9-Octadecenoic acid (9Z)-, 1,1'-[7-[4-(dipropylamino)butyl]-7-hydroxy-1,13-tridecanediyl] ester

CL4H6 is an ionizable cationic amino lipid (apparent pK_a = 6.35) that has been used in the generation of lipid nanoparticles (LNPs).¹ LNPs containing CL4H6 and encapsulating Factor VII-targeting siRNA decrease hepatic levels of Factor VII in mice. Intravenous administration of LNPs containing CL4H6 and encapsulating siRNA targeting CD45 accumulate in tumor-associated macrophages and encapsulating siRNAs targeting STAT3 and HIF-1α decrease tumor volume in OS-RC-2 renal cancer mouse xenograft models.²

1. Sato, Y., Hashiba, K., Sasaki, K., et al. Understanding structure-activity relationships of pH-sensitive cationic lipids facilitates the rational identification of promising lipid nanoparticles for delivering siRNAs in vivo J. Control. Release 295,140-152(2019).
2. Shobaki, N., Sato, Y., Suzuki, Y., et al. Manipulating the function of tumor-associated macrophages by siRNA-loaded lipid nanoparticles for cancer immunotherapy J. Control. Release 325,235-248(2020).