Lipid products — Page 15

DMPE-PEG, a synthetic lipid, possesses unique properties and finds extensive applications as liposomes. Firstly, DMPE-PEG exhibits excellent biocompatibility and solubility, allowing for its stable presence and efficient absorption and metabolism in vivo. Additionally, DMPE-PEG possesses good surface activity, aiding in the stabilization of liposome structures and enhancing their stability.

DOPE-PEG is a versatile phospholipid derivative with unique properties that make it suitable for various applications. Its hydrophobic and hydrophilic nature enables efficient encapsulation and delivery of drugs and nucleic acids, making it a valuable tool in drug delivery systems and gene therapy. Additionally, DOPE-PEG can enhance the stability and circulation time of liposomes, improving their efficacy as drug carriers.

TAMRA-PEG4-NHS ester is a TAMRA red fluorescent dye derivative containing an NHS ester group which can be used to label the primary amines (-NH2) of proteins, amine-modified oligonucleotides, and other amine-containing molecules.

DSPE-PEG(2000)-amine is a PEGylated derivative of 1,2-distearoyl-sn-glycero-3-PE (DSPE; Item No. 15095). It has been used in the synthesis of solid lipid and thermosensitive liposomal nanoparticles for the delivery of anticancer agents. DSPE-PEG(2000)-amine has also been used in the synthesis of fluorescein isothiocyanate-loaded mesoporous silica nanoparticles for imaging applications.4 It can be conjugated to a variety of functional molecules for improved cellular targeting and uptake of DSPE-PEG(2000)-amine-containing nanoparticles.

The polymer with ketone mercaptan as the fragment can form the shell of the nanocore, and simultaneously contain the polyorubicin and light sensitive compounds to achieve dual roles. Ketothiol polymers can also be used directly as drug carriers to contain paclitaxel ROS responsive groups, often in combination with a variety of methods. ROS, as the connecting part, connects the hydrophilic part and the hydrophobic part of the nanocarrier. When the nanocarrier encounters ROS, it breaks and releases drugs: the ROS responsive group can also act as the part connecting drug molecules and nanocarriers to release drugs under oxidation. Common ROS responsive groups generally contain sulfur, boron and tellurium. In addition, in order to inactivate the protein, ROS responsive groups can also be used to block the active center of the protein. Common ROS responsive genes include: polypropylene sulfide, borate, thione, tellurium, selenium, ferrocene, anthocyanins, etc.

DSPE-SPDP is a phospholipid molecule. DSPE-SPDP can orient itself to form lipid bilayer in water. DSPE-SPDP can be used for the research of various biochemical.

DSPE-NHS is a bioconjugation phospholipid molecule with two hydrophobic lipid tails. DSPE-NHS is a self-assembling reagent which forms lipid bilayer in aqueous solution. DSPE-NHS can be used to prepare liposomes as drug nanocarrier.

Endosidine 5 (ES5), is one of the most potent small molecules interferes with recycling endosomes through Annexin A6, thereby promoting the release and expression of mRNA into the cytoplasm. The delivered mRNAs is greatly enhanced via inhibition of endocytic recycling in cells and in live mice. NAV2729 (NAV) and endosidin 5 (ES5), resulted in significant enhancement (1.5–2 folds) of LNP-mediated delivery of Fluc mRNAs. Incubation of NAV and ES5 together caused modest further increases in Fluc expression in comparison to the sole application of either compound.

ART558 is a nanomolar potent, selective, low molecular weight, allosteric DNA polymerase activity of Polθ inhibitor (IC50=7.9 nM). Inhibition of TMEJ with ART558 increases the efficiency of HDR-mediated repair on Cas9-induced DSBs, most profoundly in combination with a NHEJ/DNA-PKcs inhibitor.

Bropirimine is a synthetic agonist for toll-like receptor 7 (TLR7). Bropirimine inhibits differentiation of osteoclast precursor cells into osteoclasts via TLR7-mediated production of IFN-β. Bropirimine is an orally active immunomodulator that has demonstrated anticancer activity in transitional cell carcinoma in situ (CIS) in both the bladder and upper urinary Bropirimine could enhance the transfection efficiency to 2-fold to 5-fold of Lipofectamine 3000 and LNP, all of which are currently approved for clinical use in the treatment of the most common malignant tumors.

SCH 58261 is a potent and selective A2a adenosine receptor antagonist with Ki of 2.3 nM and 2 nM for rat A2a and bovine A2a. SCH58261 could enhance the transfection efficiency to 2-fold to 5-fold of Lipofectamine 3000 and LNP, all of which are currently approved for clinical use in the treatment of the most common malignant tumors.

SH-BC-893 is a water-soluble, orally bioavailable synthetic sphingolipid that triggers nutrient transporter internalization and also blocks lysosome-dependent nutrient generation pathways in cancer cells, activates protein phosphatase 2A (PP2A), leading to mislocalization of the lipid kinase PIKfyve; selectively kills cells expressing an activated form of the anabolic oncogene Ras in vitro and in vivo.SH-BC-893, increases the activity of antisense oligonucleotides (ASOs) and small interfering RNAs (siRNAs) up to 200-fold in vitro without permeabilizing endosomes. SH-BC-893 treatment trapped endocytosed oligonucleotides within extra-lysosomal compartments thought to be more permeable due to frequent membrane fission and fusion events. Simultaneous disruption of ARF6-dependent endocytic recycling and PIKfyve-dependent lysosomal fusion was necessary and sufficient for SH-BC-893 to increase non-lysosomal oligonucleotide levels and enhance their activity. In mice, oral administration of SH-BC-893 increased ASO potency in the liver by 15-fold without toxicity. More importantly, SH-BC-893 enabled target RNA knockdown in the CNS and lungs of mice treated subcutaneously with cholesterol-functionalized duplexed oligonucleotides or unmodified ASOs, respectively. Together, these results establish the feasibility of using a small molecule that disrupts endolysosomal trafficking to improve the activity of oligonucleotides in extrahepatic tissues.

NAV 2729 (NAV2729) is a chemical potentiator for mRNA-LNPs, increasing the delivery efficiencies of mRNA-LNPs in vitro and in vivo.

AZD-7648 is a potent and selective DNA-PK inhibitor. AZD7648,enhances HDR efficiency in CRISPR-Cas9 gene editing by shifting DNA repair from the error-prone NHEJ pathway to the precise HDR pathway, significantly improving gene targeting outcomes in human cells for effective ex vivo gene therapies.

BP-1-102 is a potent, orally bioavailable and selective STAT3 inhibitor.BP-1-102 could enhance the transfection efficiency to 2-fold to 5-fold of Lipofectamine 3000 and LNP, all of which are currently approved for clinical use in the treatment of the most common malignant tumors.

Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs used as an anti-inflammatory and immunosuppressant.

BAY 11-7082 is a NF-κB inhibitor which decreases NF-κB by inhibiting TNF-α-induced phosphorylation of IκB-α. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 with IC50s of 0.19 μM and 0.96 μM, respectively.

MCC950 (CP-456773) sodium is a potent, selective, small-molecule inhibitor of NLRP3 with IC50 of 7.5 nM in BMDMs.