CFTR corrector 4 (Compound 13), an active (R,R)-form enantiomer, is a highly potent and orally active cystic fibrosis transmembrane conductance regulator (CFTR) corrector. CFTR corrector 4 can increase CFTR levels at the cell surface and have the potential for treatment of cystic fibrosis.
性状
Solid
IC50 & Target[1][2]
EC50:130 nM (CFTR)
体外研究(In Vitro)
CFTR corrector 4 possesses high potency and efficacy with a EC50 of 0.028 μM in this HBE-TECC assay that assess the CFTR function, this lead resides in undesirable drug-like space with high molecular weight, and high HPLC Log D, indicating high lipophilicity. HBE-TECC: (Human Bronchial Epithelial-Trans-Epithelial Current Clamp) assay.CFTR corrector 4 is tested its potency and efficacy in human bronchial epithelial (HBE) cells with a EC50 value 130 nM in the cell surface expression (CSE-HRP) assay. 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
参考文献
[1]. Wang X, 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)