lipid-conjugated

Brincidofovir (HDP-CDV) is an orally active, lipophilic form of cidofovir. It has enhanced activity compared to CDV against certain adenoviruses, herpesviruses, and orthopoxviruses.

Elacytarabine (M7594 0037), a lipid-conjugated derivative of the nucleoside analog cytarabine, is an antineoplastic drug. It has cytotoxicity in solid tumors.

DSPE-PEG(2000)-biotin is a biotinylated and PEGylated form of 1,2-distearoyl-sn-glycerol-3-phosphoethanolamine. This compound is extensively used in both in vitro and in vivo for the delivery of small molecule liposomes, as well as for fluorescently labeling nanoparticle lipid carriers (NLCs). Additionally, DSPE-PEG(2000)-biotin is employed to form micelles and serves as a precursor for immobilizing liposomes, utilized in biolayer interferometry binding experiments. Liposomes containing DSPE-PEG(2000)-biotin, encapsulating doxorubicin and quercetin, exhibit cytotoxicity against MCF-7 adr multidrug-resistant breast cancer cells in vitro and slow tumor growth in the MCF-7 adr mouse xenograft model. Fluorescent labeling of NLCs containing DSPE-PEG(2000)-biotin has been successfully achieved using avidin conjugated with FITC-labeled biotin.

Tenofovir exalidex (CMX 157) is a lipid-conjugated acyclic nucleotide analog of Tenofovir, demonstrating efficacy against wild-type and antiretroviral-resistant HIV strains, including those resistant to multiple nucleoside nucleotide analogs. It effectively inhibits all major HIV-1 and HIV-2 subtypes in fresh human PBMCs, as well as all evaluated HIV-1 strains in monocyte-derived macrophages, displaying EC50 values between 0.2 and 7.2 nM. Oral administration of CMX157 shows no apparent toxicity. Additionally, Tenofovir exalidex exhibits antiviral properties against HBV.

1-Pentadecanoyl-rac-glycerol is a monoacylglycerol that contains pentadecanoic acid at the sn-1 position. It has been found in wheat bran extracts.1 1-Pentadecanoyl-rac-glycerol levels are increased in a HepaRG cell-based model of hepatic steatosis induced by BSA-conjugated palmitate.2 |1. Prinsen, P., Gutiérrez, A., Faulds, C.B., et al. Comprehensive study of valuable lipophilic phytochemicals in wheat bran. J. Agric. Food Chem. 62(7), 1664-1673 (2014).|2. Brown, M.V., Compton, S.A., Milburn, M.V., et al. Metabolomic signatures in lipid-loaded HepaRGs reveal pathways involved in steatotic progression. Obesity (Silver Spring) 21(12), E561-E570 (2013).

9(Z),11(E)-Conjugated linoleic acid is an isomer of linoleic acid that has been found in beef and milk fat.1It binds to peroxisome proliferator-activated receptor α (PPARα; IC50= 140 nM) and activates the receptor in a reporter assay using COS-1 cells expressing mouse PPARα when used at a concentration of 100 μM.29(Z),11(E)-Conjugated linoleic acid inhibits TNF-α-inducedGLUT4expression and increases insulin-stimulated glucose transport in 3T3-L1 adipocytes.3Dietary administration of 9(Z)11(E)-conjugated linoleic acid reduces serum fasting glucose, insulin, and triglyceride levels and decreases white adipose tissue macrophage infiltration inob/obmice. It also increases body weight gain and body fat in weanling mice.4[Matreya, LLC. Catalog No. 1278] 1.Shultz, T.D., Chew, B.P., Seaman, W.R., et al.Inhibitory effect of conjugated dienoic derivatives of linoleic acid and β-carotene on the in vitro growth of human cancer cellsCancer Lett.63(2)125-133(1992) 2.Moya-Camarena, S.Y., Heuvel, J.P.V., Blanchard, S.G., et al.Conjugated linoleic acid is a potent naturally occurring ligand and activator of PPARαJ. Lipid Res.40(8)1426-1433(1999) 3.Moloney, F., Toomey, S., Noone, E., et al.Antidiabetic effects of cis-9, trans-11-conjugated linoleic acid may be mediated via anti-inflammatory effects in white adipose tissueDiabetes56(3)574-582(2007) 4.Pariza, M.W., Park, Y., and Cook, M.E.The biologically active isomers of conjugated linoleic acidProg. Lipid Res.40(4)283-298(2001)

DEPMPO is a nitrone that is used to spin trap reactive O-, N-, S-, and C-centered radicals and allow their characterization when used in association with electron spin resonance. It is noted for the stability of adducts formed. DEPMPO can be used in vitro or in vivo, as it crosses lipid bilayer membranes and is a good trapping agent in biological systems. DEPMPO-biotin is a biotinylated form of DEPMPO which retains the outstanding persistency of its adducts. The biotin moiety offers an effective means for monitoring biodistribution in cells, tissues, and organs when used with an avidin-conjugated reporter. Importantly, DEPMPO-biotin binds free radicals, such as S-nitroso groups, on proteins, producing adducts that can be analyzed via the biotin tag. This direct labeling of S-nitrosothiols (SNO) thus serves as an effective alternative to the more cumbersome biotin-switch method for monitoring SNO formation.

Lipoxin A4 methyl ester (LXA4 methyl ester) is a more lipid soluble, prodrug formulation of the transcellular metabolite LXA4. LXA4 is a trihydroxy fatty acid containing a conjugated tetraene, produced by the metabolism of 15-HETE or 15-HpETE with human leukocytes.[1] LXA4 is equipotent to leukotriene B4 (LTB4) in inducing superoxide generation in human neutrophils at 0.1 μM.[2] LXA4 is associated with several other biological functions including leukocyte activation, chemotaxis effects, natural killer cell inhibition, and monocyte migration and adhesion.[2],[3],[4]

3β-OH-7-Oxocholenic acid is a bile acid.1 It is also a metabolite of 7β-hydroxy cholesterol in rats. Conjugated forms of 3β-OH-7-oxocholenic acid have been found in the urine of patients with Neimann-Pick disease type C.2,3 |1. Norii, T., Yamaga, N., and Yamasaki, K. Metabolism of 7β-hydroxycholesterol-4-14C in rat. Steroids 15(3), 303-326 (1970).|2. Alvelius, G., Hjalmarson, O., Griffiths, W.J., et al. Identification of unusual 7-oxygenated bile acid sulfates in a patient with Niemann-Pick disease, type C. J. Lipid Res. 42(10), 1571-1577 (2001).|3. Maekawa, M., Omura, K., Sekiguchi, S., et al. Identification of two sulfated cholesterol metabolites found in the urine of a patient with Niemann-Pick disease type C as novel candidate diagnostic markers. Mass Spectrom. (Tokyo) 5(2), S0053 (2016).

DSPE-PEG(2000)-amine is a PEGylated derivative of 1,2-distearoyl-sn-glycero-3-PE . It has been used in the synthesis of solid lipid and thermosensitive liposomal nanoparticles for the delivery of anticancer agents.1,2,3DSPE-PEG(2000)-amine has also been used in the synthesis of fluorescein isothiocyanate-loaded mesoporous silica nanoparticles for imaging applications.4It can be conjugated to a variety of functional molecules for improved cellular targeting and uptake of DSPE-PEG(2000)-amine-containing nanoparticles.4,5 1.Sloat, B.R., Sandoval, M.A., Li, D., et al.In vitro and in vivo anti-tumor activities of a gemcitabine derivative carried by nanoparticlesInt. J. Pharm.409(1-2)278-288(2011) 2.Abd-Rabou, A.A., Bharali, D.J., and Mousa, S.A.Taribavirin and 5-fluorouracil-loaded pegylated-lipid nanoparticle synthesis, p38 docking, and antiproliferative effects on MCF-7 breast cancerPharm. Res.35(4)76(2018) 3.Affram, K., Udofot, O., Singh, M., et al.Smart thermosensitive liposomes for effective solid tumor therapy and in vivo imagingPLoS One12(9):e0815116(2017) 4.Wang, L.-S., Wu, L.-C., Lu, S.-Y., et al.Biofunctionalized phospholipid-capped mesoporous silica nanoshuttles for targeted drug delivery: Improved water suspensibility and decreased nonspecific protein bindingACS Nano4(8)4371-4379(2010) 5.Wen, X., Wang, K., Zhao, Z., et al.Brain-targeted delivery of trans-activating transcriptor-conjugated magnetic PLGA/lipid nanoparticlesPLoS One9(9):e106652(2014)

1,2-Dipalmitoyl-sn-glycero-3-PE-N-(cap biotin) is a biotinylated phospholipid. It has been used in PEGylated polyamidoamine-dendrimer-conjugated supported lipid bilayers (SLB) to isolate circulating tumor cells and tumor cell microembolis from patient-derived blood by antibody-coated microfluidics. [1] It has also been used as a component of SLBs to detect protein-ligand binding with ortho-conjugated Texas Red DHPE. [2] In addition, 1,2-dipalmitoyl-sn-glycero-3-PE-N-(cap biotin) has been used in SLBs partitioned into nanowells to create DNA curtains, which can be used as a high-throughput tool for detection of protein-DNA interactions at the single molecule level.[3]

9(Z),11(E),13(E)-Octadecatrienoic Acid ethyl ester (α-ESA) is a conjugated polyunsaturated fatty acid commonly found in plant seed oil. This fatty acid accounts for about 60% of the total fatty acid composition of bitter gourd seed oil and about 70% in tung oil. α-ESA is metabolized and converted to conjugated linoleic acid (9Z,11E-CLA) in rats. It has shown potential as a tumor growth suppressor. In colon cancer Caco-2 cells, α-ESA induced apoptosis through up-regulation of GADD45, p53, and PPARγ. In DLD-1 cells supplemented with α-ESA, apoptosis was induced via lipid peroxidation with an EC50 of 20 μM. It also inhibits DNA polymerases and topoisomerases with IC50s ranging from ~5-20 μM for different isoforms of the enzymes. α-ESA ethyl ester is a neutral, more lipid soluble form of the free acid.

Methyl alpha-eleostearate (α-ESA) is a conjugated polyunsaturated fatty acid commonly found in plant seed oil. This fatty acid accounts for about 60% of the total fatty acid composition of bitter gourd seed oil and about 70% in tung oil. α-ESA is metabolized and converted to conjugated linoleic acid (9Z,11E-CLA) in rats. It has shown potential as a tumor growth suppressor. In colon cancer Caco-2 cells, α-ESA induced apoptosis through up-regulation of GADD45, p53, and PPARγ. In DLD-1 cells supplemented with α-ESA, apoptosis was induced via lipid peroxidation with an EC50 of 20 μM. It also inhibits DNA polymerases and topoisomerases with IC50s ranging from ~5-20 μM for different isoforms of the enzymes. α-ESA methyl ester is a neutral, more lipid soluble form of the free acid.

Steryl glucosides are neutral glycolipids commonly found in plant cell membranes and vegetable oils that contain a glucose moiety conjugated to a sterol lipid. They function as glucose donors in the biosynthesis of glucocerebrosides in plant microsomes and are metabolic precursors to acylated/esterified steryl glucosides. Steryl glucosides are the major component of filter- and engine-damaging precipitates formed during biodiesel production from transesterification of vegetable oils. This product contains a mixture of steryl glucosides.

Spike Binding Peptide 1 (SBP1), representing amino acids 21-43 of angiotensin-converting enzyme 2 (ACE2), has been utilized in a novel approach involving lipid nanoparticles (LNPs) encapsulated with oseltamivir phosphate and conjugated to SBP1. This formulation aims to investigate the possibility of achieving a controlled, long-term in vivo release of oseltamivir phosphate. Furthermore, a 2% concentration of SBP1 immobilized on crosslinked networks composed of hydroxy acrylate and ethylxanthate ethyl acrylate has demonstrated enhanced in vitro efficiency in capturing the spike glycoprotein of severe acute respiratory coronavirus 2 (SARS-CoV-2), also referred to as the surface glycoprotein.

DSPE-PEG-Folate, MW 2000 is a folic acid-conjugated PEG (polyethylene glycol) derivative known for its targeting capabilities by binding to folate receptors in cancer cells. It forms micelles lipid bilayers and is utilized in the study of targeted drug delivery systems.

DPPE-PEG550 serves as a PEG lipid functional terminal group used for synthesizing liposomes (LPs) to design conjugated polymer nanoparticles. Liposome nanoparticles (LNPs) are capable of further coupling with other biomolecules through biotin modification and carboxyl terminals. Functionalized nanoparticles can target specific cell proteins for labeling purposes. Using streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles can bind with biotinylated antibodies on cell surface receptors, enabling applications in fluorescence-based imaging and sensing.

DPPE-PEG750 is a PEG lipid functional end group used for synthesizing liposomes (LPs) and designing conjugated polymer nanoparticles. Liposome nanoparticles (LNPs) modified with biotin and carboxylic ends can couple with other biomolecules. These functionalized nanoparticles are useful for targeting specific cell proteins. Using streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles can bind to biotinylated antibodies on cell surface receptors, facilitating fluorescence-based imaging and sensing applications.

DPPE-PEG1000 is a PEG lipid functional end group used for synthesizing liposomes (LPs) and is instrumental in designing conjugated polymer nanoparticles. Liposome nanoparticles (LNPs), featuring biotin modification and carboxyl terminals, can further couple with other biomolecules. These functionalized nanoparticles are useful for the targeted labeling of specific cell proteins. By employing streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles can bind to biotinylated antibodies on cell surface receptors, enabling applications in fluorescence-based imaging and sensing.

DPPE-PEG3000 is a PEG lipid functional end group used for synthesizing liposomes (LPs) and designing conjugated polymer nanoparticles. Liposome nanoparticles (LNPs) modified with biotin and having a carboxylate end can further couple with other biomolecules. The functionalized nanoparticles are applicable for targeted labeling of specific cell proteins. Using streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles can interact with biotinylated antibodies on cell surface receptors, facilitating fluorescence-based imaging and sensing applications.

DPPE-PEG5000 is a PEG lipid functional terminal group utilized for synthesizing liposomes (LPs) and designing conjugated polymer nanoparticles. Liposome nanoparticles (LNPs) with biotin modification and carboxyl ends can further couple with other biomolecules. These functionalized nanoparticles target specific cellular proteins for labeling. Using streptavidin as a linker, the biotinylated PEG lipid-conjugated polymer nanoparticles can bind to biotinylated antibodies on cell surface receptors, enabling applications in fluorescence-based imaging and sensing.

18:0 mPEG350 PE (ammonium) is a PEG lipid with functional terminal groups used in the synthesis of liposomes (LPs) for designing conjugated polymer nanoparticles. Liposome nanoparticles (LNPs), featuring biotin modification and a carboxyl terminus, enable further coupling with other biomolecules. These functionalized nanoparticles can target specific cell protein labeling. Using streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles can bind with biotinylated antibodies on cell surface receptors, providing practical applications in fluorescence-based imaging and sensing.

18:0 mPEG550 PE (ammonium) is designed for synthesizing liposomes (LPs) with PEG lipid functional end groups, facilitating the creation of conjugated polymer nanoparticles. The liposomal nanoparticles (LNPs), modified with biotin and carboxyl ends, can further couple with various biomolecules. These functionalized nanoparticles are applicable in targeting specific cellular proteins. By utilizing streptavidin as a linker, the biotinylated PEG lipid-conjugated polymer nanoparticles can bind to biotinylated antibodies on cell surface receptors, enabling applications in fluorescence-based imaging and sensing.

18:0 mPEG750 PE (ammonium) serves as a PEG lipid functional terminal for synthesizing liposomes (LPs) in the design of conjugated polymer nanoparticles. Liposomal nanoparticles (LNPs) featuring biotin modification and carboxyl terminals can couple with other biomolecules. These functionalized nanoparticles are applicable for targeting specific cellular proteins. Utilizing streptavidin as a linker, the biotinylated PEG lipid-conjugated polymer nanoparticles can bind with biotinylated antibodies on cell surface receptors, enabling fluorescence-based imaging and sensing applications.