包装: | 50mg |
规格: | 98% |
市场价: | 7497元 |
分子量: | 916.53 |
Background:
CL4H6 is a pH-sensitive cationic lipid. CL4H6 is the main component of lipid nanoparticles (LNPs), which can be used to target and deliver siRNA, and induces a potent gene-silencing response[1][2].
CL4H6 potent targeting of hepatocytes and endosomal escape, to safely and efficiently deliver a myocardin-related transcription factor/serum response factor (MRTF/SRF)-B siRNA into human conjunctival fibroblasts[2].
The optimized siRNA-loaded CL4H6-LNPs are selectively and efficiently taken up and showed strong gene silencing activity in tumor-associated macrophages (TAMs) in a human tumor xenograft model in nude mice. The anti-tumor therapeutic response is obtained through the silencing of the STAT3 and HIF-1α, which resulted in an increase in the level of infiltrated macrophage (CD11b+ cells) into the tumor-microenvironment (TME) as well as a tendency to increase the concentration of M1 macrophages (CD169+ cells). The treatment also resulted in reversing the pro-tumorous functions of TAMs -mainly angiogenesis and tumor cell activation-, as evidenced by a decrease in the related gene expression at the mRNA level[1].
[1]. Amisha Sanghani, et al. Novel PEGylated Lipid Nanoparticles Have a High Encapsulation Efficiency and Effectively Deliver MRTF-B siRNA in Conjunctival Fibroblasts. Pharmaceutics. 2021 Mar 13;13(3):382.
[2]. Nour Shobaki, et al. Manipulating the function of tumor-associated macrophages by siRNA-loaded lipid nanoparticles for cancer immunotherapy. J Control Release. 2020 Sep 10;325:235-248.