82055-94-5

Usage

Uses

Used in Click Chemistry:
O,Oμ-Bis(2-azidoethyl)polyethylene glycol, PEG-diazide is used as a cross-linking agent in click chemistry reactions. The azide groups allow for efficient and selective coupling with other molecules, making it a valuable tool in the synthesis of complex structures.
Used in Drug Delivery Systems:
O,Oμ-Bis(2-azidoethyl)polyethylene glycol, PEG-diazide is used as a component in drug delivery systems. The incorporation of PEG-diazide improves the pharmacological properties of the drug, such as increased water solubility, enhanced resistance to degradation, increased circulation half-life, and reduced antigenicity.
Used in Virology and Immunology:
O,Oμ-Bis(2-azidoethyl)polyethylene glycol, PEG-diazide is used in virology and immunology applications. The PEGylation of biological molecules can enhance their stability and bioavailability, making them more effective in their respective fields.
Used in Enzyme Conjugation:
O,Oμ-Bis(2-azidoethyl)polyethylene glycol, PEG-diazide is used as a polymer for preparing enzyme conjugates that are soluble in organic solvents. This property makes it a promising drug carrier, as it can improve the solubility and stability of enzymes in various environments.

Upstream product

• 112-26-5 1,2-bis(2-chloroethoxy)ethane 
• 19249-03-7 triethylene glycol di-(p-toluenesulfonate) 
• 31255-10-4 1,2-bis-(2-bromo-ethoxy)-ethane 
• 112-60-7 Tetraethylene glycol 
• 2615-15-8 pentaethylene glycol 
• 54797-77-2 1,23-dichloro-3,6,9,12,15,18,21-heptaoxatricosane 
• 4792-15-8 Pentaethylene glycol 
• 41024-91-3 penta(ethylene glycol) bis(p-toluenesulfonate) 
• 5197-65-9 1,14-dichloro-3,6,9,12-tetraoxatetradecane 
• 37860-51-8 tetraethylene glycol di(p-toluenesulfonate) 
• 31255-26-2 1-bromo-2-{2-[2-(2-bromoethoxy)ethoxy]-ethoxy}ethane 
• 55400-73-2 ((oxybis(ethane-2,1-diyl))bis(oxy))bis(ethane-2,1-diyl) dimethanesulfonate 
• 638-56-2 1,11-dichloro-3,6,9-trioxaundecane 
• 36839-55-1 1,2-bis-(2-iodoethoxy)ethane 

Downstream Products

• 1622913-99-8 bis{4-(4-chlorophenyl)-1-[4-(4-fluorophenyl)-4-oxobutyl]piperidin-4-yl} 3,3’-[oxybis(ethane-2,1-diyloxyethane-2,1-diyl-1H-1,2,3-triazole-1,4-diyl)]dipropanoate 
• 1622914-00-4 bis{4-(4-chlorophenyl)-1-[4-(4-fluorophenyl)-4-oxobutyl]piperidin-4-yl} 3,3’-[3,6,9,12-tetraoxatetradecane-1,14-diylbis(1H-1,2,3-triazole-1,4-diyl)]dipropanoate 
• 332941-25-0 1,23-diamino-3,6,9,12,15,18,21-heptaoxatricosane 
• 72236-26-1 2-(2-(2-(2-(2-(2-aminoethoxy)-ethoxy)-ethoxy)-ethoxy)-ethoxy)-ethyl amine 
• 890016-39-4 N-(2-(2-(2-(2-azidoethoxy)ethoxy)ethoxy)ethyl)-5-(1,2-dithiolan-3-yl)pentanamide 
• 642091-68-7 tert-butyl N-[2-[2-[2-(2-azidoethoxy)ethoxy]ethoxy]ethyl]carbamate 
• 875770-34-6 N-[2-[2-[2-(2-azidoethoxy)ethoxy]ethoxy]ethyl]biotinamide 

Relevant academic research and scientific papers

Catalytic Synthesis of PEGylated EGCG Conjugates that Disaggregate Alzheimer's Tau

The naturally occurring flavonoid ( )-epigallocatechin gallate (EGCG) is a potent disaggregant of tau fibrils. Guided by the recent cryo-electron microscopy (cryoEM) structure of EGCG bound to fibrils of tau derived from an Alzheimer s brain donor, methods to site-specifically modify the EGCG D-ring with aminoPEGylated linkers are reported. The resultant molecules inhibit tau fibril seeding by Alzheimer s brain extracts. Formulations of aminoPEGylated EGCG conjugated to the (quasi)-brain-penetrant nanoparticle Ferumoxytol inhibit seeding by AD-tau with linker length affecting activity. The protecting groupfree catalytic cycloaddition of amino azides to mono-propargylated EGCG described here provides a blueprint for access to stable nanoparticulate forms of EGCG potentially useful as therapeutics to eliminate Alzheimer s-related tau tangles.

Design and Synthesis of Oleanolic Acid Trimers to Enhance Inhibition of Influenza Virus Entry

Influenza is a major threat to millions of people worldwide. Entry inhibitors are of particular interest for the development of novel therapeutic strategies for influenza. We have previously discovered oleanolic acid (OA) to be a mild influenza hemagglutinin (HA) inhibitor. In this work, inspired by the 3D structure of HA as a homotrimeric receptor, we designed and synthesized 15 OA trimers with different linkers and central region via the copper-catalyzed azide-alkyne cycloaddition reaction. All of the OA trimers were evaluated for their antiviral activities in vitro, and 12c, 12e, 13c, and 13d were observed to exhibit robust potency (IC50 in the submicromolar range) against influenza A/WSN/33 (H1N1) virus that was stronger than that observed with oseltamivir. In addition, these compounds also displayed strong biological activity against A/Hong Kong/4801/2014 and B/Sichuan/531/2018 (BV). The results of hemagglutination inhibition assays and surface plasmon resonance binding assays suggest that these OA trimers may interrupt the interaction between the HA protein of influenza virus and the host cell sialic acid receptor, thus blocking viral entry. These findings highlight the utility of multivalent OA conjugates to enhance the ligand-target interactions in anti-influenza virus drug design and are also helpful for studying antiviral drugs derived from natural products.

DINUCLEATING LIGAND OR DINUCLEAR METAL COMPLEX

To provide a metal complex that has high cancer cell toxicity and has DNA target and cyclen.SOLUTION: The present disclosure provides a dinuclear metal complex represented by the following formula (IV).SELECTED DRAWING: None

Azo high polymer for transporting medicine to intestinal tracts and releasing medicine as well as preparation method and application of azo high polymer

The invention discloses an azo high polymer for transporting medicine to intestinal tracts and releasing the medicine as well as a preparation method and application of the azo high polymer. The azo high polymer is synthesized by taking dibromoalkane with two brominated ends, oligomeric glycol, paranitroaniline and m-hydroxybenzoic acid as main raw materials. The final structure of the azo high polymer is shown in a formula described in the specifications of the invention; in the formula, x is equal to the sum of y and z, n is equal to 2, 3, 4, 5..., m is equal to 2, 3, 4, 5...; the high polymer can wrap the medicine to form particles through a double emulsification method, the particles reach the intestinal tracts through oral administration, then azo bonds are cut off by bacteria living in the intestinal tracts, the medicine is released, and therefore the effect of treating intestinal diseases is achieved.

Tetrahydroisoquinoline derivative as well as preparation method and medical application thereof

The invention relates to a tetrahydroisoquinoline derivative, a preparation method thereof and medical application of the tetrahydroisoquinoline derivative. Specifically, the invention relates to a tetrahydroisoquinoline derivative as shown in a general formula (I) and a medicinal salt thereof, a preparation method of the tetrahydroisoquinoline derivative and the medicinal salt thereof, and application of the tetrahydroisoquinoline derivative and the medicinal salt thereof as NHE3 inhibitors, particularly as a therapeutic agent for diseases related to body fluid retention or salt overload or gastrointestinal diseases. Wherein the definition of each substituent in the general formula (I) is the same as the definition in the specification.

COMPOSITIONS AND METHODS RELATED TO MOLECULAR CONJUGATION

The invention relates to activated Michael acceptor (AMA) compounds that can undergo conjugation with biomolecules containing Michael donor moieties, thereby providing plasma-stable antibody-drug conjugates (ADCs). Pharmaceutical compositions of the ADCs are disclosed as well. Also provided herein are a number of applications (e.g., therapeutic applications) in which the compositions are useful.

A Versatile Sub-Nanomolar Fluorescent Ligand Enables NanoBRET Binding Studies and Single-Molecule Microscopy at the Histamine H3Receptor

The histamine H3 receptor (H3R) is considered an attractive drug target for various neurological diseases. We here report the synthesis of UR-NR266, a novel fluorescent H3R ligand. Broad pharmacological characterization revealed UR-NR266 as a sub-nanomolar compound at the H3R with an exceptional selectivity profile within the histamine receptor family. The presented neutral antagonist showed fast association to its target and complete dissociation in kinetic binding studies. Detailed characterization of standard H3R ligands in NanoBRET competition binding using UR-NR266 highlights its value as a versatile pharmacological tool to analyze future H3R ligands. The low nonspecific binding observed in all experiments could also be verified in TIRF and confocal microscopy. This fluorescent probe allows the highly specific analysis of native H3R in various assays ranging from optical high throughput technologies to biophysical analyses and single-molecule studies in its natural environment. An off-target screening at 14 receptors revealed UR-NR266 as a selective compound.

RADIOLABELLED TARGETING LIGANDS

The present invention relates to compounds that are useful as radioimaging agents and radiopharmaceuticals. The compounds may be coordinated with a radionuclide and may be useful in diagnostic imaging and radiotherapy. The invention also relates to method

DINUCLEATING LIGAND OR DINUCLEAR METAL COMPLEX

To provide a dinuclear metal complex that can be synthesized simply and easily and has a proper anticancer action.SOLUTION: The present disclosure provides a dinucleating ligand represented by the following formula (I) and a dinuclear metal complex thereof (where each X may be the same or different to represent H, Cl, OMe, or, Me, Y is H, a phenyl group, a substituted carbamoyl group or the like).SELECTED DRAWING: None

DINUCLEATING LIGAND OR DINUCLEAR METAL COMPLEX

To provide a dinuclear metal complex that can be synthesized simply and easily and has a proper anticancer action.SOLUTION: The present disclosure provides a dinucleating ligand represented by the following formula (I) and a dinuclear metal complex thereof (where X is H or a substituted carbamoyl group, R1, R2, R3, and R4 independently represent H or a C1-8 linear or branched alkyl group).SELECTED DRAWING: None