Catalog No.
Product Name
Application
Product Information
Citations
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CFTR Inhibitor
Oridonin (Isodonol), an entkaurane diterpenoid isolated from Rabdosia rubescens, is an important traditional Chinese herbal remedy. -
CFTR inhibitor
PTC124 also known as Ataluren is CFTR-G542X nonsense allele inhibitor.- Adi Amar-Schwartz, .et al. , Hum Mol Genet, 2023, Jul 20;32(15):2455-2463 PMID: 37145099
- L Kadunc, .et al. , FEBS Lett, 2020, May 13 PMID: 32401336
- Caspi M, .et al. , J Mol Med (Berl), 2016, Apr;94(4):469-82 PMID: 26620677
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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
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CFTR modulator
VX-809 is the second investigational oral candidate compound for the treatment of cystic fibrosis (CF).- Danny D Dinh, .et al. , EBioMedicine, 2024, Apr:102:105058 PMID: 38490104
- Daichi Hinata, .et al. , Int J Mol Sci, 2023, Jan 24;24(3):2305 PMID: 36768629
- Kusumika Saha, .et al. , Cell Mol Life Sci, 2022, Sep 27;79(10):530 PMID: 36167862
- Heledd H Jarosz-Griffiths, .et al. , Elife, 2020, Mar 2;9:e54556 PMID: 32118580
- Okiyoneda T, .et al. , Dev Cell, 2018, Mar 26;44(6):694-708.e7 PMID: 29503157
- Junko Kido, .et al. , Infect Immun, 2017, Oct; 85(10): e00311-17 PMID: 28784926
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CFTR corrector
VX-661 is another cystic fibrosis transmembrane conductance regulator (CFTR) corrector in development for the treatment of cystic fibrosis.- Daichi Hinata, .et al. , Int J Mol Sci, 2023, Jan 24;24(3):2305 PMID: 36768629
- Kusumika Saha, .et al. , Cell Mol Life Sci, 2022, Sep 27;79(10):530 PMID: 36167862
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CFTR inhibitor
CFTRinh-172 is a voltage-independent, selective CFTR inhibitor- Dao-Lai Zhang, .et al. , eLife, 2018, 7: e33432 PMID: 29393851
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CFTR inhibitor
CFTR inhibitor II, also known as GlyH-101, is a glycine hydrazide that selectively and reversibly blocks the CFTR channel (Ki = 4.3 uM).- Dao-Lai Zhang, .et al. , eLife, 2018, 7: e33432 PMID: 29393851
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CFTR potentiator
Ivacaftor benzenesulfonate is an orally bioavailable CFTR potentiator, used for cystic fibrosis treatment. -
CFTR potentiator
Ivacaftor hydrate is an orally bioavailable CFTR potentiator, used for cystic fibrosis treatment. -
CFTR corrector
CFTR corrector 2 is a cystic fibrosis transmembrane conductance corrector (CFTR), extracted from patent US20140274933. -
CFTR modulator
Elexacaftor (VX-445, Compound 1) is a modulator of cystic fibrosis transmembrane conductance regulator (CFTR). -
anticancer agent
5,7,4'-Trimethoxyflavone is isolated from Kaempferia parviflora (KP) that is a famous medicinal plant from Thailand. 5,7,4'-Trimethoxyflavone induces apoptosis, as evidenced by increments of sub-G1 phase, DNA fragmentation, annexin-V/PI staining, the Bax/Bcl-xL ratio, proteolytic activation of caspase-3, and degradation of poly (ADP-ribose) polymerase (PARP) protein.5,7,4'-Trimethoxyflavone is significantly effective at inhibiting proliferation of SNU-16 human gastric cancer cells in a concentration dependent manner. -
COX-1/COX-2 inhibitor
Glafenine is a non-selective, non-steroidal anti-inflammatory drug (NSAID) that inhibits both COX-1 and COX-2 enzymes. It exerts anti-inflammatory, anti-proliferative, and anti-migratory effects by suppressing the arachidonic acid metabolic pathway, thereby reducing prostaglandin production. Additionally, glafenine induces cell cycle arrest in vascular smooth muscle cells and endothelial cells and decreases the synthesis of the extracellular matrix protein tenascin. It is utilized in research related to inflammatory disorders, vascular restenosis, and cystic fibrosis. -
CDK Inhibitor
Aloisine A is a potent cyclin-dependent kinase (CDK) inhibitor, exhibiting IC50 values of 0.15 μM for CDK1/cyclin B, 0.12 μM for CDK2/cyclin A, 0.4 μM for CDK2/cyclin E, and 0.16 μM for CDK5/p35. In addition to its CDK inhibitory effects, Aloisine A also inhibits GSK-3α and GSK-3β with IC50 values of 0.5 μM and 1.5 μM, respectively. Notably, it enhances the activity of wild-type and mutant CFTR with submicromolar affinity through a cAMP-independent mechanism, making it a valuable tool for research related to cystic fibrosis and CFTR-related disorders. -
CFTR
H2-Gamendazole, a derivative of Lonidamine, targets the cystic fibrosis transmembrane conductance regulator (CFTR). It demonstrates significant efficacy in reducing cyst formation in polycystic kidney disease models. This compound is primarily used in research related to autosomal dominant polycystic kidney disease, contributing to a better understanding of therapeutic strategies for this condition. -
CFTR Modulator
Olacaftor is a cystic fibrosis transmembrane conductance regulator (CFTR) modulator that enhances the function of the defective CFTR protein. It has been shown to improve chloride ion transport, leading to increased hydration of airway surfaces and improved pulmonary function. Olacaftor is primarily utilized in research focused on cystic fibrosis and the development of therapies aimed at restoring CFTR activity. -
CFTR Inhibitor
BPO-27 racemate is a potent cystic fibrosis transmembrane conductance regulator (CFTR) inhibitor, exhibiting an IC50 of 8 nM. This compound has been shown to effectively suppress CFTR activity, making it valuable for research aimed at understanding CFTR-related disorders. BPO-27 racemate can be utilized in studies investigating ion channel regulation and potential therapeutic interventions for cystic fibrosis. -
CFTR Corrector
Tezacaftor-d4 is a deuterium-labeled CFTR corrector that targets the F508del mutation in the cystic fibrosis transmembrane conductance regulator (CFTR) protein. By facilitating the proper trafficking of CFTR to the cell surface, Tezacaftor-d4 enhances functional chloride transport in epithelial cells. This compound is primarily utilized in research focused on developing therapeutic strategies for cystic fibrosis by restoring CFTR activity. -
CFTR Activator
SRI-41315 is a CFTR (cystic fibrosis transmembrane conductance regulator) activator that induces a prolonged pause at stop codons and suppresses premature termination codons (PTCs) associated with cystic fibrosis. This compound restores CFTR expression and function in both immortalized and primary human bronchial epithelial cells by decreasing the levels of the termination factor eRF1. Additionally, SRI-41315 enhances aminoglycoside-mediated readthrough, resulting in synergistic increases in CFTR activity, making it a valuable tool for research into cystic fibrosis and related therapies. -
CFTR Modulator
Vanzacaftor is a novel CFTR modulator that acts as a corrector of the cystic fibrosis transmembrane conductance regulator (CFTR) protein. It enhances the proper processing and trafficking of CFTR, thereby promoting increased chloride ion transport in combination with Tezacaftor and Deutivacaftor. This combination has shown efficacy in improving lung function and alleviating respiratory symptoms in cystic fibrosis patients, making it a valuable tool for research aimed at understanding and treating cystic fibrosis-related conditions. -
CFTR Modulator
Ivacaftor-d9 is a potent CFTR modulator that enhances CFTR function, demonstrating an EC50 value of 255 nM for potentiation in G551D/F508del human bronchial epithelial cells. As a deuterated analog of Ivacaftor, it exhibits improved stability and pharmacokinetic properties, making it a valuable tool for cystic fibrosis research. Ivacaftor-d9 is suitable for studies aimed at understanding CFTR modulation and its implications in therapeutic development for cystic fibrosis. -
CFTR Modulator
NJH-2-057 is a CFTR modulator that functions as an EN523 OTUB1 recruiter. It is designed to enhance the activity of the ΔF508-CFTR mutant protein, which is associated with cystic fibrosis. This compound has potential applications in studying CFTR modulation and offers insights into therapeutic strategies for cystic fibrosis treatment. -
CFTR Regulator
(R)-Vanzacaftor is a selective regulator of the cystic fibrosis transmembrane conductance regulator (CFTR) protein. It enhances CFTR activity, which plays a crucial role in chloride ion transport across epithelial cell membranes. This compound is primarily utilized in research applications aimed at understanding and treating cystic fibrosis, particularly in studies focusing on CFTR modulation and function. -
CFTR Potentiator
Icenticaftor is an orally active potentiator of the cystic fibrosis transmembrane conductance regulator (CFTR) channel, demonstrating EC50 values of 79 nM and 497 nM for the F508del and G551D CFTR mutations, respectively. This compound is valuable for research focused on chronic obstructive pulmonary disease (COPD) and cystic fibrosis, facilitating the study of disease mechanisms and potential therapeutic strategies. -
CFTR Corrector
IDOR-4 is a type IV CFTR corrector that enhances the trafficking of the F508del-CFTR mutant to the cell surface. This compound is crucial for restoring functional chloride ion transport in cystic fibrosis research and can be utilized to study the dynamics of CFTR correction mechanisms in cellular models. Its application may contribute to the development of therapeutic strategies for patients with cystic fibrosis caused by the F508del mutation. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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.
