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-106203
    Crinecerfont
    		Antagonist 98.08%
    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.
    Crinecerfont
  • HY-B1153A
    Glafenine hydrochloride
    		Activator 99.03%
    Glafenine (Glafenin) hydrochloride is a non-selective, non-steroidal anti-inflammatory drug-based COX-1/COX-2 inhibitor. Glafenine hydrochloride exerts anti-inflammatory, anti-proliferative and anti-cell migration effects by inhibiting the arachidonic acid metabolic pathway and reducing prostaglandin synthesis. Glafenine hydrochloride can induce cell cycle arrest in vascular smooth muscle cells and endothelial cells and reduce the synthesis of the extracellular matrix protein Tenascin. Glafenine hydrochloride can be used in the research of inflammatory-related diseases, vascular restenosis and cystic fibrosis (CF).
    Glafenine hydrochloride
  • HY-N2057
    Steviol
    		Inhibitor 99.85%
    Steviol is the main metabolite of steviol glycosides and an inhibitor of AQP2/CFTR. Steviol slows down the growth of renal cysts by inhibiting the activity of CFTR, reducing the expression of AQP2, and promoting the degradation of AQP2 and CFTR. Steviol can be used in the research of polycystic kidney disease.
    Steviol
  • 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
  • HY-115878
    NJH-2-057
    		Modulator 98.84%
    NJH-2-057 is an EN523 OTUB1 recruiter linked to lumacaftor, a agent used to treat cystic fibrosis that binds ΔF508-CFTR.
    NJH-2-057
  • HY-145603A
    (R)-Vanzacaftor
    		Modulator 98.02%
    (R)-Vanzacaftor ((R)-VX-121) is a Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) modulator with max activity of 30-60% and EC50 <1 μM in enteroid cells. (R)-Vanzacaftor can be used for the research of cystic fibrosis.
    (R)-Vanzacaftor
  • HY-109177
    Icenticaftor
    		Activator 99.66%
    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-111099
    GLPG1837
    		Agonist 99.87%
    GLPG1837 is a potent and reversible CFTR potentiator, with EC50s of 3 nM and 339 nM for F508del and G551D CFTR, respectively.
    GLPG1837
  • HY-18337
    IOWH-032
    		Inhibitor 99.63%
    IOWH-032 is a a synthetic anti-secretory molecule, is a potent CFTR inhibitor with an IC50 value of 8 μM. IOWH-032 also is a anti-diarrheal agent.
    IOWH-032
  • HY-15206S1
    Glyburide-d3
    		Inhibitor 99.64%
    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-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-111680
    Nesolicaftor
    		Modulator 99.37%
    Nesolicaftor (PTI-428) is a specific cystic fibrosis transmembrane conductance regulator (CFTR) amplifier.
    Nesolicaftor
  • HY-P1106A
    K41498 TFA
    		Antagonist 98.71%
    K41498 TFA is a highly selective CRF 2 receptor antagonist, with a Ki of 0.66 nM for human CRF2α receptor and a Ki of 0.62 nM for human CRF2β receptor. K41498 TFA inhibits cAMP accumulation in cells expressing CRF2. K41498 TFA antagonizes the hypotensive response induced by systemic administration of urocortin in conscious rats. K41498 TFA undergoes radioiodination without loss of activity and serves for autoradiographic studies of native CRF2 receptors in rat brain and peripheral tissues.
    K41498 TFA
  • HY-158002
    IDOR-4
    		Modulator
    IDOR-4 is a type IV CFTR corrector. IDOR-4 restores F508del-CFTR trafficking to the cell surface.
    IDOR-4
  • HY-111111
    Galicaftor
    		Modulator 98.56%
    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-106203A
    Crinecerfont hydrochloride
    		Antagonist 98.82%
    Crinecerfont (SSR-125543) hydrochloride is an orally effective corticotropin-releasing factor receptor type-1 (CRF1 receptor) antagonist. Crinecerfont hydrochloride blocks CRF1 receptor signaling to reduce adrenocorticotropic hormone secretion. Crinecerfont hydrochloride improves hypothalamic-pituitary-adrenal axis negative feedback sensitivity in chronically stressed mice. Crinecerfont hydrochloride can be used for the research of chronic stress conditions and classic congenital adrenal hyperplasia due to 21-hydroxylase deficiency. 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-150089
    SRI-37240
    		Modulator 98.29%
    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-109187A
    Posenacaftor sodium
    		Modulator 99.69%
    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-158991
    I1421
    		Agonist 99.15%
    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
Cat. No. Product Name / Synonyms Application Reactivity