CFTR corrector 4
目录号: PL03448 纯度: ≥99%
CAS No. :1918142-34-3
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中文名称
CFTR corrector 4
英文名称
CFTR corrector 4
英文别名
1-(2,2-Difluoro-1,3-benzodioxol-5-yl)-N-[(2R,4R)-2-(3,4-dimethoxyphenyl)-3,4-dihydro-7-methoxy-2H-1-benzopyran-4-yl]cyclopropanecarboxamide
Cas No.
1918142-34-3
分子式
C29H27F2NO7
分子量
539.52
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
CFTR corrector 4,化合物 13,是一种有效的 (R,R) 型活性对映体,是一种高效且口服的囊性纤维化跨膜电导调节剂 (CFTR) 校正剂。CFTR corrector 4 可以增加细胞表面的 CFTR 水平,有潜力用于囊性纤维化的研究。
生物活性
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)
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2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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