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

CFTR

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.

CFTR Related Products (32):

Cat. No. Product Name Effect Purity
  • HY-13262
    Lumacaftor Modulator 99.19%
    Lumacaftor (VX-809; VRT 826809) is a CFTR modulator that corrects the folding and trafficking of CFTR protein.
  • HY-111772
    Elexacaftor Modulator 99.77%
    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.
  • HY-15206
    Glibenclamide Inhibitor 99.79%
    Glibenclamide is a high affinity P-glycoprotein inhibitor and appears to be general inhibitor of ABC transporters. Glibenclamide binds to the sulphonylurea receptor (SUR) and to the cystic fibrosis transmembrane conductance regulator proteins (CFTR) and blocks their function. Glibenclamide is a potent second-generation sulfonylurea agent that improves glucose control by acting both on insulin secretion and on insulin action..
  • HY-15448
    Tezacaftor Modulator 99.94%
    Tezacaftor (VX-661) is a second F508del CFTR corrector and help CFTR protein reach the cell surface.
  • HY-13017
    Ivacaftor Agonist 99.96%
    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.
  • HY-14832
    Ataluren Inhibitor 99.71%
    Ataluren (PTC124) is an orally available CFTR-G542X nonsense allele inhibitor.
  • HY-109177
    Icenticaftor Activator
    Icenticaftor (QBW251) is an orally active CFTR channel potentiator, with EC50s of 79 nM and 497 nM for F508del and G551D CFTR, respectively. Icenticaftor can be used for chronic obstructive pulmonary disease (COPD) and cystic fibrosis research.
  • HY-106203A
    Crinecerfont hydrochloride Antagonist
    Crinecerfont (SSR-125543) hydrochloride is a potent, orally active, non-peptide CRF1 receptor antagonist. Crinecerfont can be used for Classic congenital adrenal hyperplasia (CAH) research.
  • HY-16671
    CFTR(inh)-172 Inhibitor 98.70%
    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.
  • HY-111680
    PTI-428 Modulator 99.77%
    PTI-428 is a specific cystic fibrosis transmembrane conductance regulator (CFTR) amplifier.
  • HY-19778
    (R)-BPO-27 Inhibitor 99.86%
    (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.
  • HY-111099
    GLPG1837 Agonist 99.03%
    GLPG1837 is a potent and reversible CFTR potentiator, with EC50s of 3 nM and 339 nM for F508del and G551D CFTR, respectively.
  • HY-119936
    GLPG2451 Activator 99.62%
    GLPG2451 is a cystic fibrosis transmembrane conductance regulator (CFTR) potentiator, which effectively potentiates low temperature rescued F508del CFTR with an EC50 of 11.1 nM.
  • HY-18336
    GlyH-101 Inhibitor 99.0%
    GlyH-101 is a cell-permeable glycinyl hydrazone compound that blocks CFTR with Ki of 1.4 uM.
  • HY-19778A
    BPO-27 racemate Inhibitor 98.37%
    BPO-27 racemate is a potent CFTR inhibitor with an IC50 of 8 nM.
  • HY-18337
    IOWH-032 Inhibitor 99.66%
    IOWH-032 is a novel and potent CFTR inhibitor (IC50=1.01 uM) in T84 and CHO-CFTR cell based assays.
  • HY-14179
    PPQ-102 Inhibitor 99.82%
    PPQ-102 is a potent CFTR inhibitor which can completely inhibited CFTR chloride current with IC50 of ~90 nM.
  • HY-19970
    KM11060 Activator 99.80%
    KM11060 is a corrector of the F508 deletion (F508del)-cystic fibrosis transmembrane conductance regulator (CFTR) trafficking defect. KM11060 can be used for the research of F508del-CFTR processing defect and development of cystic fibrosis therapeutics.
  • HY-125381
    CFTR corrector 2 Modulator 99.85%
    CFTR corrector 2 is a cystic fibrosis transmembrane conductance corrector (CFTR), extracted from patent US20140274933.
  • 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).
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