114.Comparative pharmacokinetic profile of cyclosporine (CsA) with a decapeptide and a linear analogue

David A. Price,*Heather Eng,   Kathleen A. Farley,b Gilles H. Goetz,  Yong Huang, Zhaodong Jiao,  Amit S. Kalgutkar,  Natasha M. Kablaoui, Bhagyashree Khunte,  Spiros Liras,  Chris Limberakis， Alan M. Mathiowetz,  Roger B. Ruggeri,Jun-Min Quan  and  Zhen Yang

Org. Biomol. Chem. 2017, 15, 2501

The synthesis and in vivo pharmacokinetic profile of an analogue of cyclosporine is disclosed. An acyclic congener was also profiled in in vitro assays to compare cell permeability. The compounds possess similar calculated and measured molecular descriptors however have different behaviors in an RRCK assay to assess cell permeability.