Catalog No.
Product Name
Application
Product Information
Citations
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CFTR Corrector
CFTR Corrector 18 is a potent cystic fibrosis transmembrane conductance regulator (CFTR) corrector. It enhances the processing and trafficking of CFTR, thereby increasing the presence of functional CFTR protein on the cell surface. This compound is a valuable tool for research applications focused on cystic fibrosis, aiming to elucidate pathways for therapeutic intervention and improve understanding of CFTR-related pathophysiology. -
CFTR Modulator
(R)-Olacaftor, a CFTR modulator, functions by enhancing the activity of the cystic fibrosis transmembrane conductance regulator. This compound demonstrates significant potential in the therapeutic investigation of cystic fibrosis, making it a valuable tool for research into CF-related pathophysiology and treatment strategies. Its role in restoring CFTR function supports studies targeting the underlying mechanisms of cystic fibrosis. -
CFTR Modulator
CFTR Corrector 9 is a small molecule modulator targeting the cystic fibrosis transmembrane conductance regulator (CFTR). This compound is designed to enhance the trafficking and functionality of mutant CFTR proteins, making it valuable for research into cystic fibrosis and other CFTR-related disorders. Its application can facilitate studies aimed at understanding disease mechanisms and developing therapeutic strategies for CF. -
CFTR Blocker
AF-2785 is a potent blocker of the cystic fibrosis transmembrane conductance regulator (CFTR). It effectively inhibits the cAMP-activated chloride current in rat epididymal cells, exhibiting an IC50 of 170.6 μM. This reagent is primarily utilized in research focused on contraceptive mechanisms and related studies. -
CFTR Modulator
Zatonacaftor is a cystic fibrosis transmembrane conductance regulator (CFTR) modulator designed to enhance the activity of the CFTR protein. This compound is primarily used in research studies focusing on cystic fibrosis, providing insights into disease mechanisms and potential therapeutic strategies. Its role in restoring CFTR function may aid in the development of new treatment approaches for cystic fibrosis patients. -
CFTR Corrector
Bamocaftor potassium is a CFTR corrector that targets the cystic fibrosis transmembrane conductance regulator (CFTR) protein, specifically aimed at restoring the function of the F508del mutant variant. This compound is particularly useful in cystic fibrosis research when used in combination with Tezacaftor and Ivacaftor, providing insights into pharmacological interventions for improving chloride ion transport in affected patients. Its role in potentiating drug efficacy makes it significant for developing combination therapies in the treatment of cystic fibrosis. -
CFTR Activator
CP-628006 is a small molecule CFTR potentiator that enhances ATP-dependent gating of the cystic fibrosis mutant G551D-CFTR. This compound has demonstrated key biological activity in restoring channel function, making it a valuable tool for research focused on cystic fibrosis pathophysiology and potential therapeutic interventions. Its utility in studying CFTR modulation may aid in the development of novel treatments for cystic fibrosis and related disorders. -
CFTR Activator
CFTR Activator 2 (WAY-326769) is a selective activator of the cystic fibrosis transmembrane conductance regulator (CFTR), specifically targeting mutant forms of the protein. This compound enhances chloride ion transport across epithelial cell membranes, thereby improving ion permeability and function in cells expressing mutant CFTR. CFTR Activator 2 is valuable for research applications aimed at understanding cystic fibrosis pathophysiology and developing potential therapeutic strategies. -
CAL/CFTR Inhibitor
PGD97 is a selective cyclic peptide inhibitor that targets the CAL/CFTR interactions, exhibiting a KD value of 6 nM for its desulfide cyclized form at the CAL PDZ domain. Demonstrating a selectivity of ≥ 130-fold compared to NHERF1/2 PDZ domains, PGD97 effectively stabilizes F508del-CFTR at the cell membrane, enhancing CFTR function essential for maintaining fluid homeostasis in the lung. This compound is valuable for research applications focused on cystic fibrosis. -
CFTR Corrector
CFTR Corrector 11 is a chemical compound that acts as a corrector for the Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) protein. It is primarily utilized in research focused on cystic fibrosis, where it aids in the rescue of misfolded CFTR proteins, thereby improving chloride ion transport. This compound is instrumental in studying therapeutic strategies for cystic fibrosis and evaluating the functional restoration of CFTR activity in affected cells. -
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. -
CLCN2 Activator
Lubiprostone (hemiketal) is a selective activator of chloride channel 2 (CLCN2). It effectively increases chloride ion secretion in the intestine, enhancing fluid secretion and promoting intestinal peristalsis, making it valuable for studying chronic idiopathic constipation and opioid-induced constipation. This compound is also applicable in cancer research, providing insights into gastrointestinal function and potential therapeutic interventions. -
GABA/Glutamate-gated Chloride Channel Potentiator
4''-Oxoavermectin B1a is a potent modulator of GABA (γ-aminobutyric acid) and glutamate-gated chloride channels, exhibiting significant insecticidal and acaricidal properties. This compound demonstrates efficacy in disrupting neurological processes in target pests, making it a valuable tool for research in agricultural pest management. Its application contributes to understanding the mechanisms of action in pest control strategies. -
TMEM16A Modulator
TMEM16A modulator-1 is a positive modulator of the calcium-activated chloride channel TMEM16A. This compound enhances the activity of TMEM16A, making it valuable for investigating its roles in various biological processes. It is particularly relevant for research into TMEM16A-related diseases, such as respiratory disorders, where modulation of ion channels may reveal therapeutic possibilities. -
Type-2 Chloride Channel Activator
Cobiprostone is a type-2 chloride channel activator known for its protective effects against NSAID-induced cellular damage. It effectively prevents Indomethacin-induced depolarization of mitochondrial membrane potential and reverses subsequent loss of membrane integrity. This compound is valuable for research focused on mitochondrial function and cellular responsiveness to ion channel modulation. -
Chloride Channel Inhibitor
NS3736 is an orally bioavailable inhibitor of chloride channels, specifically targeting the CIC-7 channel in osteocytes. This compound effectively blocks osteoclast acidification and resorption in vitro, exhibiting an IC50 of 30 μM. In preclinical studies using a rat model of ovariectomy-induced osteoporosis, NS3736 has demonstrated the ability to enhance bone strength and increase bone density, making it a valuable tool for researching osteoporosis. -
BK/ClC-2 Chloride Channels Activator
Unoprostone is an activator of BK (large conductance Ca2+-activated K+) channels and ClC-2 chloride channels. This compound has demonstrated the ability to protect retinal cells from oxidative stress and light-induced damage, while also improving phagocytic function. Additionally, Unoprostone effectively reduces intraocular pressure, making it a valuable tool for research into glaucoma, ocular hypertension, and retinitis pigmentosa. -
Anxiolytic Agent
BTG 1640 is a potent anxiolytic agent classified as an isoxazoline. It selectively inhibits GABA- and glutamate-gated chloride channels, contributing to its anxiolytic effects. This compound is of significant interest in neuropharmacological research for studying anxiety disorders and their treatment mechanisms. -
GABAA Receptor Chloride channel Inhibitor
Leptophos oxon is a potent GABAA receptor chloride channel inhibitor, exhibiting an IC50 value of 89.6 μM. This compound effectively inhibits GABA-induced chloride influx through binding to the TBPS sites associated with GABAA receptors, as well as inhibiting TBPS binding to voltage-dependent chloride channels. Leptophos oxon is primarily utilized in studies related to neurological diseases and functions as an insecticide, making it relevant for research in both neurobiology and pest management. -
Chloride Channel Inhibitor
NS5818 is a potent chloride channel inhibitor that effectively disrupts acidification and bone resorption processes. Its mechanism of action makes it a valuable tool for studying osteoporosis and associated bone metabolic disorders. Researchers can utilize NS5818 to gain insights into chloride channel functions and their implications in bone health. -
Chloride Channel Inhibitor
Alilusem potassium is a selective chloride channel inhibitor known for its diuretic properties. Studies have demonstrated its effectiveness in reducing free water clearance while enhancing sodium and chloride excretion in urine during water diuresis in anesthetized canine models. Additionally, Alilusem potassium, when administered with Furosemide or Hydrochlorothiazide, further diminished free water clearance. This compound has also been shown to inhibit lumen-positive transepithelial voltage and chloride flux across isolated rabbit cortical thick ascending limbs of Henle, making it a valuable tool for research in renal physiology and electrolyte transport mechanisms. -
Stable Isotope
Niflumic Acid-d5 is a deuterium-labeled derivative of Niflumic acid, which acts primarily as a calcium-activated chloride channel blocker. This compound exhibits significant analgesic and anti-inflammatory properties, making it useful in the management of conditions such as rheumatoid arthritis. Its stable isotope form is valuable for research applications in pharmacokinetics, metabolic studies, and mechanistic investigations of calcium channel modulation. -
CRM1 Degrader
CRM1 Degrader 1 is a targeted agent that selectively degrades chromosome region maintenance 1 (CRM1), a nuclear exporter critical for the transport of various tumor suppressor proteins. By inducing apoptosis in gastric carcinoma cells, CRM1 Degrader 1 demonstrates significant anti-proliferative effects, making it a valuable tool for cancer research. This compound is primarily used to explore therapeutic strategies aimed at regulating CRM1-related pathways in cancer biology. -
EAAT Inhibitor
DL-TBOA is a potent non-transportable inhibitor of excitatory amino acid transporters (EAATs), specifically targeting EAAT1, EAAT2, and EAAT3 with IC50 values of 70 μM, 6 μM, and 6 μM, respectively. This compound effectively inhibits the uptake of [14C]glutamate in COS-1 cells expressing human EAAT1 and EAAT2, demonstrating Ki values of 42 μM and 5.7 μM, respectively. Additionally, DL-TBOA competitively blocks EAAT4 and EAAT5 with Ki values of 4.4 μM and 3.2 μM, respectively. This reagent is valuable for studying excitatory neurotransmission and related pathologies in research applications. -
GLT-1/EAAT2 Activator
LDN-212320 is a potent activator of the glutamate transporter GLT-1 (EAAT2), primarily functioning at the translational level. This compound is known to mitigate nociceptive pain by enhancing astroglial GLT-1 expression in both the hippocampus and anterior cingulate cortex. LDN-212320 is valuable in research focused on pain modulation and neuroprotection, offering insights into the role of glutamate transporters in neurological conditions. -
Human EAAT2 Inhibitor
WAY-213613 hydrochloride is a potent and selective inhibitor of the human excitatory amino acid transporter 2 (EAAT2). With an IC50 value of 85 nM, it effectively modulates glutamate transport, making it a valuable tool for investigating glutamatergic signaling in the central nervous system. This compound is suitable for research applications exploring neurobiology and potential therapeutic interventions related to neurodegenerative diseases. -
EAAT2 PAM
NA-014 is a selective positive allosteric modulator (PAM) of the excitatory amino acid transporter 2 (EAAT2), exhibiting an EC50 of 3 nM. This compound enhances the transport activity of EAAT2, which is crucial for regulating glutamate levels in the synaptic cleft. NA-014 is valuable for research into neurodegenerative diseases and synaptic dysfunction, providing insights into therapeutic strategies that target glutamate homeostasis. -
EAAT1 Inhibitor
UCPH-102 is a highly selective inhibitor of the excitatory amino acid transporter 1 (EAAT1), exhibiting an IC50 value of 0.43 µM. This compound demonstrates significant anti-proliferative effects on T-cell acute lymphoblastic leukemia (T-ALL) cells. Furthermore, UCPH-102's favorable blood-brain barrier permeability makes it a valuable tool for research in neurodegenerative diseases such as amyotrophic lateral sclerosis and Alzheimer’s disease, as well as conditions related to chronic pain and obsessive-compulsive disorder. -
EAAT Inhibitor
L-threo-3-Hydroxyaspartic acid functions as a selective inhibitor of excitatory amino acid transporters (EAATs), exhibiting inhibitory constants (Kis) of 11, 19, and 14 μM for EAAT1, EAAT2, and EAAT3, respectively, in HEK293 cell lines. This compound plays a crucial role in the study of neurotransmitter regulation and excitotoxicity, making it valuable for research related to neurological disorders and synaptic transmission. Its ability to modulate glutamate signaling contributes to understanding potential therapeutic pathways for conditions such as epilepsy and neurodegenerative diseases. -
EAAT Modulator
Nε-(Carboxyethyl)lysine is a known modulator of excitatory amino acid transporters (EAATs). As an advanced glycation end product (AGE), it facilitates protein cross-linking, leading to alterations in protein structure and function, ultimately resulting in protein denaturation. Nε-(Carboxyethyl)lysine interacts with RAGE receptors, influencing cell signaling pathways critical for inflammatory response, cell proliferation, and apoptosis. Additionally, it affects glutamate transporter activity, reducing glutamate uptake and S100B protein secretion, thereby impacting neurotransmission and demonstrating neurotoxic effects associated with diabetes. -
EAAT2 Activator
EAAT2 Activator 1 is a potent activator of the excitatory amino acid transporter 2 (EAAT2), a critical protein responsible for the clearance of glutamate from synaptic clefts. This compound enhances EAAT2 protein levels in a dose-dependent manner, promoting efficient glutamate uptake. EAAT2 Activator 1 is relevant for research applications aimed at understanding glutamatergic signaling and neuroprotection in various neurological disorders. -
EAAT2 Modulator
(R)-AS-1 is a selective positive allosteric modulator of the excitatory amino acid transporter 2 (EAAT2), exhibiting an EC50 of 11 nM. This compound enhances spontaneous locomotor activity in murine models at doses of 60 and 90 mg/kg. Additionally, (R)-AS-1 demonstrates significant anticonvulsant effects in various seizure models, with ED50 values of 66.3 mg/kg for maximal electroshock, 36.3 mg/kg for pentylenetetrazole, and 41.6 mg/kg for electrical stimuli. This agent is valuable for research in neurological disorders. -
EAAT3 Inhibitor
SLC1A1/EAAT3-IN-1 is a selective inhibitor of the excitatory amino acid transporter 3 (EAAT3), exhibiting an IC50 of 7.2 μM for human EAAT3 while showing significantly reduced inhibition of EAAT1, 2, and 4 (IC50: ~250 μM). This compound is primarily utilized in research related to psychiatric disorders, including obsessive-compulsive disorder and schizophrenia, and can aid in the investigation of neurotransmitter dynamics and therapeutic strategies targeting EAAT3. -
EAAT Blocker
(±)-HIP-B is a non-competitive blocker of excitatory amino acid transporters (EAATs), demonstrating effective inhibition of glutamate uptake with an IC50 of 17-18 μM. This compound serves as a valuable lead in research focused on ischemia-induced neuronal degeneration. Its application extends to the investigation of various neurological disorders, contributing to a deeper understanding of excitotoxicity and neuronal survival mechanisms. -
EAAT Inhibitor
DL-TBOA ammonium is a selective inhibitor of excitatory amino acid transporters (EAATs), demonstrating IC50 values of 70 μM, 6 μM, and 6 μM for EAAT1, EAAT2, and EAAT3, respectively. This compound effectively inhibits the uptake of [14C]glutamate in COS-1 cells expressing human EAAT1 and EAAT2, with Ki values of 42 μM and 5.7 μM. Additionally, DL-TBOA ammonium competitively inhibits EAAT4 and EAAT5, featuring Ki values of 4.4 μM and 3.2 μM, respectively. Its distinct mechanism renders it a valuable tool for studies on excitatory neurotransmission and the role of glutamate transporters in neurological research. -
EAAT2/4 Inhibitor
(±)-threo-3-Methylglutamic acid is a potent inhibitor of excitatory amino acid transporters EAAT2 and EAAT4. It functions as an ionotropic glutamate receptor agonist and is effective in inhibiting glutamate uptake in rod outer segments. This compound is valuable for research applications focusing on glutamatergic signaling and transport mechanisms in the nervous system. -
EAAT2 Positive Allosteric Modulator, neurological disease
DA-023 is a selective positive allosteric modulator of the excitatory amino acid transporter 2 (EAAT2) with an EC50 value of 1 nM. This compound enhances EAAT2 activity, which is crucial for glutamate regulation in the central nervous system. DA-023 is particularly relevant for research into neurological diseases, offering potential insights into therapeutic strategies for conditions associated with glutamate dysregulation. -
EAAT Blocker
(±)-HIP-A is a non-competitive blocker of excitatory amino acid transporters (EAATs) that inhibits glutamate uptake with an IC50 value of 17-18 μM. This compound serves as a lead candidate for research into ischemia-induced neuronal degeneration. (±)-HIP-A is particularly valuable for studying the pathophysiology of neurological diseases and the mechanisms underlying excitotoxicity. -
GABAA Receptor Antagonist
Bicuculline (methochloride) is a selective antagonist of the GABAA receptor, exhibiting an IC50 value of 3 μM. This compound is known to induce clonic-tonic convulsions in mammals and is also capable of blocking Ca2+-activated potassium channels. Bicuculline (methochloride) is utilized in research focused on epilepsy and related psychiatric disorders, providing valuable insights into neuronal excitability and inhibitory transmission. -
GABA Uptake Inhibitor
Nipecotic acid is a potent inhibitor of GABA uptake in neurons and glial cells, significantly impacting GABAergic neurotransmission. This compound has also been shown to directly activate GABAA-like chloride channels, with an effective concentration (EC50) of approximately 300 μM. Its biological activity makes nipecotic acid valuable for research applications focused on GABAergic signaling and associated neurological processes.
