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-161895
    CFTR corrector 14
    Modulator
    CFTR corrector 14 (Compound SVQ26) is a class 3 corrector for cystic fibrosis transmembrane conductance regulator (CFTR), that promotes the CFTR activity (EC50 of 3.08 μM with presence of C1 class corrector VX-809). CFTR corrector 14 regulates the mutant-caused misfolding and impaired function of the CFTR protein. CFTR corrector 14 can be used in research about cystic fibrosis.
    CFTR corrector 14
  • HY-164037
    Riselcaftor
    Modulator
    Riselcaftor (Example 33) is a CFTR modulator, with an EC50 of 20.1 nM in human bronchial epithelial cells. Riselcaftor can be used for research of cystic fibrosis.
    Riselcaftor
  • HY-158144
    GLPG2737
    Modulator
    GLPG2737 is a potent CFTR type 2 corrector, and GLPG2737 can be used in combination with a type 1 co-corrector in the study of cystic fibrosis.
    GLPG2737
  • HY-112363
    Aloisine A
    Activator
    Aloisine A (RP107) is a a potent cyclin-dependent kinase (CDK) inhibitor with IC50s of 0.15 μM, 0.12 μM, 0.4 μM, 0.16 μM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK5/p35, respectively. Aloisine A ininhibits GSK-3α (IC50=0.5 μM) and GSK-3β (IC50=1.5 μM). Aloisine A stimulates wild-type CFTR and mutated CFTR, with submicromolar affinity by a cAMP-independent mechanism. Aloisine A has the potential for CFTR-related diseases, including cystic fibrosis research.
    Aloisine A
  • HY-114725
    VRT-532
    Modulator 98.98%
    VRT-532 (CFpot-532) is a potent is a potent CFTR modulator. VRT-532 enhances channel activity in G551D-CFTR and intrinsic ATPase activity of G551D-CFTR. VRT-532 has the potential for the research of cystic fibrosis.
    VRT-532
  • HY-161894
    CFTR corrector 13
    Modulator
    CFTR corrector 13 (SVQ18) is a cystic fibrosis transmembrane conductance regulator (CFTR) corrector (EC50=3.14 μM). CFTR corrector 13 enhances the function of CFTR channels, especially when used in combination with Lumacaftor (HY-13262), it can produce a dose-dependent increase in CFTR function. CFTR corrector 13 can be used in the study of cystic fibrosis (CF) and other CFTR-related diseases.
    CFTR corrector 13
  • HY-15206R
    Glibenclamide (Standard)
    Inhibitor
    Glibenclamide (Standard) is the analytical standard of Glibenclamide. This product is intended for research and analytical applications. 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 (Standard)
  • HY-172555
    CFTR corrector 18
    Modulator
    CFTR corrector 18 (Compound I-99) is a cystic fibrosis transmembrane conductance regulator (CFTR) corrector. CFTR corrector 18 facilitates the processing and trafficking of CFTR, increasing the number of CFTR on the cell surface. CFTR corrector 18 is promising for research of cystic fibrosis (CF).
    CFTR corrector 18
  • 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-112267A
    (R)-Olacaftor
    Modulator 98.07%
    (R)-Olacaftor ((R)-VX-440) is a Cystic fibrosis transmembrane conductance regulator (CFTR) modulator. (R)-Olacaftor has good potential for the study of cystic fibrosis (CF).
    (R)-Olacaftor
  • HY-174821
    VU439
    Modulator
    VU439 is a functionalized photoaffinity ligand of Elexacaftor (HY-111772). VU439 retains the activity of Elexacaftor as a CFTR corrector and can identify SCCPDH as a specific off-target of Elexacaftor through chemoproteomics.
    VU439
  • HY-B1125R
    Glucosamine (Standard)
    Isomogroside V (Standard) is the analytical standard of Isomogroside V. This product is intended for research and analytical applications. Isomogroside V is a sweetener, which extracted from Siraitia grosvenorii (Swingle).
    Glucosamine (Standard)
  • HY-106203B
    (R)-Crinecerfont
    Antagonist
    (R)-Crinecerfont is the R-enantiomer of Crinecerfont (HY-106203). Crinecerfont (SSR-125543) is an orally effective corticotropin-releasing factor receptor type-1 (CRF1 receptor) antagonist. Crinecerfont blocks CRF1 receptor signaling to reduce adrenocorticotropic hormone secretion. Crinecerfont improves hypothalamic-pituitary-adrenal axis negative feedback sensitivity in chronically stressed mice. Crinecerfont can be used for the research of chronic stress conditions and classic congenital adrenal hyperplasia due to 21-hydroxylase deficiency. Crinecerfont is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    (R)-Crinecerfont
  • HY-147315
    CFTR corrector 9
    Modulator 98.84%
    CFTR corrector 9 (compound 42) is a cystic fibrosis transmembrane conductance regulator (CFTR) modulator. CFTR corrector 9 can be used for researching cystic fibrosis (CF) and other CFTR associated disorders.
    CFTR corrector 9
  • HY-106203C
    Crinecerfont tosylate
    Antagonist
    Crinecerfont (SSR-125543) tosylate is an orally effective corticotropin-releasing factor receptor type-1 (CRF1 receptor) antagonist. Crinecerfont tosylate blocks CRF1 receptor signaling to reduce adrenocorticotropic hormone secretion. Crinecerfont tosylate improves hypothalamic-pituitary-adrenal axis negative feedback sensitivity in chronically stressed mice. Crinecerfont tosylate can be used for the research of chronic stress conditions and classic congenital adrenal hyperplasia due to 21-hydroxylase deficiency. Crinecerfont tosylate 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 tosylate
  • HY-116806
    AF-2785
    Inhibitor
    AF-2785 is a potent CFTR blocker. AF-2785 inhibits the cAMP-activated chloride current in rat epididymal cells with an IC50 of 170.6 μM. AF-2785 can be used in research related to contraceptives.
    AF-2785
  • HY-177313
    AAG561
    Antagonist
    AAG561 is a corticotropin-releasing factor receptor 1 (CRF1) antagonist. AAG561 can be used for the study of the underlying emotion dysregulation of a mental disease or disorder.
    AAG561
  • HY-P3597
    Urocortin III (mouse) free acid
    Agonist
    Urocortin III (mouse) (free acid) is a selective CRF2 receptor agonist (with high affinity for the CRF2 receptor). Urocortin III (mouse) (free acid) significantly inhibits gastric emptying without modifying colonic transit.
    Urocortin III (mouse) free acid
  • HY-148806
    Zatonacaftor
    Modulator
    Zatonacaftor is a modulator of cystic fibrosis transmembrane regulator (CFTR) protein. Zatonacaftor can be used for research of cystic fibrosis.
    Zatonacaftor
  • HY-P10806
    kCAL01
    Inhibitor
    kCAL01 is a CAL inhibitor with a Ki value of 2.3 μM. kCAL01 is promising for research of cystic fibrosis (CF).
    kCAL01
Cat. No. Product Name / Synonyms Application Reactivity