Cationic/Ionizable Lipids

As one of the major supplier in market, DC Chemicals provide more than 500 novel cationic ionizable lipids with wide range of diverse chemical structures for RNA delivery.

Cationic ionizable lipids play a major role in the LNP formulation and its ability to transfect target cells with its cargo. The ionizable lipids are used to complex negatively charged nucleic acid cargo. The mRNA-cationic lipid complex fuses with the cell membrane and is then delivered into the cytosol. To be able to play these roles efficiently, a cationic ionizable lipid must be engineered with a suitable apparent acid dissociation constant (pKa). The apparent pKa of a cationic ionizable lipid is the likely pKa at the LNP surface. Currently, the cationic ionizable lipids in FDA-approved therapeutics all have an apparent pKa between 6-7. This is crucial for the cationic ionizable lipid to maintain a neutral charge while in systemic circulation (pH above the pKa of the lipid, pH ~7.5), as well as its ability to become positively charged in the endosome (pH ~6.5) and facilitate membrane fusion and subsequent cytosolic release.

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Cat. No.	Product Name	Field of Application
DC65852	C3-K2-E14	C3-K2-E14 is an ionizable cationic lipid (pKa = 5.5).1 It has been used in the generation of lipid nanoparticles (LNPs) for the delivery of mRNA or siRNA in vitro and in vivo. LNPs containing C3-K2-E14 and encapsulating siRNA targeting the gene encoding colony-stimulating factor 1 (Csf1) reduce the percentage of circulating Ly6Chi monocytes and increase the percentage of circulating Ly6Cint monocytes in mice.
DC65853	(S)-C12-200	(S)-C12-200 is an ionizable cationic lipid (pKa = 7.12) and an isomer of C12-200 (Item No. 36699).1 It has been used in the formation of lipid nanoparticles (LNPs) for the delivery of mRNA in vivo. Intravenous administration of LNPs containing (S)-C12-200 and encapsulating mRNA encoding Cre recombinase increase the percentage of tdTomato+ hepatocytes, endothelial cells, and Kupffer cells in the livers of Ai14 mice greater than (R)-C12-200-containing and Cre mRNA-encapsulating LNPs.
DC65854	PPPDA-O16B	PPPDA-O16B is a disulfide bond-containing ionizable cationic lipid that has been used in the generation of lipid nanoparticles (LNPs) for plasmid delivery in vitro and in vivo.1 LNPs containing PPPDA-O16B and encapsulating plasmids encoding Ras/Rap1-specific endopeptidase (RRSP) increase RRSP levels and decrease Ras levels in, and reduce the viability of, HeLa cervical cancer cells. LNPs containing PPPDA-O16B and encapsulating plasmids encoding RRSP selectively localize to tumors over the heart, liver, spleen, lungs, and kidneys, as well as decrease tumor volume without reducing body weight, in an HCT116 colorectal cancer mouse xenograft model.
DC65856	Lipid C3	Lipid C3 is an ionizable cationic lipid (pKa = 5.05-5.671).1,2 It has been used in the formation of lipid nanoparticles (LNPs) for the delivery of mRNA in vitro and in vivo.1 Intracerebroventricular administration of LNPs containing lipid C3 and encapsulating mRNA encoding α-L-iduronidase (Idua) to neonates increase midbrain and hippocampal α-L-iduronidase enzyme activity and decrease forebrain, midbrain, and hippocampal glycosaminoglycan levels in an Idua-W392X mouse model of the lysosomal storage disorder mucopolysaccharidosis type I, also known as Hurler syndrome. Intracerebroventricular administration of LNPs containing lipid C3 and encapsulating an mRNA reporter to fetal macaques in utero increase brain GFP expression.
DC65857	BAmP-O16B	BAmP-O16B is an ionizable cationic amino lipid that has been used in the generation of lipid nanoparticles (LNPs).1 LNPs containing BAmP-O16B and encapsulating NSA-inactivated RNase A reduce the viability of SiHa and HeLa cancer cells, but not non-cancerous NIH3T3 and HEK293T cells, upon intracellular reactivation of RNase A by glutathione (GSH).
DC65858	Lipid OA2 (hydrochloride)	Lipid OA2 is an ionizable cationic lipid that has been used in the generation of single-component lipid nanoparticles (LNPs) for the delivery of siRNA.1 LNPs containing lipid OA2 and siRNA targeting the gene encoding suppressor of cytokine signaling 1 (Socs1) decrease Socs1 expression by approximately 50% in isolated mouse bone marrow dendritic cells (BMDCs). Vaccination with ovalbumin-induced isolated mouse BMDCs transfected with LNPs composed of lipid OA2 and Socs1-targeting siRNA increases survival and decreases tumor volume in a B16-OVA murine melanoma model.
DC60561	DB-lipidoid 11-10-8	DB-lipidoid 11-10-8 is a degradable branched (DB) lipidoid. 11-10-8 LNP is more potent than MC3 LNP at delivering mRNA. 11-10-8 LNP enables roughly five-fold higher TTR genome editing efficiency and therapeutic FGF21 protein expression compared to MC3 LNP.
DC60564	Lipid GVS-18-B6 Featured	Lipid GVS-18-B6 is a silicon ether ionizable lipid for mRNA delivery. GVS-18-B6 showes particularly good liver specificity, with a liver-to-spleen EGFP signal ratio of 92:1. GVS-18-B6 also showes rapid tissue clearance within 6 hours of dosing.
DC60566	Lipid CAD9 (3-A2-7b) Featured	Lipid CAD9 (3-A2-7b is a cationic degradable (CAD) lipid. 3-A2-7b formulated LNP, LNP-CAD9, can deliver FLuc mRNA to the lungs in vivo. LNP-CAD9 co-delivering Cas9 mRNA/VEGFR2 single guide RNA (sgRNA) effectively induces VEGFR2 knock out in lung endothelial cells of female mice.
DC60575	U-101 Featured	U-101 is an ionizable lipid for mRNA delivery. U-101-LNP/IL-2F mRNA formulation demonstrats effective antitumor activity and safety.LNPs containing lipid U-101 and encapsulating mRNA encoding a fusion protein composed of IL-2, a linker, and CD25 inhibit tumor growth in an MC-38 mouse xenograft model.
DC60578	TE-EP8-S	Lipid TE-EP8-S is a one-component ionizable cationic lipid for mRNA delivery to splenic T cells.
DC60579	Lipid B3 Featured	Lipid B3 is a biodegradable ionizable lipid for liver targeted delivery. Lipid B3-LNP shows high delivery efficacy and low toxicity in delivering RNA to liver cells.
DC66219	Lipid 88	Lipid 88 is an ionizable cationic lipid that has been used in the generation of lipid nanoparticles (LNPs) for the delivery of mRNA in vivo.1 LNPs containing lipid 88 and encapsulating mRNA encoding severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) spike glycoprotein increase anti-spike glycoprotein IgG titers in bronchoalveolar lavage fluid (BALF), as well as increase the percentage of CD8+, CD8+CD44+, CD4+, and CD4+CD44+ T cells in the lungs and spleen, in mice after two doses three weeks apart. LNPs containing lipid 88 and encapsulating mRNA expressing SARS-CoV-2 spike glycoprotein inhibit reductions in body weight, increase serum levels of anti-spike glycoprotein IgG and IgA titers, and reduce lung and nasal wash viral titers in a hamster model of SARS-CoV-2 Omicron BQ.1 subvariant infection.
DC60603	O12-D3-I3	O12-D3-I3 is an imidazole-based lipid for siRNA delivery. O12-D3-I3-LNPs encapsulating FVII siRNA (FVII@O-LNP) elicites greater gene silencing than those with the DLin-MC3-DMA (MC3) due to its stronger endosomal escape.
DC60605	Lipid 119-23 Featured	Lipid 119-23 is an ionizable lipid for mRNA delivery. 119-23 LNP exhibits an enhanced capability to express functional mCre in several categories of immune cells, spanning the liver, spleen and lung.
DC66508	BP Lipid 222	BP Lipid 222 BP Lipid 222 is an butanolamine ionizable lipid with both ester bonds located adjacent to C8 relative to the amine head. The introduction of ester linkages can improve the clearance of the lipid in the liver. This compound is analgous to ALC-0315 (BP-25498). The lipid can be used for mRNA-based therapies which depends on the availability of a safe and efficient delivery vehicle. Reagent grade, for research purpose. Please contact us for GMP-grade inquiries.
DC66509	BP Lipid 211	BP Lipid 211 is an ethanolamine ionizable lipid with 9 carbon of primary-ester lipid tail. The ethanolamine head helps with mRNA encapsulation. Both ester bonds are located at C10 position relative to the amine nitrogen. The introduction of ester linkages can improve the clearance of the lipid in the liver. Reagent grade, for research purpose.
DC66511	BP Lipid 309	BP Lipid 309 is an ionizable lipid analogue of ALC-0315 featuring a tertiary amine head, a central tertiary amine, and two identical esters linking to nonpolar tails. Ionizable lipids such as this may be applied in the development of lipid nanoparticles for drug discovery.
DC66512	BP Lipid 307	BP Lipid 307 is a multi-ionizable amino-lipid featuring a dimethylamine headgroup, a central tertiary amine, and two identical ester branches linking to saturated C17 tails. This compound may be employed in the development of lipid nanoparticles for drug delivery.
DC66513	BP Lipid 318	BP Lipid 318 is a lipid analog comprised of three unsaturated fatty acid tails and an ionizable dimethylamino butanoate head group. This lipid may be used in the generation of lipid nanoparticles (LNPs) for mRNA delivery.
DC66514	BP Lipid 316	BP Lipid 316 is an ionizable lipid analogue of DLin-MC3-DMA featuring a 4-(dimethylamino)butanoate head, two linoleic acid tails, and one primary alcohol. The alcohol may be used to further derivatize this compound. Ionizable lipids such as this may be applied in the development of lipid nanoparticles for drug discovery.
DC66515	BP Lipid 317	BP Lipid 317 is an amino lipid featuring a dimethylamine headgroup connected to two oleic esters and a hydroxy group which may be used for further derivatization. Ionizable lipids such as this may be applied in the development of lipid nanoparticles for drug discovery.
DC66516	BP Lipid 320	BP Lipid 320 is an ionizable amino lipid comprised of three oleic fatty acid tails and a novel pyrrolidine head group four carbon atoms in length. This lipid may be used in the generation of lipid nanoparticles (LNPs) for mRNA delivery.
DC66517	BP Lipid 315	BP Lipid 315 is a cationic ionizable lipid ALC-0315 analogue featuring a Boc-protected primary amine, a central tertiary amine, and two ester tails located at the C8 position relative to the amine. One of these esters features a symmetrical branched C17 tail, while the other is an asymmetric C11 tail. Ionizable lipids such as this may be applied in the development of lipid nanoparticles for drug discovery.
DC66518	BP Lipid 319	BP Lipid 319 is a multi-ionizable amino lipid analogue of ALC-0315 featuring a propylamino headgroup and two acyl tails, one being a branched symmetrical C17 and the other being an asymmnetrical C11 chain. Ionizable lipids such as this may be applied in the development of lipid nanoparticles.
DC66519	BP Lipid 312	BP Lipid 312 is a cationic ionizable lipid analogue of LP01, with the substitution of a polyunsaturated tail for a monounsaturated equivalent. Ionizable lipids such as this may be applied in the development of lipid nanoparticles for drug discovery.
DC66520	BP Lipid 311	BP Lipid 311 is a branched amino lipid featuring a dimethylamino headgroup, esters of a palmitoleic acid group and an aliphatic acetal. Ionizable lipids such as this may be applied in the development of lipid nanoparticles for drug discovery.
DC66521	BP Lipid 308	BP Lipid 308 has a terminal tertiary amine group, a linoleic group, and a 4,4-bis(octyloxy)butanoic acid sodium salt tail. This compound can be useful for the building or modification of lipid nanoparticles. Reagent grade, for research use only.
DC66522	BP Lipid 314	BP Lipid 314 is an ionizable amino lipid featuring a dimethylamino head group, a carbamate linking to a central tertiary carbon with two other branches, a linoleate ester, and an aliphatic acetal ester. A compound like this may be employed in the development of lipid nanoparticles for drug delivery.
DC66523	BP Lipid 310	BP Lipid 310 is an ionizable aminolipid analog of CL1. The structure features an ethanolamine head and an ester linking to a polyunsaturated hydrophobic tail. This lipid may be used to encapsulate nucleic acids or small-molecule drugs to form lipid nanoparticles for drug discovery.

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Cationic/Ionizable Lipids

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