Fig. 2: Dose-dependent activation of wildtype CFTR in primary human bronchial epithelial cells by two HDCF analogs. | npj Drug Discovery

Fig. 2: Dose-dependent activation of wildtype CFTR in primary human bronchial epithelial cells by two HDCF analogs.

From: A novel drug series optimized to address cystic fibrosis and other CFTR deficiency diseases of human airways

Fig. 2: Dose-dependent activation of wildtype CFTR in primary human bronchial epithelial cells by two HDCF analogs.

a Escalating doses of HDCF104 provide robust WT CFTR activation with EC50 = 4.16 μM (95% CI 2.748 μM to 5.572 μM). b Data summarized by dose-activity profile. c, d In similar fashion, escalating doses of uHTS159 demonstrate activation of WT CFTR with EC50 = 0.71 μM (95% CI 0.558 μM to 0.864 μM). Data is representative of 4 biological replicates and expressed as mean ± SD. Addition of amiloride (100 µM), forskolin (10 µM), inh-172 (10 µM), and UTP (stimulates non-CFTR chloride channels as a control for monolayer integrity; 100 µM) are shown. HBEC = primary human bronchial epithelial cells. Statistics were by use of GraphPad Prism 10 software with the function of Sigmoidal, 4PL, with X as concentration. Panels (a, c) plotted with Microsoft Excel; (b, d) plotted (and compound EC50 calculated) using GraphPad Prism 10 software; panels arranged and presented using Affinity Designer.

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