| Bioactivity | 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]. | ||||||||||||
| Target | EC50:130 nM (CFTR) | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | CFTR corrector 4 | ||||||||||||
| CAS | 1918142-34-3 | ||||||||||||
| Formula | C29H27F2NO7 | ||||||||||||
| Molar Mass | 539.52 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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) |
CFTR corrector 4
CAS: 1918142-34-3 F: C29H27F2NO7 W: 539.52
CFTR corrector 4 (Compound 13), an active (R,R)-form enantiomer, is a highly potent and orally active cystic fibrosis tr
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