanobacterium.(±)-Anatoxin A fumarate is a potent nicotinic receptor agonist and exhibits Ki values of 1.25 nM and 1.84 μM for binding to putative α4β2-type nAChR and α7-type nAChR in rat brain membranes, respectively. (±)-Anatoxin A fumarate stimulates [3H]-dopamine release from rat striatal synaptosomes (EC50=134 nM).

NF279 is a potent selective and reversible P2X1 receptor antagonist, with an IC50 of 19 nM. NF279 displays good selectivity over P2X2, P2X3 (IC50=1.62 μM), P2X4 (IC50>300 μM). NF279 is a dual HIV-1 coreceptor inhibitor that interferes with the functional engagement of CCR5 and CXCR4 by Env.

Ilaprazole (IY-81149) sodium is an orally active proton pump inhibitor. Ilaprazole sodium irreversibly inhibits H+/K+-ATPase in a dose-dependent manner with an IC50 of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium is used for the research of gastric ulcers. Ilaprazole sodium is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.

Cloperastine hydrochloride inhibits the hERG K+ currents in a concentration-dependent manner with an IC50 value of 27 nM.