1069067-08-8

Usage

Chemical Properties

Light yellow oil

Upstream product

• 1100909-84-9 methyl 2,2-dimethyl-4,13-dioxo-3,8,11,17,20-pentaoxa-5,14-diazadocosan-22-oate 
• 911102-04-0 2-(2-(2-tert-butoxycarbonylamino-ethoxy)ethoxy)acetic acid N-hydroxy-succinimide ester 
• 134978-97-5 [2-(N-2-amino ethoxy)ethoxy] acetic acid 
• 108466-89-3 N-(tert-butyloxycarbonyl)-8-amino-3,6-dioxaoctanoic acid 

Downstream Products

• 1143516-05-5 [2-(2-{2-[2-(2-amino-ethoxy)-ethoxy]-acetylamino}-ethoxy)-ethoxy]-acetic acid 

Relevant academic research and scientific papers

PCSK9 ANTAGONIST COMPOUNDS

Disclosed are compounds of Formula (A), or a pharmaceutically acceptable salt thereof: where A, X, R1, and R2 are as defined herein, which compounds have properties for antagonizing PCSK9. Also described are pharmaceutical formulations comprising the compounds of Formula (I) or their salts, and methods of treating cardiovascular disease and conditions related to PCSK9 activity, e.g. atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions.

METHOD FOR PREPARING LONG-CHAIN COMPOUND

The present invention relates to a preparation method of a long-chain compound, which includes the following steps: (1) carrying out condensation reaction on H—R2 and R5N-Glu(OR4)—OR3, wherein, R3 is a carboxyl protecting group, R4 is a carboxyl activating group, and R5 is an amino protecting group; obtaining a compound of formula II; (2) removing carboxyl protecting group R3 and amino protecting group R5 of the compound shown in formula II to obtain a compound of formula III; (3) carrying out condensation reaction on the compound shown in formula III and to obtain a compound shown in formula I. The method reduces the time of deprotection, and all the reactions can be carried out in a solvent with low boiling point. The post-processing requires only simple washing and recrystallization to obtain the product with higher purity, so the method is suitable for large-scale production.

A novel heterotrifunctional peptide-based cross-linking reagent for facile access to bioconjugates. Applications to peptide fluorescent labelling and immobilisation

A convenient, versatile and straightforward synthesis of a novel heterotrifunctional peptide-based linker molecule is described. This generic bio-labelling reagent contains an amine-reactive N-hydroxysuccinimidyl carbamate moiety, an aldehyde/ketone-reactive aminooxy group and a thiol group with a propensity to form urea, oxime and thioether linkages respectively. The full chemical orthogonality between the free aminooxy and thiol functionalities was demonstrated through the preparation of a fluorescent reagent suitable for the selective staining of a carboxaldehyde-modified surface by means of oxime ligation. The absence of reactivity of these two functions toward the nucleophile-sensitive active carbamate was obtained by using temporary aminooxy- and thiol-protecting groups removable under mild conditions. The utility of the linker molecule to cross-link three different molecular partners has been illustrated by the preparation of fluorescent tripod-functionalised surfaces which may be useful in developing new peptide microarrays and related immunosensors.