1. Signaling Pathways
  2. Membrane Transporter/Ion Channel
  3. CFTR

CFTR

Cystic fibrosis transmembrane conductance regulator

CFTR (Cystic fibrosis transmembrane conductance regulator), mutations of which cause cystic fibrosis, belongs to the ATP-binding cassette (ABC) transporter family and works as a channel for small anions, such as chloride and bicarbonate. CFTR is composed of two homologous halves, each comprising a transmembrane (TMD) and a nucleotide binding domain (NBD). CFTR activity is regulated by phosphorylation of its cytosolic regulatory (R) domain, and ATP binding and hydrolysis at two NBDs.

CFTR is expressed in many cell types throughout the body, but in the airways it is found mainly in secretory serous cells of the submucosal glands. Transitions between open and closed states of CFTR are regulated by ATP binding and hydrolysis on the cytosolic nucleotide binding domains, which are coupled with the transmembrane (TM) domains forming the pathway for anion permeation. CFTR function is normally tightly controlled as dysregulation can lead to life-threatening diseases such as secretory diarrhoea and cystic fibrosis.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-13017
    Ivacaftor
    Agonist 99.90%
    Ivacaftor (VX-770) is a potent and orally bioavailable CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with EC50s of 100 nM and 25 nM, respectively.
    Ivacaftor
  • HY-13262
    Lumacaftor
    Modulator 99.83%
    Lumacaftor (VX-809; VRT 826809) is a CFTR modulator that corrects the folding and trafficking of CFTR protein.
    Lumacaftor
  • HY-15206
    Glibenclamide
    Inhibitor 99.92%
    Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR). Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability. Glibenclamide can induce autophagy.
    Glibenclamide
  • HY-16671
    CFTR(inh)-172
    Inhibitor 99.25%
    CFTR(inh)-172 is a potent and selective blocker of the CFTR chloride channel; reversibly inhibits CFTR short-circuit current in less than 2 minutes with a Ki of 300 nM.
    CFTR(inh)-172
  • HY-14832
    Ataluren
    Inhibitor 99.82%
    Ataluren (PTC124) is an orally available CFTR-G542X nonsense allele inhibitor.
    Ataluren
  • HY-P1108A
    Astressin 2B TFA
    Antagonist
    Astressin 2B TFA is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist, with the IC50 values of 1.3 nM and > 500 nM for CRF2 and CRF1, respectively. Astressin 2B TFA antagonizes CRF2-mediated inhibition of gastric emptying.
    Astressin 2B TFA
  • HY-155742
    CFTR corrector 12
    Modulator
    CFTR corrector 12 (compound 17C) is a bithiazole derivative, serving as CFTR corrector. CFTR corrector 12 has the ability to correct some folding defective mutants of the channel responsible for the control of chloride transport across the plasma membrane. CFTR corrector 12 recovers the α-sarcoglycan (α-SG) content in mutant cells.
    CFTR corrector 12
  • HY-156522
    CRF1 receptor antagonist-1
    Antagonist
    CRF1 receptor antagonist-1 (Compound 2) is a CRF1 receptor antagonist. CRF1 receptor antagonist-1 can be used for research of congenital adrenal hyperplasia (CAH).
    CRF1 receptor antagonist-1
  • HY-15448
    Tezacaftor
    Modulator 99.94%
    Tezacaftor (VX-661) is a F508del CFTR corrector. It helps CFTR protein reach the cell surface. However, Ivacaftor (VX-770, HY-13017), a CFTR potentiator, helps to prolong the opening time of cell surface CFTR protein channels. Tezacaftor combining with Ivacaftor, shows potent efficacy against cystic fibrosis and diseases with homozygous for the CFTR Phe508del mutation. Moreover, Elexacaftor (VX-445, HY-111772) is also a CFTR corrector. Elexacaftor-Tezacaftor-Ivacaftor aims at with cystic fibrosis (CF) with at least one Phe508del mutation, often avoids the indication for lung transplantation.
    Tezacaftor
  • HY-111772
    Elexacaftor
    Modulator 99.50%
    Elexacaftor (VX-445, Compound 1) is a modulator of cystic fibrosis transmembrane conductance regulator (CFTR). Elexacaftor (VX-445, Compound 1) facilitates the processing and trafficking of CFTR to increase the amount of CFTR at the cell surface.
    Elexacaftor
  • HY-19778
    (R)-BPO-27
    Inhibitor 99.66%
    (R)-BPO-27, the R enantiomer of BPO-27, is a potent, orally active and ATP-competitive CFTR inhibitor with an IC50 of 4 nM.
    (R)-BPO-27
  • HY-18336
    GlyH-101
    Inhibitor 98.24%
    GlyH-101 is a potent CFTR inhibitor. GlyH-101 also is a potent and reversible inhibitor of the VSORC conductance. GlyH-101 shows antiproliferative activity. GlyH-101 inhibits CFTR-like current and VSORC current.
    GlyH-101
  • HY-111680
    Nesolicaftor
    Modulator 99.65%
    Nesolicaftor (PTI-428) is a specific cystic fibrosis transmembrane conductance regulator (CFTR) amplifier.
    Nesolicaftor
  • HY-18337
    IOWH-032
    Inhibitor 99.63%
    IOWH-032 is a a synthetic anti-secretory molecule, is a potent CFTR inhibitor with an IC50 value of 8 µM. IOWH-032 also is a anti-diarrheal agent.
    IOWH-032
  • HY-150090
    SRI-41315
    Activator 99.94%
    SRI-41315 induces a prolonged pause at stop codons and suppresses PTCs (premature termination codons) associated with cystic fibrosis in immortalized and primary human bronchial epithelial cells, restoring CFTR (cystic fibrosis transmembrane conductance regulator) expression and function. SRI-41315 suppresses PTCs by reducing the abundance of the termination factor eRF1. SRI-41315 also potentiates aminoglycoside-mediated readthrough, leading to synergistic increases in CFTR activity.
    SRI-41315
  • HY-111099
    GLPG1837
    Agonist 99.86%
    GLPG1837 is a potent and reversible CFTR potentiator, with EC50s of 3 nM and 339 nM for F508del and G551D CFTR, respectively.
    GLPG1837
  • HY-109152
    Navocaftor
    Modulator 99.05%
    Navocaftor (GLPG 3067), as a cystic fibrosis transmembrane regulator (CFTR), is a protein modulator (US 20200377491 Al, example 1).
    Navocaftor
  • HY-109187A
    Posenacaftor sodium
    Modulator 99.65%
    Posenacaftor (PTI-801) sodium is a cystic fibrosis transmembrane regulator (CFTR) protein modulator that corrects the folding and trafficking of CFTR protein. Posenacaftor sodium is used for the research of cystic fibrosis (CF).
    Posenacaftor sodium
  • HY-14179
    PPQ-102
    Inhibitor 99.82%
    PPQ-102 (CFTR Inhibitor) is a reversible CFTR inhibitor that completely inhibits CFTR chloride currents (IC50 ~90 nM). PPQ-102 is not affected by membrane potential-dependent cell allocation or blocking efficiency (uncharged at physiological pH) and effectively prevents cyst enlargement in polycystic kidney disease.
    PPQ-102
  • HY-109027
    Cavosonstat
    Modulator 99.22%
    Cavosonstat (N91115) is an orally active S-nitrosoglutathione reductase (GSNOR) inhibitor. Cavosonstat is a CFTR stabilizer, and can be used for cystic fibrosis research.
    Cavosonstat
Cat. No. Product Name / Synonyms Application Reactivity