Catalog No.
Product Name
Application
Product Information
Citations
- Lubiprostone is a bicyclic fatty acid metabolite analog of Prostaglandin E1. It activates specific chloride channels in the gastrointestinal tract to stimulate intestinal fluid secretion, and increase gastrointestinal transit.
-
CFTR activator
VX-770 (Ivacaftor) is known as a CFTR potentiator.- Daichi Hinata, .et al. , Int J Mol Sci, 2023, Jan 24;24(3):2305 PMID: 36768629
- Okiyoneda T, .et al. , Dev Cell, 2018, Mar 26;44(6):694-708.e7 PMID: 29503157
-
COX inhibitor
Flufenamic acid is a nonsteroidal anti-inflammatory drug (NSAID). Inhibits calcium-activated chloride channels (CaCCs). Also increases currents through TRPC6 channels and inhibits currents through TRPC3 and TRPC7 channels. -
CaCC blocker
Talniflumate is a calcium-activated chloride channel (CaCC) (hCLCA1/mCLCA3) blocker; reduces mucin synthesis and release in cell culture and animal models. -
CaCCs Inhibitor
CaCCinh-A01 inhibits CaCC currents in human bronchial and intestinal cells. Also inhibits TMEM16A channels (IC50 = 2.1 uM, in TMEM16A-expressing FRT cells). -
TMEM16A Inhibitor
T16Ainh-A01 is a selective TMEM16A calcium-activated chloride channel inhibitor that strongly inhibits chloride current in salivary gland cells. -
Chloride Channel/GABA Receptor blocker
Picrotoxinin negatively modulate the action of GABA on GABAA receptors. - Fluralaner (INN) is a systemic insecticide and acaricide Fluralaner through potent blockage of GABA and L-glutamate gated chloride channels.
- Fluxametamide is an insecticide with wide spectrum, acts as an antagonist of GABA- and glutamate-gated chloride channels, with IC50 of 1.95 nM and 225 nM for M. domestica GABACls and GluCls.
-
Chloride Channel Inhibitor
Shikonin is a potent inhibitor of the TMEM16A chloride channel, exhibiting an IC50 value of 6.5 μM. This compound functions as a specific inhibitor of pyruvate kinase M2 (PKM2) and also modulates inflammatory pathways by inhibiting TNF-α and NF-κB activation. In addition, Shikonin decreases exosome secretion by impairing glycolytic processes and effectively inhibits AIM2 inflammasome activation. Its diverse activities make it a valuable reagent for investigating cellular signaling and inflammatory responses in research applications. -
Antibiotic
Milbemycin α10 is a macrolide antibiotic that targets glutamate-gated chloride channels in nematodes and arthropods. It exhibits potent insecticidal activity, effectively controlling a variety of agricultural pests, including larvae and other harmful insects. This compound is valuable for research in agricultural biotechnology and pest management. -
Parasite Inhibitor
Milbemycin oxime is an orally active macrolide that serves as a potent inhibitor of parasite activity. This compound, a mixture of oxime derivatives related to milbemycin A4 and A3, selectively binds to glutamate-gated chloride channels, leading to paralysis and death of various intestinal nematodes and lung/heart worms. It is widely utilized in research focused on antiparasitic drug development and mechanisms of parasitic resistance. -
Dopamine D2/5-HT2A Receptor Antagonist
Spiperone hydrochloride is a potent antagonist of dopamine D2 and 5-HT2A receptors, exhibiting Ki values of 0.06 nM and 1 nM, respectively. In addition, it selectively antagonizes the α1B-adrenoceptor and activates calcium-activated chloride channels (CaCC). This compound has demonstrated significant antipsychotic and anti-inflammatory properties, making it a valuable tool for research in neuropharmacology and inflammation studies. -
8,9-Z-isomer of Abamectin B1a
8,9-Z-Abamectin B1a is the 8,9-Z isomer of Abamectin B1a, a key antiparasitic agent. It effectively paralyzes nematodes by interacting with glutamate-gated chloride channels, leading to increased permeability of cell membranes and subsequent paralysis. This compound is widely utilized in research related to parasitology and therapeutic development for nematode infections. -
Antiparasitic Agent
Avermectin A1a is a potent antiparasitic agent that primarily targets nematodes and arthropods. It binds to glutamate-gated chloride channels, effectively blocking nerve signal transmission, which leads to paralysis of the parasites. Avermectin A1a is valuable for research on parasitic infections and contributes to the understanding of mechanisms involved in parasitic control. -
Insecticide
Avermectin B2a is an insecticide that targets glutamate-gated chloride channels (GluCls). Its primary mechanism induces hyperpolarization in nematode and insect neurons, leading to paralysis and mortality. This compound is relevant for research into the control of agricultural pests and the exploration of neurotoxic mechanisms in pests. -
Antiparasitic Agent
Δ2-Avermectin B1a is an antiparasitic agent that targets glutamate-gated chloride channels (GluCls) in the neuromuscular systems of invertebrates. By enhancing chloride ion influx, it induces hyperpolarization of the neuromuscular cell membrane, which inhibits neural signal transmission and ultimately results in paralysis and death of parasites. This compound is of significant interest for research applications aimed at controlling agricultural pests. -
Stable Isotope
Flufenamic acid-d4 is a deuterium-labeled derivative of Flufenamic acid, a non-steroidal anti-inflammatory drug. It primarily functions as a cyclooxygenase (COX) inhibitor while also activating AMP-activated protein kinase (AMPK) and modulating various ion channels, including chloride channels and L-type Ca2+ channels. This compound inhibits TEAD2 YBD functionality, affecting YAP-dependent processes such as cell migration and proliferation. Flufenamic acid-d4 is thus a valuable tool for studies in inflammation, cell signaling, and cancer research. -
Parasite
Doramectin monosaccharide, an acid degradation product of Doramectin, targets glutamate- and GABA-gated chloride channels in nematodes, enhancing their opening and resulting in effective anthelminthic activity. This compound is useful for studying the pharmacodynamics of anthelmintics and exploring mechanisms of resistance in parasitic infection research. Its significance lies in its role in understanding the biochemical pathways involved in nematode neuromuscular function and development. -
Parasiticide
Sisapronil is a phenylpyrazole compound that functions as an ectoparasiticide by inhibiting the GABA-gated chloride channels in parasites, leading to paralysis and death. It exhibits potent activity against a variety of ectoparasites, making it valuable in veterinary medicine for controlling infestations. This compound is utilized in research to investigate mechanisms of action against parasitic infections. -
Antiparasitic Agent
Tigolaner is an antiparasitic agent that targets γ-aminobutyric acid (GABA) and glutamate-gated chloride channels. This compound exhibits significant antiparasitic activity, making it valuable for research on parasitic infections. Its mechanism of action disrupts neurotransmission in parasites, which can aid in the development of novel therapeutic strategies. -
Antiparasitic
Modoflaner is an isophenylamide compound that primarily targets gamma-aminobutyric acid-gated chloride channels, functioning as a powerful antiparasitic agent. It demonstrates significant insecticidal activity by allosterically modulating these channels, leading to increased neuronal excitability and paralysis in target pests. This compound is widely utilized in research focused on insect control and parasitic disease management. -
Anti-parasitic Agent
Umifoxolaner is a γ-aminobutyric acid (GABA) regulated chloride channel antagonist with potent anti-parasitic properties. This compound is primarily utilized in research applications targeting parasitic infections, showcasing its potential in controlling and managing various parasitic diseases. The mechanism of action involves interference with chloride ion flow, contributing to the disruption of parasitic neuronal signaling. -
Drug Metabolite
15-Hydroxy Lubiprostone is an active metabolite of the laxative drug Lubiprostone, primarily targeting chloride channels. This compound exhibits biological activity by promoting fluid secretion in the intestinal lumen, thereby facilitating bowel movements. It is mainly utilized in research applications focused on gastrointestinal pharmacology and the mechanisms of action related to chloride channel activation. -
Active Metabolite
Desacetyl bisacodyl is the active metabolite of the laxative bisacodyl, primarily targeting epithelial chloride channels. This compound is known to stimulate chloride secretion in the colon and rectum of rat models, leading to increased mucus and electrolyte secretion. It is utilized in research applications focused on gastrointestinal physiology and the mechanisms underlying laxative action. -
Antiarrhythmic Agent
Tedisamil is an antiarrhythmic agent primarily targeting the transient outward potassium current (I(to)) in the atrium, leading to a significant reduction in heart rate. This compound also inhibits various potassium currents, including IK and K(ATP), as well as PKA-activated chloride channels, ultimately prolonging the cardiac action potential and QT interval. Tedisamil demonstrates effective antiarrhythmic properties against ventricular arrhythmias and atrial flutter in preclinical animal models, making it a valuable tool for cardiovascular research. -
Antiarrhythmic Agent
Tedisamil dihydrochloride is an antiarrhythmic agent primarily targeting the transient outward potassium current (I(to)) in cardiac tissue. This compound significantly slows heart rate by inhibiting multiple potassium channels, including IK, K(ATP), and PKA-activated chloride channels, which prolongs the cardiac action potential and QT interval. Tedisamil dihydrochloride is effective in demonstrating antiarrhythmic effects against ventricular arrhythmias and atrial flutter in various animal models, making it a valuable tool for cardiovascular research. -
KCC2 Antagonist
ML077 is a selective antagonist of the potassium-chloride co-transporter 2 (KCC2), with an IC50 of 537 nM for KCC2, while exhibiting minimal activity on KCC1 (IC50 > 50 μM). By inhibiting the chloride ion excretion function of KCC2, ML077 increases intracellular chloride concentrations, resulting in enhanced depolarization through chloride channels. This compound has demonstrated the ability to promote glucose-stimulated insulin secretion (GSIS) independent of KATP channels and is valuable for studying the physiological processes related to pain, epilepsy, and insulin secretion. -
Calmodulin inhibitor
Kobusin is a bisepoxylignan that functions as a calmodulin inhibitor. It is known to activate cystic fibrosis transmembrane conductance regulator (CFTR) and calcium-activated chloride channels (CaCC) while inhibiting the ANO1/ CaCC channel. This compound is valuable for research applications aimed at understanding calcium signaling and chloride transport mechanisms in various biological systems. -
Chloride Channel Activator
CBIQ (4-Chlorobenzo[f]isoquinoline) functions as a chloride channel activator, specifically targeting the cystic fibrosis transmembrane conductance regulator (CFTR) Cl- ion channels as well as the intermediate-conductance calcium-sensitive K+ channel (KCNN4). With Kd values of 0.1 μM for CFTR and 3.9 μM for KCNN4, CBIQ demonstrates significant potency. This compound is particularly valuable for research focused on cystic fibrosis and related ion transport disorders. -
Chloride Channel Inhibitor
R(+)-Methylindazone is a potent inhibitor of epithelial chloride channels. This compound effectively disrupts the interaction between Nef and the single-domain antibody Nef-sdAb19, demonstrating its ability to influence chloride channel activity. R(+)-Methylindazone is valuable for research exploring chloride channel regulation and the role of Nef in various biological processes. -
Chloride Channel Inhibitor
Ani9 is a selective inhibitor of the ANO1 chloride channel, exhibiting an IC50 of 77 nM. This compound effectively modulates smooth muscle contractions in murine models, making it a valuable tool for research on pathophysiological conditions such as tumors. Its inhibitory effects on chloride channels propose potential applications in studies targeting gastrointestinal disorders and related diseases. -
ANO1 Inhibitor
DFBTA is a potent inhibitor of ANO1 (anoctamin-1), a calcium-activated chloride channel, with an IC50 of 24 nM. This compound exhibits analgesic properties and demonstrates efficacy in models of inflammatory pain. It is a valuable reagent for research in pain pathways and the pharmacological modulation of ion channels. -
Chloride Current Blocker
Anthracene-9-carboxylic acid is an anthracene derivative that functions as a chloride current blocker, primarily targeting Ca2+-activated chloride channels (CaCCs). This compound has been utilized to investigate CaCCs in a variety of cell types, including smooth muscle cells, epithelial cells, and salivary gland cells. Its ability to selectively block chloride currents makes it a valuable tool in electrophysiological studies and research focused on cellular ion transport mechanisms. -
ClC-1 Inhibitor
NMD670 is an orally active inhibitor of the skeletal muscle chloride channel ClC-1, exhibiting an EC50 of 1.6 μM. This compound enhances neuromuscular transmission and contributes to improvements in muscle contraction and strength. NMD670 is valuable for research applications focused on muscle weakness and fatigue. -
Chloride Channel Inhibitor
MONNA is a potent inhibitor of the transmembrane protein 16A (TMEM16A, Anoctamin-1) with an IC50 of 80 nM. It effectively induces vasorelaxation in rodent resistance arteries, demonstrating its ability to modulate vascular tone regardless of chloride ion presence. This compound is valuable for research focused on chloride channel functions and their roles in cardiovascular physiology. -
ANO1 Inhibitor
ANO1-IN-4 is a reversible inhibitor of the calcium-activated chloride channel transmembrane protein 16A (TMEM16A, also known as ANO1), exhibiting an IC50 of 0.030 µM. This compound demonstrates favorable metabolic stability in rat liver microsomes, making it suitable for in vivo applications. ANO1-IN-4 effectively inhibits spontaneous contractions in mouse isolated ileum, indicating its potential for studies related to gastrointestinal motility and related disorders. -
Antiepileptic Compound
Losigamone is an orally active antiepileptic compound that primarily targets sodium channels. It enhances GABA-mediated responses by stimulating neuronal chloride channels, thus increasing chloride influx. This mechanism effectively reduces epileptiform activity induced by chloride channel antagonists, making Losigamone a valuable tool for research in epilepsy and related neuronal disorders. -
TMEM16A Inhibitor
T16A(inh)-C01 is a potent inhibitor of the TMEM16A (ANO1) chloride channel. It effectively blocks chloride ion transport mediated by ANO1 with an IC50 of 8.4 μM, while maintaining normal calcium signaling pathways. This compound is valuable for studying the physiological roles of TMEM16A in various cellular processes and examining its potential relevance in disease models. -
ClC-ec1 Inhibitor
OADS is a selective inhibitor of the chloride channel antiporter ClC-ec1, exhibiting an IC50 value of 29 μM. This compound specifically interferes with the ClC-ec1 antiporter pathway, while showing no inhibitory effects on the ClC-1 channel. OADS is utilized in research related to osteoporosis, as well as various neurodegenerative and cardiovascular diseases, facilitating the study of these critical health conditions.
