Galicaftor

Modify Date: 2024-01-28 17:32:08

Galicaftor Structure
Galicaftor structure
Common Name Galicaftor
CAS Number 1918143-53-9 Molecular Weight 559.46
Density 1.6±0.1 g/cm3 Boiling Point 701.1±60.0 °C at 760 mmHg
Molecular Formula C28H21F4NO7 Melting Point N/A
MSDS N/A Flash Point 377.8±32.9 °C

 Use of Galicaftor


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].

 Names

Name ABBV-2222 (GLPG2222)
Synonym More Synonyms

 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
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

 Synonyms

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