O-2545 is a potent water-soluble central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptor agonist with Ki values of 1.5 and 0.32 nM, respectively. Typically, cannabinoid agonists are highly lipophilic and require solubilization through surfactant agents or binding to water miscible substances like albumin, Tween80, or Emulphor for use. When dissolved in saline, O-2545 has shown high efficacy in mouse behavioral models, administered either intravenously or intracerebroventricularly.
OH-Chol is a cationic cholesterol derivative.1 OH-Chol, as a component of lipoplexes with DOPE , has been used for siRNA delivery and gene silencing in MCF-7 cells, as well as in mice via intravenous injection, resulting in lipoplex accumulation in the liver. It has also been used in cationic nanoparticles in combination with Tween80 to transfect pDNA and siRNA into PC3 mouse xenografts via intratumoral injection and with Tween80 and folate-PEG2000-DSPE in a KB mouse xenograft model for intratumoral gene delivery.2References1. Hattori, Y., Nakamura, M., Takeuchi, N., et al. Effect of cationic lipid in cationic liposomes on siRNA delivery into the lung by intravenous injection of cationic lipoplex. J. Drug. Target 27(2), 217-227 (2019).2. Hattori, Y. Development of non-viral vector for cancer gene therapy. Yakugaku Zasshi 130(7), 917-923 (2010). OH-Chol is a cationic cholesterol derivative.1 OH-Chol, as a component of lipoplexes with DOPE , has been used for siRNA delivery and gene silencing in MCF-7 cells, as well as in mice via intravenous injection, resulting in lipoplex accumulation in the liver. It has also been used in cationic nanoparticles in combination with Tween80 to transfect pDNA and siRNA into PC3 mouse xenografts via intratumoral injection and with Tween80 and folate-PEG2000-DSPE in a KB mouse xenograft model for intratumoral gene delivery.2 References1. Hattori, Y., Nakamura, M., Takeuchi, N., et al. Effect of cationic lipid in cationic liposomes on siRNA delivery into the lung by intravenous injection of cationic lipoplex. J. Drug. Target 27(2), 217-227 (2019).2. Hattori, Y. Development of non-viral vector for cancer gene therapy. Yakugaku Zasshi 130(7), 917-923 (2010).