Membrane Transporters-Ion Channels

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  1. CFTR Corrector

    Galicaftor is a potent and orally active cystic fibrosis transmembrane conductance regulator (CFTR) corrector. It plays a crucial role in restoring the function of the CFTR protein, which is often impaired in cystic fibrosis patients. This compound is primarily utilized in research focusing on cystic fibrosis therapies and the modulation of ion transport involved in this condition.
  2. CFTR Modulator

    Posenacaftor sodium is a modulator of the cystic fibrosis transmembrane conductance regulator (CFTR) protein, facilitating its proper folding and trafficking. This compound is predominantly utilized in research on cystic fibrosis (CF), aiming to enhance CFTR function and investigate potential therapeutic approaches for this genetic disorder. Its role in correcting defects in CFTR provides valuable insights into the disease mechanism and efficacy of treatment strategies.
  3. CFTR Activator

    CFTR activator 1 is a potent and selective modulator of the cystic fibrosis transmembrane conductance regulator (CFTR) channel, exhibiting an EC50 of 23 nM. This compound effectively enhances CFTR function and is applicable in research related to dry eye disease treatment. Its ability to promote chloride ion transport makes it a valuable tool for investigating therapeutic strategies in CFTR-related pathologies.
  4. CFTR Corrector

    Bamocaftor is a CFTR corrector that specifically targets the cystic fibrosis transmembrane conductance regulator (CFTR) protein, aiming to restore function to the F508del-CFTR variant. This compound is instrumental in cystic fibrosis research, particularly when used in conjunction with Tezacaftor and Ivacaftor, to enhance CFTR functionality and evaluate therapeutic strategies for cystic fibrosis management.
  5. CFTR Activator

    CFTR Corrector 6 is a potent activator of the Cystic Fibrosis Transmembrane Conductance Regulator (CFTR). It is specifically designed for research into cystic fibrosis and other disorders associated with CFTR dysfunction. This compound enhances CFTR protein function, making it a valuable tool for investigating therapeutic strategies and understanding the underlying mechanisms of CFTR-related diseases.
  6. CFTR Modulator

    (R)-Elexacaftor is an enantiomeric modulator of the cystic fibrosis transmembrane conductance regulator (CFTR), specifically targeting the F508del mutation. With an EC50 value of 0.29 µM, it exhibits potent biological activity in restoring CFTR function. This compound is essential for research focused on cystic fibrosis therapies and drug discovery aimed at improving CFTR activity in affected individuals.
  7. CFTR

    VRT-325 is a small molecule designed to target the cystic fibrosis transmembrane conductance regulator (CFTR), specifically addressing the ΔF508 mutation associated with cystic fibrosis. This compound promotes the efflux of ΔF508-CFTR from the endoplasmic reticulum, thereby restoring chloride transport in epithelial cells derived from CF patients. VRT-325 is valuable for research into therapeutic strategies aimed at correcting CFTR function and enhancing epithelial ion transport in cystic fibrosis.
  8. CFTR Corrector

    CFTR Corrector 4 is an (R,R)-form enantiomer that acts as a potent corrector of the cystic fibrosis transmembrane conductance regulator (CFTR). This compound enhances the expression of CFTR at the cellular surface, making it a promising candidate for therapeutic applications in cystic fibrosis research. Its ability to modulate CFTR levels may contribute to correcting defective chloride ion transport associated with the disease.
  9. CFTR Corrector

    CFTR Corrector 12 (compound 17C) is a bithiazole derivative that acts as a CFTR corrector by promoting the proper folding of defective CFTR mutants. This compound enhances chloride transport across the plasma membrane, making it beneficial for studies involving cystic fibrosis and related disorders. Additionally, CFTR Corrector 12 has been shown to recover α-sarcoglycan (α-SG) levels in mutant cells, indicating its potential in therapeutic approaches targeting CFTR-related pathologies.
  10. CFTR Corrector

    CFTR Corrector 15 (Compound 4172) is a corrector of the cystic fibrosis transmembrane conductance regulator (CFTR), specifically designed to repair the folding defect associated with the F508del mutation when used in conjunction with VX-809. This compound is valuable in the research of cystic fibrosis disease, providing insights into therapeutic strategies for restoring proper CFTR function and improving chloride ion transport in epithelial cells. Researchers can utilize CFTR Corrector 15 to advance studies investigating the molecular pathophysiology of cystic fibrosis and the effectiveness of combined drug therapies.
  11. CFTR Modulator

    CFTR Corrector 8 is a potent modulator of the cystic fibrosis transmembrane conductance regulator (CFTR) protein. It enhances the function of misfolded CFTR mutants, thereby improving chloride transport across epithelial cell membranes. This compound is valuable for research applications focused on cystic fibrosis and related therapies, facilitating investigations into drug efficacy and cellular rescue mechanisms.
  12. 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.
  13. CFTR Modulator

    CFTR Corrector 17 is a modulator targeting the cystic fibrosis transmembrane conductance regulator (CFTR). This compound enhances the function and trafficking of misfolded CFTR proteins, making it valuable for the study of CFTR-mediated diseases such as cystic fibrosis. It serves as a critical tool in pharmacological research aimed at developing therapies for conditions associated with CFTR dysfunction.
  14. CFTR Modulator

    UCCF-853 is a CFTR modulator that targets the Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) protein, enhancing its chloride ion channel activity. This compound has demonstrated the ability to improve epithelial ion transport, making it a valuable tool for research into therapies for cystic fibrosis and related disorders. UCCF-853 is essential for studying the modulation of CFTR function and potential rescue of defective CFTR variants in cellular models.
  15. CFTR Modulator

    Corr4A is a chemical corrector that targets the cystic fibrosis transmembrane conductance regulator (CFTR). It enhances the surface expression of the ΔF508 CFTR mutant by facilitating its proper folding and trafficking to the plasma membrane. This compound demonstrates significant potential for improving the stability and function of the rescued protein, making it valuable for research focused on cystic fibrosis and related therapies.
  16. CFTR Corrector

    GLPG-3221 is a potent, orally active corrector of cystic fibrosis transmembrane conductance regulator (CFTR), exhibiting an EC50 value of 105 nM. This compound plays a crucial role in restoring CFTR function, making it significant for the treatment of cystic fibrosis. Its primary application lies in research focused on therapies aimed at enhancing CFTR activity and improving chloride transport in epithelial cells.
  17. CFTR Corrector

    Posenacaftor is a CFTR corrector that facilitates the proper folding and trafficking of the cystic fibrosis transmembrane conductance regulator protein. This compound is primarily utilized in research focused on cystic fibrosis, aiming to enhance the functionality of defective CFTR proteins. Its ability to correct misfolded proteins makes it a valuable tool in the study of cellular mechanisms and therapeutic strategies for cystic fibrosis.
  18. CFTR Corrector

    CFTR Corrector 16 targets the cystic fibrosis transmembrane conductance regulator (CFTR) protein, functioning as a corrector to enhance its trafficking and function. It exhibits significant biological activity in restoring chloride ion channel function, making it a valuable tool for studying cystic fibrosis pathology. This compound is useful for research applications focused on the development of therapies for cystic fibrosis and related ion channel disorders.
  19. CFTR Corrector

    ARN23765 is a CFTR corrector specifically designed to target the F508del mutation. With an EC50 of 38 pM in human bronchial epithelial cells, ARN23765 enhances the maturation and membrane expression of F508del-CFTR, thereby improving ion transport and secretion. This compound plays a significant role in addressing the underlying pathological mechanisms associated with cystic fibrosis, making it a valuable tool for research in therapeutic interventions for this condition.
  20. CFTR Modulator

    Riselcaftor is a CFTR modulator that exhibits an EC50 value of 20.1 nM in human bronchial epithelial cells. This compound is primarily utilized in research focused on cystic fibrosis, facilitating investigations into the modulation of cystic fibrosis transmembrane conductance regulator activity. Its potent effects on CFTR function make it a valuable tool for studying therapeutic pathways in the treatment of cystic fibrosis.
  21. CFTR Corrector

    GLPG2737 is a potent CFTR type 2 corrector that enhances the functional activity of the CFTR protein in cystic fibrosis models. This compound can be utilized alongside a type 1 co-corrector to investigate synergistic effects on protein correction and improve chloride transport. Its application in research aids in elucidating therapeutic avenues for cystic fibrosis treatment and understanding CFTR-related pathophysiology.
  22. CFTR Modulator

    VRT-532 is a potent modulator of the cystic fibrosis transmembrane conductance regulator (CFTR) channel. It significantly enhances channel activity and intrinsic ATPase activity in G551D-CFTR variants, providing valuable insights into cystic fibrosis mechanisms. This compound is suitable for research applications focused on developing therapeutic strategies for cystic fibrosis and understanding CFTR-related dysfunction.
  23. 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.
  24. 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.
  25. 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.
  26. 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.
  27. 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.
  28. 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.
  29. 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.
  30. 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.
  31. 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.
  32. 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.
  33. 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.
  34. 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.
  35. 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.
  36. 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.
  37. 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.
  38. 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.
  39. 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.
  40. 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.
  41. 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.
  42. 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.
  43. 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.
  44. 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.
  45. 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.
  46. 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.
  47. 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.
  48. 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.
  49. 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.
  50. 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.

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