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.
性状
Solid
体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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 T 1/2 is 2.7 hours (i.v.). And for intragastric administration, the bioavailability (%F) is 74%. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[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 [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.
溶解度数据
In Vitro: DMSO : 50 mg/mL (89.37 mM; Need ultrasonic)配制储备液