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

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-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-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-13017S
    Ivacaftor-d9
    		Activator 99.83%
    Ivacaftor-d9 is a potent CFTR modulator and exhibits an EC50 value of 255 nM for CFTR potentiation in G551D/F508del HBE Cells. Ivacaftor-D9 acts as an orally active and improved deuterated Ivacaftor analog for cystic fibrosis research[1].
    Ivacaftor-d<sub>9</sub>
  • 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-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-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-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-14179
    PPQ-102
    		Inhibitor 99.73%
    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-145603A
    (R)-Vanzacaftor
    		Modulator 98.07%
    (R)-Vanzacaftor ((R)-VX-121) is a regulator of cystic fibrosis transmembrane conduction regulator (CFTR).
    (R)-Vanzacaftor
  • HY-19778A
    BPO-27 racemate
    		Inhibitor 98.50%
    BPO-27 racemate is a potent CFTR inhibitor with an IC50 of 8 nM.
    BPO-27 racemate
  • 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-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-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-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-13017S3
    Ivacaftor-d4
    		Agonist
    Ivacaftor-d4 (VX-770-d4) is the deuterium labeled-Ivacaftor (HY-13017). Ivacaftor is a potent and orally active CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with EC50s of 100 nM and 25 nM, respectively.
    Ivacaftor-d4
  • HY-15206S1
    Glyburide-d3
    		Inhibitor 99.24%
    Glyburide-d3 is the deuterium labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity[1]. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR)[3]. Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability[4]. Glibenclamide can induce autophagy[5].
    Glyburide-d<sub>3</sub>
  • HY-12129
    CP 154526 hydrochloride
    		Antagonist 99.76%
    CP 154526 hydrochloride is a potent, brain-penetrant and selective corticotropin-releasing factor receptor 1 (CRF1) antagonist with a Ki of 2.7 nM. CP 154526 hydrochloride shows selective for CRF1 over CRF2 (Ki = >10 μM). CP 154526 hydrochloride has anxiolytic activities.
    CP 154526 hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity