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Galicaftor

Names

[ CAS No. ]:
1918143-53-9

[ Name ]:
Galicaftor

[Synonym ]:
Benzoic acid, 4-[(2R,4R)-4-[[[1-(2,2-difluoro-1,3-benzodioxol-5-yl)cyclopropyl]carbonyl]amino]-7-(difluoromethoxy)-3,4-dihydro-2H-1-benzopyran-2-yl]-
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

Biological Activity

[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.

Chemical & Physical Properties

[ Density]:
1.6±0.1 g/cm3

[ Boiling Point ]:
701.1±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C28H21F4NO7

[ Molecular Weight ]:
559.46

[ Flash Point ]:
377.8±32.9 °C

[ Exact Mass ]:
559.125427

[ LogP ]:
6.05

[ Vapour Pressure ]:
0.0±2.3 mmHg at 25°C

[ Index of Refraction ]:
1.640