GLPG2451 是一种囊性纤维化跨膜电导调节器 (CFTR) 的增强剂,有效增强低温挽救的 F508del CFTR,EC50 为 11.1 nM。
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GLPG2451 is a cystic fibrosis transmembrane conductance regulator (CFTR) potentiator, which effectively potentiates low temperature rescued F508del CFTR with an EC50 of 11.1 nM[1]. Cystic fibrosis transmembrane conductance regulator[1]
GLPG2451 has an EC50 value of 675 nM and an efficacy level of 147% of that of VX770 in G551D/F508del cells[1].
[1]. Gees M, et al. Identification and Characterization of Novel CFTR Potentiators. Front Pharmacol. 2018 Oct 26;9:1221.
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