VX-770/VX770

VX-770/VX770

VX-770/VX770

编号ABP000259 化学名称VX-770/VX770 CAS873054-44-5 分子式C24H28N2O3 分子量392.4907 纯度 >99%

化学名称 : VX-770/VX770

CAS : 873054-44-5

英文名称: VX-770/VX770

英文同义词: N-[2,4-Bis(tert-butyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxo-3-quinolinecarboxamide

溶解度:DMSO

储存条件:at -20℃ 2 years

生物活性

VX-770 is a CFTR potentiator with an IC50 of 43 ± 38 nM. In recombinant cells VX-770 increased CFTR channel open probability (P(o)) in both the F508del processing mutation and the G551D gating mutation. VX-770 also increased Cl(-) secretion in cultured human CF bronchial epithelia (HBE) carrying the G551D gating mutation on one allele and the F508del processing mutation on the other allele by approximately 10-fold, to approximately 50% of that observed in HBE isolated from individuals without CF. Furthermore, VX-770 reduced excessive Na(+) and fluid absorption to prevent dehydration of the apical surface and increased cilia beating in these epithelial cultures.

参考文献

[1] Van Goor F et al. Proc Natl Acad Sci U S A. 2009 Nov 3;106(44):18825-30

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