现货,Ivacaftor (VX-770),CAS号:873054-44-5,美国进口,跨膜转运体(T T) , CFTR , CFTR 抑制剂,selleck,S1144

信号转导通路: 跨膜转运体(T T) >> CFTR >> CFTR 抑制剂 >> Ivacaftor (VX-770)http://www.selleck.cn/vx-770-S1144.html

技术数据:

分子量(MW): 392.49

化学式:

C24H28N2O3

 

溶解度: DMSO ≥79mg/mL Water <1mg/mL Ethanol ≥4mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 873054-44-5

生物活性

 

 

Ivacaftor (VX-770) is a CFTR potentiator with an IC50 of 43 ± 38 nM. In recombinant cells Ivacaftor (VX-770) increased CFTR channel open probability (P(o)) in both the F508del processing mutation and the G551D gating mutation. Ivacaftor (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,Ivacaftor (VX-770) reduced excessive Na(+) and fluid absorption to prevent dehydration of the apical surface and increased cilia beating in these epithelial cultures. [1]

 

 

 

参考文献

Rescue of CF airway epithelial cell function in vitro by a CFTR potentiator, VX-770 Fredrick Van Goora,Sabine Hadida,et al. PNAS November 3, 2009;106:18825–18830

 

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