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CFTR (Cystic fibrosis transmembrane conductance regulator) is a membrane protein in vertebrates that is encoded by the CFTR gene. CFTR is an ABC transporter-class ion channel that conducts chloride and thiocyanate ions across epithelial cell membranes. Mutations of the CFTR gene affecting chloride ion channel function lead to dysregulation of epithelial fluid transport in the lung, pancreas and other organs, resulting in cystic fibrosis. Complications include thickened mucus in the lungs with frequent respiratory infections, and pancreatic insufficiency giving rise to malnutrition and diabetes. These conditions lead to chronic disability and reduced life expectancy. CFTR functions as a cAMP-activated ATP-gated anion channel, increasing the conductance for certain anions to flow down their electrochemical gradient. ATP-driven conformational changes in CFTR open and close a gate to allow transmembrane flow of anions down their electrochemical gradient. CFTR is an ion channel that evolved as a 'broken' ABC transporter that leaks when in open conformation.

Cat. No. Product Name CAS No. Information
GY03983

KM 11060

774549-97-2

A potent corrector of the F508del-CFTR trafficking defect that partially restores F508del trafficking and increases maturation significantly in BHK cells (10 nM for 24 h or 10 uM for 2 h); also can significantly increase plasma lipoxin A4 levels in F508del relevant to wildtype mice.

GY03957

Lumacaftor

936727-05-8

VX-809 (Lumacaftor, VRT 826809) is a potent CFTR corrector that increases F508del-CFTR-mediated chloride transport amd improves F508del-CFTR maturation in FRT cells with EC50 of 0.1 and 0.5 uM, respectively; improves F508del-CFTR processing in the endoplasmic reticulum and enhances chloride secretion to approximately 14% of non-CF human bronchial epithelial cells (EC50=81 nM); exhibits biochemical and functional characteristics similar to normal CFTR, including biochemical susceptibility to proteolysis, residence time in the plasma membrane, and single-channel open probability after F508del-CFTR corrected by VX-809.

GY07063

Corr4A

421580-53-2

Corr4A is a small molecule corrector of ΔF508-CFTR with IC50 of 6.0 uM.

GY05214

Olacaftor

1897384-89-2

Olacaftor (VX-440, VX440) is a next-generation CFTR corrector, shows the potential to enhance the amount of CFTR protein at the cell’s surface and for treatment of cystic fibrosis.

GY05212

GLPG-2222

1918143-53-9

GLPG-2222 (ABBV-2222, Galicaftor) is a novel potent and efficacious CFTR corrector with EC50 of 5 nM; is highly potent (5 nM) and efficacious in cells from multiple CF patient donors that have F508del homozygous mutation; shows potential in clinical trials in patients harboring the F508del CFTR mutation on at least one allele.

GY04100

Ivacaftor

873054-44-5

Ivacaftor (VX-770, VX770) is a potent, orally bioavailable CFTR potentiator, increases G551D- and F508del CFTR-mediated Cl- secretion with EC50 of 100 nM; increases CFTR channel open probability (Po) in both the F508del processing mutation and the G551D gating mutation in recombinant cells, increases the Po of G551D CFTR by 6-fold, the Po of F508del- and wild-type CFTR by 5-fold and 2-fold, respectively; also potentiates CFTR-mediated Cl− secretion in primary cultures of G551D/F508del HBE and F508del HBE; demonstrates potential for treatment of cystic fibrosis with certain mutations in CFTR gene (primarily the G551D mutation).

GY05362

Ivacaftor hydrate

1134822-07-3

Ivacaftor (VX-770, VX770) is a potent, orally bioavailable CFTR potentiator, increases G551D- and F508del CFTR-mediated Cl- secretion with EC50 of 100 nM; increases CFTR channel open probability (Po) in both the F508del processing mutation and the G551D gating mutation in recombinant cells, increases the Po of G551D CFTR by 6-fold, the Po of F508del- and wild-type CFTR by 5-fold and 2-fold, respectively; also potentiates CFTR-mediated Cl− secretion in primary cultures of G551D/F508del HBE and F508del HBE; demonstrates potential for treatment of cystic fibrosis with certain mutations in CFTR gene (primarily the G551D mutation).

GY05361

Ivacaftor benzenesulfonate

1134822-09-5

Ivacaftor (VX-770, VX770) is a potent, orally bioavailable CFTR potentiator, increases G551D- and F508del CFTR-mediated Cl- secretion with EC50 of 100 nM; increases CFTR channel open probability (Po) in both the F508del processing mutation and the G551D gating mutation in recombinant cells, increases the Po of G551D CFTR by 6-fold, the Po of F508del- and wild-type CFTR by 5-fold and 2-fold, respectively; also potentiates CFTR-mediated Cl− secretion in primary cultures of G551D/F508del HBE and F508del HBE; demonstrates potential for treatment of cystic fibrosis with certain mutations in CFTR gene (primarily the G551D mutation).

GY04294

CFTR Inhibitor II

328541-79-3

CFTR Inhibitor II is a potent CFTR inhibitor with Ki of 4.3 uM; rapidly and reversibly inhibited forskolin-induced hyperpolarization in nasal potential differences in mice; effectively reduces cholera toxin-induced intestinal fluid secretion in a closed-loop model of cholera.

GY04702

GLPG-1837

1654725-02-6

GLPG-1837 (ABBV-974) is a potent, orally available CFTR potentiator with EC50 of 3 nM and 339 nM on F508del and G551D CFTR, respectively; shows enhanced efficacy on CFTR mutants harboring Class III mutations compared to Ivacaftor.

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