1918143-53-9

1918143-53-9 structure

Name: Galicaftor
Chemical Name: ABBV-2222 (GLPG2222)
CAS Number: 1918143-53-9
Molecular Formula: C₂₈H₂₁F₄NO₇
Molecular Weight: 559.46
Catalog: Signaling Pathways Membrane Transporter/Ion Channel CFTR
Create Date: 2018-06-26 22:28:24
Modify Date: 2025-08-27 16:54:29
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[1].

Name	ABBV-2222 (GLPG2222)
Synonyms	4-[(2R,4R)-4-({[1-(2,2-Difluoro-1,3-benzodioxol-5-yl)cyclopropyl]carbonyl}amino)-7-(difluoromethoxy)-3,4-dihydro-2H-chromen-2-yl]benzoic acid galicaftor

Description	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[1].
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> CFTR Research Areas >> Inflammation/Immunology
In Vitro	Galicaftor (ABBV-2222; GLPG-2222) exhibits potent in vitro functional activity in primary patient cells harboring F508del/F508del CFTR, with an EC50 <10 nM[2].
In Vivo	The rat pharmacokinetic tests are performed on Galicaftor (ABBV-2222; GLPG-2222; 1 mg/kg, i.v.; 1 mg/kg, p.o.) to illustrate its pharmacokinetic properties in rats. The T1/2 is 2.7 hours (i.v.). And for intragastric administration, the bioavailability (%F) is 74%[1].
References	[1]. Xueqing Wang, et al. Discovery of 4-[(2R,4R)-4-({[1-(2,2-Difluoro-1,3-benzodioxol-5-yl)cyclopropyl]carbonyl}amino)-7-(difluoromethoxy)-3,4-dihydro-2H-chromen-2-yl]benzoic Acid (ABBV/GLPG-2222), a Potent Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Corrector for the Treatment of Cystic Fibrosis. J Med Chem. 2018 Feb 22;61(4):1436-1449. [2]. Ashvani K Singh, et al. Biological Characterization of F508delCFTR Protein Processing by the CFTR Corrector ABBV-2222/GLPG2222. J Pharmacol Exp Ther. 2020 Jan;372(1):107-118.