DOSPA is a cationic lipid. The formulation of DNA with DOSPA is a very promising transfection system.

Loxoprofenol-SRS tromethamine (HR1405-01), an active metabolite of Loxoprofen, is a Safe intravenous non-steroidal anti-inflammatory drug (NSAID) with superior anti-inflammatory and analgesic activities.

Val-Cit-PAB-MMAF sodium is a drug-linker conjugate for ADC. Val-Cit-PAB-MMAF sodium contains the ADCs linker (peptide Val-Cit-PAB) and a potent tubulin polymerization inhibitor MMAF.

Val-Cit-PAB-MMAF is a drug-linker conjugate for ADC. Val-Cit-PAB-MMAF contains the ADCs linker (peptide Val-Cit-PAB) and a potent tubulin polymerization inhibitor MMAF.

Iu1-248, a derivative of IU1, is a potent and selective ubiquitin specific peptidase 14 (USP14) inhibitor with an IC50 of 0.83 μM.

EZM0414 is a potent, selective, and orally bioavailable inhibitor of Histone-lysine N-methyltransferase SETD2.

IMD-0560 is an Inhibitor of nuclear factor kappa-B kinase (IKK) which can suppress the production of inflammatory cytokines and chemokines.

Decanoic acid, 2-hexyl-, 6-oxohexyl ester-1 is a lipid product can be used for drug delivery.

Dlin-MeOH is a lipid product for use in drug delivery systems.

K145 is a selective, substrate-competitive and orally active sphingosine kinase-2 (SphK2) inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM in biochemical assays.

Amgen-23 (compound 23) is a potent sphingosine kinases (SPHK) inhibitor with IC50 values of 20 nM and 1.6 μM for SPHK1 and SPHK2, respectively. Amgen-23 can be used for researching anticancer.

Dioctadecylamine (DODA) is a secondary amine that has been shown to self-organize in plate-like structures in aqueous solution. Dioctadecylamine exhibits sufficiently hydrophobic properties of nanoparticles and good dispersibility in nonpolar solvent. Dioctadecylamine does not form a monolayer above pH 3.9.

DHAPC is a phospholipid that is very sensitive to oxidation.

Ionizable lipid A6 (di(dec-3-yn-1-yl) 9-((4-(dimethylamino) butanoyl)oxy) heptadecanedioate) was developed by modifying the backbone structure of Dlin-MC3-DMA through introducing alkynyl and ester groups into the lipid tails. Alkyne lipid A6 demonstrated a significant improvement in transfection efficiency (~8.5, ~2.0, and ~2.5-fold higher than the original MC3, C12-200 and cKK-E12 containing LNPs, respectively).The performance of the A6 coprepared into iLNPs with other amine-containing lipid materials (cKKE12) was evaluated, and the molar ratio of the formulation was changed to 35:16.0:46.5:2.5 (A6/cKKE12: DOPE: Chol: PEG). The results showed that these formulations synergistically facilitated more effective mRNA delivery and improved tolerability following single and repeated dosing. It was confirmed that albumin-associated macrophage phagocytosis and endocytosis is an apolipoprotein-independent cellular internalization pathway of iLNPs in the liver. According to the fusion kinetics, the lipids with highfrequency tail protrusion and high lateral diffusion coefficient can perturb and trigger membrane sprouting, which in turn promotes membrane fusion. The application of iLNPs with those lipids (such as A6) may be an effective method to further enhance the release of mRNA in vivo.

S-2302 is a Chromogenic substrate for plasma kallikrein, factor XIa and factor XIIa.

p-Cresol glucuronide is a metabolite of p-cresol, a uremic toxin formed by bacterial fermentation of proteins in the large intestine. It is formed from p-cresol primarily by the UDP-glucuronosyltransferase (UGT) isoform UGT1A6, but also by UGT1A9, in huma

113-O12B is a disulfide bond-containing ionizable cationic lipidoid. 113-O12B LNP, an LN-targeting LNP delivery system, is developed for a mRNA cancer vaccine. The 113-O12B/mRNA shows enhanced expression in APCs compared with ALC-0315/mRNA, indicating the LN-specific targeting ability.

306Oi10 is a branched-chain ionizable lipidoid and may be useful in the generation of lipid nanoparticles (LNPs). 306Oi10 ionizable lipids tail is isodecyl acrylate, affording the lipid tail a carbon branch, which confers significant improvement of the mRNA deliver efficiency. Compared with the straight-tailed 306O10, the 306Oi10 with carbon branches at the lipid tail generates more powerful surface ionization at late endosomal pH of 5.0 to improve the delivery efficiency of mRNA. The studies showed that 306Oi10 iLNPs significantly promoted mRNA expression in liver (more than 10- fold).306Oi10 iLNPs could induce stronger protein expression than two benchmark lipids, C12-200 and DLin-MC3-DMA. The total organ protein expression produced by 306Oi10 iLNPs was threefold higher than MC3 and over 20-fold higher expression than C12-200. The 306Oi10 iLNPs could codeliver three distinct mRNAs (luciferase, mCherry, and erythropoietin), or deliver Cas9 mRNA and single guide RNA (sgRNA) separately. Besides, 306Oi10 iLNPs have the potential of mRNA therapy for hepatocellular carcinoma, because they could target malignant hepatocytes, endothelial cells, and Kupffer cells simultaneously. To enable 306Oi10 iLNPs to deliver mRNA to extrahepatic organs, charged phospholipids were used in place of neutral phospholipids. The substitution of DOPE with DOTAP increased the positive surface charge of iLNPs at pH 7 about fivefold and changed the protein expression ratio of liver/lung from 36:1 to 1:56. Similarly, the substitution of DOPE with PS decreased the positive charge and changed the protein expression ratio of liver/spleen from 8:1 to 1:3. Further, the lung-target of DOTAP was better than that of neutral or anionic lipids, which might reduce immune cells infiltration in the lung.

PL1 is a novel biomimetic phospholipid. PL1 nanoparticle delivery of costimulatory receptor CD137 mRNA improved the immunotherapy with an anti-CD137 Ab to some extent in both tumor models with better results obtained in the B16F10 melanoma model as compared to the A20 lymphoma model.

OF-Deg-Lin is a biodegradable lipid containing an ester group, developed from the nonbiodegradable, linoleic acid derived OF-02; mRNA-LNPs containing OF-Deg-Lin showed high expression in the spleen. The ionizable lipid Of-Deg-Lin was synthesized, which possessed the similar chemical structure with OF-02.Both Of-Deg-Lin and OF-02 had diketopiperazine core and doubly unsaturated tails, and the difference between them was that Of-02 contained nondegradable 1,2-amino-alcohol linkages, whereas Of-Deg-Lin contained degradable ester linkages The change of linker altered iLNPs distribution and mRNA expression in vivo. Although the Of-Deg-Lin iLNPs could accumulate in the liver and spleen, they induced the expression of most functional proteins in B lymphocytes of spleen (over 85% of the total protein), not in the liver. Of-Deg-Lin iLNPs can deliver mRNA and express functional proteins in the spleen specifically, but the mechanism is unclear.

A2-Iso5-2DC18 is a top-performing lipid for mRNA delivery in bone marrow-derived dendritic cells (BMDCs), BMDMs and HeLa cells.

A18-Iso5-2DC18 that could not only deliver mRNA vaccines robustly but also activate the stimulator of interferon genes (STING) pathway. A18-Iso5-2DC18 strongly binds to the stimulator of interferon genes (STING) and induces potent cytolytic T lymphocyte responses, resulting in substantial antitumor immunity (Miao et al. 2019).