2. Membrane Transporter/Ion Channel
  3. CFTR

CFTR

CFTR

Related Products

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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.

CFTR Related Products (98):

Cat. No. Product Name Effect Purity
  • HY-13017
    Ivacaftor Agonist
    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-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.
  • HY-15206
    Glibenclamide Inhibitor 99.94%
    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].
  • 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[1][2][3][4].
  • HY-111772
    Elexacaftor Modulator 99.74%
    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[1].
  • 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).
  • HY-108772
    Crofelemer Modulator
    Crofelemer (Provir) is an orally active antidiarrheal agent. Crofelemer acts on the cystic fibrosis transmembrane conductance regulator (CFTR) and calcium-activated chloride channels (CACC) , which are responsible for chloride and fluid secretion in the gastrointestinal tract. Crofelemer can be used in the research of diarrheal diseases[1].
  • HY-106203C
    Crinecerfont tosylate Antagonist
    Crinecerfont tosylate is an effective orally active antagonist of the CRF1 receptor. Crinecerfont tosylate can be used in research on congenital adrenal hyperplasia (CAH)[1].
  • HY-13017A
    Ivacaftor benzenesulfonate Agonist
    Ivacaftor benzenesulfonate is an orally bioavailable CFTR potentiator, used for cystic fibrosis treatment.
  • HY-169000
    CFTR corrector 16 Modulator
    CFTR corrector 16 (Compound 39) is a corrector for cystic fibrosis transmembrane conductance regulator (CFTR), that can be used in research of cystic fibrosis disease[1].
  • HY-B0679
    Lubiprostone Activator
    Lubiprostone (SPI-0211; RU0211) increases intestinal fluid secretion through generation of CIC-2/CFTR and activation of cAMP signaling pathway. Lubiprostone inhibits myeloperoxidase (MPO) activity, downregulates Indomethacin (HY-14397)-induced iNOS and TNFα expression. Lubiprostone can be used for chronic constipation research[1][2][3].
  • HY-161753
    CFTR potentiator 1 Activator
    CFTR potentiator 1 (I1421) is a potent CFTR potentiator with an EC50 value of 64 nM. CFTR potentiator 1 allosterically activates a wide range of CF-causing mutants, such as ΔF508 and G551D CFTR[1].
  • 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[1].
  • HY-N6818R
    5,​7,​4'-​Trimethoxyflavone (Standard) Activator
    5,?7,?4'-Trimethoxyflavone (Standard) is the analytical standard of 5,?7,?4'-Trimethoxyflavone. This product is intended for research and analytical applications. 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[1][2][3].
  • 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[1][2][3].
  • 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[1].
  • HY-108575
    Chromanol 293B Inhibitor
    Chromanol 293B is a selective blocker of the slow delayed rectifier K+ current (IKs) with IC50 of 1-10 μM and a weak inhibitor of KATP channel. Chromanol 293B also blocks the CFTR chloride current with an IC50 of 19 μM[1].
  • 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[1].
  • HY-15448A
    (Rac)-Tezacaftor Modulator
    (Rac)-Tezacaftor ((Rac)-VX-661) is a racemate of Tezacaftor (HY-15448). Tezacaftor is a F508del CFTR corrector. (Rac)-Tezacaftor can be used for the research of cystic fibrosis[1].
  • 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[1].