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

CFTR

Cystic fibrosis transmembrane conductance regulator

CFTR

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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-150089
    SRI-37240
    		Modulator 99.21%
    SRI-37240 is a potent premature termination codons (PTCs) inhibitor. SRI-37240 suppresses CFTR nonsense mutations. SRI-37240 alters cellular translation termination at PTCs in HEK293T cells. SRI-37240 can also restore CFTR function in primary bronchial epithelial cells when combination with G418.
    SRI-37240
  • HY-N6818
    5,​7,​4'-​Trimethoxyflavone
    		Activator 99.65%
    5,7,4’-Trimethoxyflavone can be isolated from the medicinal plant Kaempferia parviflora (KP). 5,7,4’-Trimethoxyflavone is a CFTR activator and EC50 is 64 μM. 5,7,4’-Trimethoxyflavone induces apoptosis, increases proteolytic activation of caspase-3, and degradation of ADP-ribose polymerase (PARP) protein. 5,7,4’-Trimethoxyflavone has antitumor activity. 5,7,4’-Trimethoxyflavone can be used to prevent skin aging and oxidative stress.
    5,​7,​4'-​Trimethoxyflavone
  • HY-126394
    Bamocaftor
    		Modulator 99.09%
    Bamocaftor (VX-659) is a cystic fibrosis transmembrane conductance regulator (CFTR) corrector designed to restore F508del-CFTR protein function. Bamocaftor can be used combine with Tezacaftor (HY-15448) and Ivacaftor (HY-13017) in cystic fibrosis research.
    Bamocaftor
  • HY-109152
    Navocaftor
    		Modulator 99.20%
    Navocaftor (GLPG 3067), as a cystic fibrosis transmembrane regulator (CFTR), is a protein modulator (US 20200377491 Al, example 1).
    Navocaftor
  • HY-111111
    Galicaftor
    		Modulator 98.93%
    Galicaftor (ABBV-2222; GLPG-2222) is a potent and orally active cystic fibrosis transmembrane conductance regulator (CFTR) corrector. Galicaftor can be used for cystic fibrosis research.
    Galicaftor
  • HY-19778A
    BPO-27 racemate
    		Inhibitor 98.61%
    BPO-27 racemate is a potent CFTR inhibitor with an IC50 of 8 nM.
    BPO-27 racemate
  • 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-109177
    Icenticaftor
    		Activator 99.87%
    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.
    Icenticaftor
  • HY-109187A
    Posenacaftor sodium
    		Modulator 99.79%
    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-109027
    Cavosonstat
    		Modulator 99.36%
    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
  • HY-P1108A
    Astressin 2B TFA
    		Antagonist 99.35%
    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-145603A
    (R)-Vanzacaftor
    		Modulator 98.07%
    (R)-Vanzacaftor ((R)-VX-121) is a regulator of cystic fibrosis transmembrane conduction regulator (CFTR).
    (R)-Vanzacaftor
  • HY-106203A
    Crinecerfont hydrochloride
    		Antagonist 98.06%
    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. Crinecerfont (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Crinecerfont hydrochloride
  • HY-112267
    Olacaftor
    		Modulator 99.26%
    Olacaftor (VX-440) is a cystic fibrosis transmembrane conductance regulator (CFTR) modulator extracted from patent US9782408.
    Olacaftor
  • HY-119936
    GLPG2451
    		Activator 99.68%
    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.
    GLPG2451
  • HY-19970
    KM11060
    		Activator 98.71%
    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 research.
    KM11060
  • HY-P1106A
    K41498 TFA
    		Antagonist 99.40%
    K41498 TFA is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF2α, CRF2β and CRF1 receptors respectively. K41498 TFA is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF2α- and hCRF2β-expressing cells. K41498 TFA can be used for hypotension study.
    K41498 TFA
  • HY-143344
    NJH-2-056
    		Modulator 98.23%
    NJH-2-056 is a deubiquitinase-targeting chimera (DUBTAC) linking the OTUB1 recruiter EN523 to the CFTR chaperone lumacaftor. NJH-2-056 can be used for cystic fibrosis research.
    NJH-2-056
  • HY-155742
    CFTR corrector 12
    		Modulator 99.85%
    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-136939
    CFTR corrector 6
    		Activator 98.15%
    CFTR corrector 6 is a potent potentiator of Cystic Fibrosis Transmembrane conductance Regulator (CFTR). CFTR corrector 6 has the potential for cystic fibrosis (CF) and other CFTR associated disorders research.
    CFTR corrector 6
Cat. No. Product Name / Synonyms Application Reactivity