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-103369
    PG01
    		Activator ≥98.0%
    PG01 is a potent CFTR Cl- channel potentiator. PG01 can correct gating defects of CFTR mutants, is effective on b>E193K, G970R and G551D (CFTR mutants) with Kd values of 0.22 μM, 0.45 μM and 1.94 μM, respectively. PG01 is also effective on ΔF508 (Ka of 0.3 μM). PG01 increases ΔF508-CFTR Cl- current after adding Forskolin.
    PG01
  • HY-111772A
    (R)-Elexacaftor
    		Modulator 99.44%
    (R)-Elexacaftor is an enantiomer of Elexacaftor (HY-111772). (R)-Elexacaftor is the Compound 37 from patent WO2018107100A1. (R)-Elexacaftor is a modulator of cystic fibrosis transmembrane conductance regulator (CFTR), the EC50 for CFTR dF508 is 0.29 uM.
    (R)-Elexacaftor
  • HY-135279
    CFTR corrector 4
    		Modulator 99.60%
    CFTR corrector 4 (Compound 13), an active (R,R)-form enantiomer, is a highly potent and orally active cystic fibrosis transmembrane conductance regulator (CFTR) corrector. CFTR corrector 4 can increase CFTR levels at the cell surface and have the potential for treatment of cystic fibrosis.
    CFTR corrector 4
  • HY-125381
    CFTR corrector 2
    		Modulator 98.92%
    CFTR corrector 2 is a cystic fibrosis transmembrane conductance corrector (CFTR), extracted from patent US20140274933.
    CFTR corrector 2
  • HY-158002
    IDOR-4
    		Modulator 98.29%
    IDOR-4 is a type IV CFTR corrector. IDOR-4 restores F508del-CFTR trafficking to the cell surface.
    IDOR-4
  • HY-158991
    I1421
    		Agonist
    I1421 is an activator of the cystic fibrosis transmembrane conductance regulator (CFTR) with an EC50 of 64 nM for WT CFTR currents. I1421 also allosterically activates multiple mutants causing cystic fibrosis (CF) with good in vivo potency, with an oral bioavailability of 60% in mice corresponding to a half-life of 75 min. I1421 synergizes with Elexacaftor (HY-111772) to enhance CFTR currents.
    I1421
  • HY-N5101
    Kobusin
    		Activator 99.93%
    Kobusin is a bisepoxylignan isolated from the Pnonobio biondii Pamp. Kobusin is an activator of CFTR and CaCCgie chloride channels and a inhibitor of ANO1/CaCC (calcium-activated chloride channel) channel.
    Kobusin
  • HY-147249
    CFTR corrector 8
    		Modulator
    CFTR corrector 8 is a potent CFTR modulator. CFTR can be used in the research of cystic fibrosis.
    CFTR corrector 8
  • HY-13017A
    Ivacaftor benzenesulfonate
    		Agonist
    Ivacaftor benzenesulfonate is an orally bioavailable CFTR potentiator, used for cystic fibrosis treatment.
    Ivacaftor benzenesulfonate
  • HY-13017B
    Ivacaftor hydrate
    		Agonist
    Ivacaftor hydrate (VX-770 hydrate) is an orally bioavailable CFTR potentiator, used for cystic fibrosis treatment.
    Ivacaftor hydrate
  • HY-119179
    UCCF-853
    		Modulator 99.93%
    UCCF-853 is a CFTR modulator.
    UCCF-853
  • HY-106203
    Crinecerfont
    		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. 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.
    Crinecerfont
  • HY-133013
    GLPG-3221
    GLPG-3221 is a potent, orally active corrector of CFTR (cystic fibrosis transmembrane conductance regulator), with an EC50 of 105 nM. GLPG-3221 can be uesd for the treatment of cystic fibrosis.
    GLPG-3221
  • HY-109187
    Posenacaftor
    		Modulator
    Posenacaftor (PTI-801) is a cystic fibrosis transmembrane regulator (CFTR) protein modulator that corrects the folding and trafficking of CFTR protein. Posenacaftor is used for the research of cystic fibrosis (CF).
    Posenacaftor
  • HY-145126
    CP-628006
    		Activator
    CP-628006, a small molecule CFTR potentiator, restores ATP-dependent channel gating to the cystic fibrosis mutant G551D-CFTR.
    CP-628006
  • 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.
    CFTR potentiator 1
  • 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-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.
    (Rac)-Tezacaftor
  • 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
Cat. No. Product Name / Synonyms Application Reactivity