Cationic Lipids & Ionizable Lipids
The molecular architecture of cationic lipids used as nucleic acid carriers is similar to that of natural lipids, with the major difference being their cationic head group, so cationic lipids have the ability to form aggregate complexes with anionic nucleic acids such as DNA or RNA. Advantages of cationic lipid-mediated transfection include high efficiency, ability to transfect a wide range of cell types, reproducibility, and simplicity.
Ionizable cationic lipids (including DOTMA, DODAP, DLin-KC2-DMA, and D-Lin-MC3-DMA) are pH sensitive and highly effective for in vivo transfection. These ionizable cationic lipids are positively charged at low pH (the ability to complex nucleic acids), but mostly uncharged at the pH of blood (pH 7.4) (slow elimination and good tolerability). The ionizable cationic lipids shape and acid-dissociation constant optimization dramatically improved lipid nanoparticles (LNPs) potency, thereby enabling clinical translation.
- Formula: C36H72INO6
- Molecular Weight: 741.86
DMDHP ((±)-Dimyristoyl-2,3-dimethylhydroxypropylamine) is a cationic lipid with a polar head group containing a dihydroxy group. DMDHP exhibits superior transfection efficiency and lower toxicity at high DNA doses in mouse intrapulmonary transfection model. DMDHP is commonly used for gene delivery.
- Formula: C55H115N5O5
- Molecular Weight: 926.53
C9-200 is an ionizable cationic lipid that has been used in the formation of lipid nanoparticles (LNPs). C9-200-based LNPs encapsulating mRNA encoding erythropoietin (EPO) can induced EPO production and stimulate red blood cell production in mice.
- Formula: C42H76ClNO4
- Molecular Weight: 694.51
18:2 TAP (chloride) is a cationic lipid .
- Formula: C48H95NO5
- Molecular Weight: 766.29
((1-Hydroxybutan-2-yl)azanediyl)bis(hexane-6,1-diyl) bis(2-hexyldecanoate) is an ionizable cationic lipid (pKa = 4.67) and a derivative of ALC-0315).
- Formula: C40H79NO7S
- Molecular Weight: 718.12
16:0 SB (DPSB) is a fixed cationic lipid.
- Formula: C52H98NO10P
- Molecular Weight: 928.31
DOPE-C8 (1,2-Dioloeoyl-sn-glycero-3-phosphoethanolamine-C8; 1,2-DOPE-C8) is a zwitterionic phospholipid derived from DOPE that has been used to generate lipid nanoparticles (LNPs) for in vivo delivery of mRNA.
- Formula: C45H87N3O4S
- Molecular Weight: 766.25
CP-LC-0743 is an ionizable cationic amino lipid efficient delivery of different kinds of RNA (mRNA, cRNA and saRNA).
- Formula: C49H98INO5
- Molecular Weight: 908.21
- Formula: C50H93N3O6
- Molecular Weight: 832.29
LNP Lipid-182 can be employed in the development of lipid nanoparticles (LNPs).
- Formula: C59H113N3O8S3
- Molecular Weight: 1088.74
CP-LC-1073 is a specific ionizable cationic amino lipid derived from the amino acid homocysteine. CP-LC-1073 can used in lipid nanoparticle (LNP) formulations for efficient in vivo delivery and expression of RNA (mRNA, cRNA, saRNA).
- Formula: C26H48N2O4
- Molecular Weight: 452.67
THP1 Lipid is an ionizable lipidoid. THP1 Lipid can be used to synthesize lipid nanoparticles (LNPs) for delivering mRNA to muscles with minimal toxicity and editing genes in specific liver tissues in tdTomato transgenic mice model. THP1 Lipid can be used for vaccine delivery and CRISPR/Cas9-mediated gene editing research.
- Formula: C59H116N4O2
- Molecular Weight: 913.58
BCP-NC2-C12 is an ionizable cationic lipid. BCP-NC2-C12 can be used to generate lipid nanoparticles (LNPs) for in vivo delivery of mRNA. BCP-NC2-C12 LNPs mediated an approximately 90% reduction in PCSK9 serum protein levels via CRISPR/Cas9 gene knockout.
- Formula: C55H100N4O8S3
- Molecular Weight: 1041.60
CP-LC-1447 is an ionizable cationic amino lipid derived from homocysteine.
- Formula: C60H118N2O5
- Molecular Weight: 947.59
LNP Lipid II-10 can be used in the development of lipid nanoparticles (LNPs).
- Formula: C56H100N2O8
- Molecular Weight: 929.40
MeDZ lipid is a zwitterion-type ionizable endosomal membrane destabilizer and anti-inflammatory agent that promotes endosomal escape. When incorporated into LNP formulations, MeDZ lipid enhances mRNA expression in lymph node antigen-presenting cells and promotes cytotoxic T cell activation. MeDZ lipid is compatible with existing targeted nanoparticle formulations to improve mRNA delivery efficiency.
- Formula: C43H79N3O4
- Molecular Weight: 702.11
DLin-C-DAP is a cationic lipid that can be used to prepare lipid nanoparticles (LNPs) for drug delivery.
- Formula: C64H126N2O5
- Molecular Weight: 1003.70
LNP Lipid-12 can be exploited for creating lipid nanoparticles (LNPs).
- Formula: C59H110N2O5
- Molecular Weight: 927.52
IR-117-17 is an ionizable cationic amino lipid, targeting conducting airways of the lung. IR-117-17 could be degraded via esterase cleavage and thus be unlikely to accumulate upon repeated dosing. It can be used in research related to diseases that manifest outside alveolar spaces.
- Formula: C45H85NO7
- Molecular Weight: 752.16
Lipid 7-1 is an ionizable cationic lipid that can be used for the preparation of liposomes.
