lipid 5

Lipid 5, an amino lipid compound, demonstrates proficient mRNA delivery in rodent and primate models, with favorable pharmacokinetics and minimal toxicity.

LNP Lipid-5 is an ionizable lipid (amino lipid) used in the formulation of lipid nanoparticles (LNP).

3D-Monophosphoryl Lipid A-5 (free acid) is a TLR agonist used as an adjuvant in vaccines to enhance their immunogenicity.

3D-Monophosphoryl Lipid A-5 (3D-MPLA-5) triethylamine is a TLR agonist that acts as an adjuvant for vaccines, enhancing their immunogenicity.

3D-Monophosphoryl Lipid A-5 (3D-MPLA-5) is a TLR agonist that can serve as an adjuvant in vaccines to enhance their immunogenicity.

Lipid TD5, an ionizable cationic lipid (pKa = 7.3), is utilized in the creation of lipid nanoparticles (LNPs) for mRNA delivery both in vitro and in vivo. These LNPs are internalized via endocytosis in a serotonin (5-HT) receptor subtype 1A-dependent manner in primary mouse astrocytes. When administered intrathecally, LNPs containing lipid TD5 preferentially target the brain over the liver and spleen in mice.

Lipid A (14:0(5)-cyclopropyl17:0(1)) diammonium is a lipid that can be used as an adjuvant, possessing immunostimulatory properties.

Lipid A (14:0(5)-iso15:0(1)) diammonium is a lipid with adjuvant properties, known for its immune-stimulating characteristics.

Sphingosine-1-phosphate (S1P) is an agonist for S1P1-5 receptors and a ligand for GPR3, GPR6, and GPR12. As an intracellular second messenger, it mobilizes Ca2+ and acts as an extracellular ligand for G-protein coupled receptors. This important lipid mediator is generated from sphingosine or other membrane phospholipids.

1. Berberine (Umbellatine) is a potent oral hypoglycemic agent with beneficial effects on lipid metabolism. 2. Berberine may as a broad-spectrum anti-microbial medicine, a complementary therapeutic agent for HIV/AIDS. 3. Berberine seems to act as an herbal antidepressant and a neuroprotector against neurodegenerative disorders. 4. Berberine is used in histology for staining heparin in mast cells. As a natural dye, berberine has a colour index of 7516. 5. Berberine reduces hepatic fat content in rats with nonalcoholic fatty liver disease; also prevents proliferation of hepatic stellate cells (HSCs), which are central for the development of fibrosis during liver injury. 6. Berberine can ameliorate proinflammatory cytokines-induced intestinal epithelial tight junction damage in vitro, and berberine may be one of the targeted therapeutic agents that can restore barrier function in intestinal disease states. 7. Berberine has antineoplastic effects, including breast cancer, leukemia, melanoma, epidermoid carcinoma, hepatoma, pancreatic cancer, oral carcinoma, tongue carcinoma, glioblastoma, prostate carcinoma and gastric carcinoma, etc.

Uridine 5'-monophosphate disodium salt (Disodium UMP) has been used to study the effect of pyrimidine synthesis inhibitor, 5-azacytidine, on cholesterol and lipid metabolism. It has been used to study the effect of nucleotides on growth of specific intestinal bacteria.

Bragsin2 (6-methoxy-5-nitro-2-(trifluoromethyl)chromen-4-one) is a hydration-resistant cell penetrant, selective and non-competitive inhibitor of Afr guanine nucleotide exchange factor BRAG2 that inhibits Arf GTPase activation, with an IC50 of 3 μM. Bragsin2 binds at the interface between the pleckstrin homology domain of BRAG2 and the lipid bilayer, leading BRAG2 unable to activate lipidated Arf GTPase.

Photosensitizer-5, a photodynamic agent, exhibits cytotoxicity towards HeLa and HepG2 cells, with IC50 values of 10.4 nM and 6.9 nM, respectively. It induces cell death through lipid peroxidation via an iron-independent ferroptosis pathway. Additionally, Photosensitizer-5 displays antitumor activity in HeLa-tumor-bearing mice.

Ferroptosisinducer-4 (Compound 5) is a phospholipid-based ferroptosis inducer featuring a terminal double bond at the sn-2 position. It exhibits significant cytotoxicity towards HT-1080 cells with an IC50 value of 18 μM. The toxicity mechanism involves the generation of lipid peroxides and oxidative damage to the cell membrane induced by the terminal double bond. Ferroptosisinducer-4 can be utilized in studies pertaining to the regulation of ferroptosis.

Ionizable Lipid 4 is an ionizable cationic lipid that forms as a product of the rearrangement of cationic lipid CA-lipid 5 under hydrogen peroxide induction.

PPARγ-IN-5 (Compound A3) is an inhibitor of PPARγ. In liver cells, it reduces lipid accumulation and shows no significant cytotoxicity in HepG2 cells at a concentration of 400 µM. PPARγ-IN-5 is applicable for research on non-alcoholic fatty liver disease.

HDAC11-IN-2 (compound B6) is a highly selective inhibitor of Histone Deacetylase 11 (HDAC11). It demonstrates IC50 values of 51.1 ×10^-3 μM for HDAC11 and 5 μM for HDAC8. HDAC11-IN-2 reduces de novo lipogenesis (DNL) and enhances fatty acid oxidation, which alleviates hepatic lipid accumulation and pathological symptoms in MASLD mice. By inhibiting HDAC11, HDAC11-IN-2 enhances the phosphorylation of AMPKα1 at the Thr172 site, thereby modulating de novo lipogenesis and fatty acid oxidation in the liver.

3-(4-Hydroxy-3-methoxyphenyl)-1-(2-hydroxyphenyl)prop-2-en-1-one (Compound 5) acts as a selective inhibitor of lipid peroxidation. It holds potential for research into oxidative stress-related diseases such as cardiovascular and neurodegenerative disorders.

TMX-4102 is a highly selective binder of phosphatidylinositol 5-phosphate 4-kinase Type II gamma (PIP4K2C). It demonstrates binding activity to PIP4K2C with a dissociation constant (KD) of 0.45 nM, and does not significantly affect other lipid and non-lipid kinases. By specifically binding to PIP4K2C, TMX-4102 regulates its scaffold function rather than its enzymatic activity. TMX-4102 serves as a tool molecule for studying the biological functions and potential therapeutic value of PIP4K2C.

3’,5’-DiOA-dC is a hydrophobic nucleotide lipid and acts as a ligand for the STING agonist c-di-GMP (CDG). It can assemble with CDG to form stable cyclic dinucleotide nanoparticles through molecular recognition-driven supramolecular forces. This interaction reduces tumor weight and volume while increasing the levels of CD8 T cells, neutrophils, and NK cells in the tumor microenvironment. Additionally, 3’,5’-DiOA-dC enhances TNF-α and IFN-γ levels in a mouse melanoma model.

TREM2 agonist-5 is a ligand for the microglial lipid-sensing receptor (TREM2) and acts as an agonist with a Kd of 71.36 μM. It is the racemic analog of the TREM2 agonist VG-3927 and demonstrates excellent microglial phagocytic activity in HEK293-hTREM2/DAP12 cells, effectively activating TREM2 signaling. TREM2 agonist-5 has superior in vitro pharmacokinetics compared to VG-3927 and is potentially useful for Alzheimer's disease research.

AzoLPA ammonium is a photoswitchable lipid that activates signaling of lysophosphatidic acid receptors 1-5 (LPA1-5).

Choline is a vital nutrient essential for maintaining liver, neurological, hematological, and skeletal muscle balance. It serves as a precursor in the biosynthesis of membrane phospholipids, like phosphatidylcholine, which aid in cell signaling and membrane transport, and is also a precursor to the neurotransmitter acetylcholine. Choline is crucial for hepatic lipid transport. In animal studies, perinatal administration of choline (18.8 mg/kg) has been shown to enhance cognitive function impaired by prenatal alcohol exposure in rats. Additionally, choline (13 mg/animal per day) improves motor coordination and addresses behavioral issues in a mouse model of Rett syndrome, and mitigates recognition memory deficits caused by early-life iron deficiency in rats when provided in drinking water at 5 ppm. Low choline intake is linked to muscle wasting, and dietary choline (1,000 mg/kg) boosts leg and breast muscle protein content in broiler chickens.

FABP4/5-IN-2 is a potent dual inhibitor of fatty acid binding protein 4 (FABP4) and fatty acid binding protein 5 (FABP5) that robustly interferes with intracellular lipid trafficking and fatty acid signaling pathways, making it a valuable pharmacological tool for investigating metabolic inflammation, insulin resistance, and lipid-driven disease mechanisms in both in vitro and in vivo experimental systems.