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Cat. No. Product Name CAS No. Information
PC-60232

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.

Cystic Fibrosis

Phase 2 Clinical

PC-60231

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.

Cystic Fibrosis

Phase 2 Clinical

PC-35461

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.

Fibrosis

Phase 2 Clinical

PC-43442

VX-809

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.

Fibrosis

Phase 3 Discontinued

PC-43327

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).

Fibrosis

Approved

PC-43326

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).

Fibrosis

Approved

PC-43325

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).

Fibrosis

Approved

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