Home Transmembrane Transporters CFTR

CFTR inhibitors/modulators

Cystic fibrosis transmembrane conductance regulator (CFTR),a cAMP-activated Cl channel, is expressed in epithelial cells in the airways, sweat duct, testis, pancreas,intestine and other fluid-transporting tissues. CFTR is related to cystic fibrosis which is a hereditary lethal disease.CFTR is a large transmembrane glycoprotein containing two six-helix membrane-spanning domains, each followed by a nucleotide-binding domain (NBD), with a regulatory domain linking the first NBDand the second membrane-spanning domain Cytosolic cAMP can activate CFTR by promoting CFTR phosphorylation and blocking CFTR dephosphorylation at the same time.

 

Other Transmembrane Transporters Inhibitors

CRM1 Calcium Channel Proton Pump P-gp Sodium Channel ATPase Potassium Channel CD markers GLUT Amino acid transporter
Cat.No. Product Name Information Product Use Citations Product Validations
S7059 Tezacaftor (VX-661) Tezacaftor (VX-661) is a second F508del CFTR corrector and is believed to help CFTR protein reach the cell surface. Phase 2.
Nucleic Acids Res, 2025, 53(13)gkaf675
Mol Ther Nucleic Acids, 2025, 36(4):102756
Cell Mol Life Sci, 2025, 82(1):109
Verified customer review of Tezacaftor (VX-661)
S1565 VX-809 (Lumacaftor) Lumacaftor (VX-809, VRT 826809) acts to correct CFTR mutations common in cystic fibrosis by increasing mutant CFTR (F508del-CFTR) maturation, EC50 of 0.1 μM in fisher rat thyroid cells. Phase 3.
Nucleic Acids Res, 2025, 53(13)gkaf675
Br J Pharmacol, 2025, 10.1111/bph.70176
iScience, 2025, 28(3):111942
Verified customer review of VX-809 (Lumacaftor)
S8851 VX-445 (Elexacaftor) Elexacaftor (VX-445) is a next-generation cystic fibrosis transmembrane conductance regulator (CFTR) corrector.This is a compound which is not chiral purity.
Nucleic Acids Res, 2025, 53(13)gkaf675
Mol Ther Nucleic Acids, 2025, 36(4):102756
Cell Mol Life Sci, 2025, 82(1):109
E1701 Vanzacaftor (VX-121) Vanzacaftor (VX-121) is an orally active corrector of Cystic fibrosis transmembrane conductance regulator (CFTR). Vanzacaftor improves the processing and trafficking of CFTR protein and increases chloride transport in combination with Tezacaftor and Deutivacaftor.
S1144 Ivacaftor (VX-770) Ivacaftor (VX-770) is a selective potentiator of CFTR targeting G551D-CFTR and F508del-CFTR with EC50 of 100 nM and 25 nM in fisher rat thyroid cells, respectively.
Nucleic Acids Res, 2025, 53(13)gkaf675
Cell Mol Life Sci, 2025, 82(1):109
JCI Insight, 2025, 10(9)e191098
Verified customer review of Ivacaftor (VX-770)
E1743 VX-561(CTP-656) VX-561 (CTP-656) is a potent CFTR modulator and exhibits an EC50 value of 255 nM for CFTR potentiation in G551D/F508del HBE cells.
S6003 Ataluren (PTC124) Ataluren (PTC124) selectively induces ribosomal read-through of premature but not normal termination codons, with EC50 of 0.1 μM in HEK293 cells, and may provide treatment for genetic disorders caused by nonsense mutations (e.g. CF caused by CFTR nonsense mutation). This compound is currently in Phase 3.
Int J Mol Med, 2025, 55(5)69
Stem Cell Reports, 2022, 17(10):2187-2202
Int J Mol Sci, 2022, 23(7)3541
Verified customer review of Ataluren (PTC124)
S7139 CFTRinh-172 CFTRinh-172 (CFTR inhibitor 172) is a voltage-independent, selective CFTR inhibitor with Ki of 300 nM, showing no effects on MDR1, ATP-sensitive K+ channels, or a series of other transporters.
Mol Ther Nucleic Acids, 2025, 36(4):102756
J Cyst Fibros, 2025, S1569-1993(25)01612-1
Nat Cancer, 2024, 10.1038/s43018-024-00731-2
Verified customer review of CFTRinh-172
S8698 GLPG1837 GLPG1837 (ABBV-974) is a novel CFTR potentiator with an EC50 value of 3 nM for F508del, showing enhanced efficacy on CFTR mutants harboring class III mutations compared to Ivacaftor.
Cell Mol Life Sci, 2024, 81(1):426
iScience, 2022, 25(1):103710
Int J Mol Sci, 2022, 23(18)10758
S8795 FDL169 FDL169 is a CFTR corrector that is designed to fix and restore the function of the defective CFTR protein.
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00158-2
J Pers Med, 2021, 11(7)643
JCI Insight, 2020, 5(18)139983