CL4H6|pH-sensitive cationic lipid|DC Chemicals

Cas No.:	2256087-35-9
Chemical Name:	[7-[4-(dipropylamino)butyl]-7-hydroxy-13-[(Z)-octadec-9-enoyl]oxytridecyl] (Z)-octadec-9-enoate
Synonyms:	[7-[4-(dipropylamino)butyl]-7-hydroxy-13-[(Z)-octadec-9-enoyl]oxytridecyl] (Z)-octadec-9-enoate
SMILES:	OC(CCCCCCOC(CCCCCCC/C=C\CCCCCCCC)=O)(CCCCCCOC(CCCCCCC/C=C\CCCCCCCC)=O)CCCCN(CCC)CCC
Formula:	C₅₉H₁₁₃NO₅
M.Wt:	916.532239675522
Purity:	>95%
Sotrage:	Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Publication:	[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.

Description:

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].

References:

[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.

MSDS

COA

LOT NO.	DOWNLOAD
2018-0101

Cat. No.	Product name	Field of application
DC58047	DSPE-PEG 2000	PEG2000-DSPE is used for creating micelles that are able to carry drugs with low solubility.
DC31000	LP-01	LP-01 is an ionizable cationic amino lipid (pKa = ~6.1). It has been used in the generation of lipid nanoparticles (LNPs). LNPs containing LP-01 and encapsulating both Cas9 mRNA and modified single-guide RNA (sgRNA) for the transport protein transthyretin (Ttr) induce gene editing in liver cells in mice in a dose-dependent manner resulting in reduced serum Ttr levels for at least 12 months.
DC60580	Endosidin5(ES5)	Endosidine 5 (ES5), is one of the most potent small molecules interferes with recycling endosomes through Annexin A6, thereby promoting the release and expression of mRNA into the cytoplasm. The delivered mRNAs is greatly enhanced via inhibition of endocytic recycling in cells and in live mice. NAV2729 (NAV) and endosidin 5 (ES5), resulted in significant enhancement (1.5–2 folds) of LNP-mediated delivery of Fluc mRNAs. Incubation of NAV and ES5 together caused modest further increases in Fluc expression in comparison to the sole application of either compound.
DC80021	DSPE-PEG2000-MAL	DSPE-PEG-MAL is one of the reactive phospholipid PEG reagents that can react with sulfhydryl group (mercaptan, -SH). DSPE (1, 2-distearyl-Sn-glycerol 3-phosphate ethanolamine) is a highly hydrophobic saturated 18C phospholipid.
DC57086	CL4H6	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].
DC60076	DEPC	DEPC, also known as DC22:1PC or SJN79954, is a phospholipid containing erucic acid at the sn-1 and sn-2 positions. DEPC is a useful reagent in drug formulation study. It has been used in the study of lipid membranes and to determine the effect of long-chain phospholipids on the secondary structure of human islet amyloid polypeptide (hIAPP).