CFTR corrector 4

Modify Date: 2024-01-12 10:18:40

CFTR corrector 4 Structure
CFTR corrector 4 structure
Common Name CFTR corrector 4
CAS Number 1918142-34-3 Molecular Weight 539.52
Density N/A Boiling Point N/A
Molecular Formula C29H27F2NO7 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of CFTR corrector 4


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[1].

 Names

Name CFTR corrector 4

 CFTR corrector 4 Biological Activity

Description 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[1].
Related Catalog
Target

EC50:130 nM (CFTR)[1]

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[1]. 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[1].
References

[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) Corrector for the Treatment of Cystic Fibrosis.

 Chemical & Physical Properties

Molecular Formula C29H27F2NO7
Molecular Weight 539.52