Name: 2,5-dioxopyrrolidin-1-yl 15-(2,5-dioxo-2H-pyrrol-1(5H)-yl)-13-oxo-3,6,9-trioxa-12-azapentadecan-1-oate
Brand: BOC Sciences
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Mal-PEG-NHS;

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2,5-Dioxopyrrolidin-1-yl 15-(2,5-dioxo-2H-pyrrol-1(5H)-yl)-13-oxo-3,6,9-trioxa-12-azapentadecan-1-oate is a specialized chemical reagent often used in biochemical and molecular biology applications. Here are some key applications of this compound:

Protein Labeling: This molecule can be used for protein labeling by forming stable covalent bonds with amino groups. This allows researchers to attach various probes or tags to proteins, enabling the study of protein localization, interaction, and function. Labeling proteins with fluorescent tags, for example, enhances the visualization in microscopy and flow cytometry.

Peptide Synthesis: The compound is useful in solid-phase peptide synthesis, where it acts as a coupling reagent. It assists in forming peptide bonds between amino acids, facilitating the synthesis of complex peptide chains. This is particularly valuable for producing peptides for research, pharmaceutical development, and therapeutic applications.

Drug Development: In the field of drug development, the molecule can be employed to modify drug candidates to improve their solubility, stability, or bioavailability. By attaching this reagent to small molecules or peptides, the pharmacokinetic properties of therapeutic agents can be optimized. This leads to the creation of more effective and safer pharmaceuticals.

Bioconjugation: The compound is instrumental in bioconjugation techniques, where it is used to attach biomolecules to various surfaces or other biomolecules. It can link enzymes to substrates, antibodies to surfaces, or drugs to targeting moieties, among others. This application is essential for developing diagnostic assays, biosensors, and targeted drug delivery systems.

1. New hybrid molecules with anticonvulsant and antinociceptive activity derived from 3-methyl- or 3,3-dimethyl-1-[1-oxo-1-(4-phenylpiperazin-1-yl)propan-2-yl]pyrrolidine-2,5-diones

Anna Rapacz, Michał Abram, Krzysztof Kamiński, Mirosław Zagaja, Jarogniew J Łuszczki, Marta Andres-Mach, Jolanta Obniska Bioorg Med Chem . 2016 Feb 15;24(4):606-18. doi: 10.1016/j.bmc.2015.12.027.

The purpose of this study was to synthetize the focused library of 34 new piperazinamides of 3-methyl- and 3,3-dimethyl-(2,5-dioxopyrrolidin-1-yl)propanoic or butanoic acids as potential new hybrid anticonvulsants. These hybrid molecules join the chemical fragments of well-known antiepileptic drugs (AEDs) such as ethosuximide, levetiracetam, and lacosamide. Compounds 5-38 were prepared in a coupling reaction of the 3-methyl- or 3,3-dimethyl-2-(2,5-dioxopyrrolidin-1-yl)propanoic (1, 2) or butanoic acids (3, 4) with the appropriately substituted secondary amines in the presence of the N,N-carbonyldiimidazole reagent. The initial anticonvulsant screening was performed in mice (ip) using the 'classical' maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) tests as well as in the six-Hertz (6Hz) model of pharmacoresistant limbic seizures. The acute neurological toxicity was determined applying the chimney test. The broad spectra of activity across the preclinical seizure models in mice ip displayed compounds 7, 15, and 36. The most favorable anticonvulsant properties demonstrated 15 (ED50 MES=74.8mg/kg, ED50scPTZ=51.6mg/kg, ED50 6Hz=16.8mg/kg) which showed TD50=213.3mg/kg in the chimney test that yielded satisfying protective indexes (PI MES=2.85, PI scPTZ=4.13, PI 6Hz=12.70) at time point of 0.5h. As a result, compound 15 displayed comparable or better safety profile than clinically relevant AEDs: ethosuximide, lacosamide or valproic acid. In the in vitro assays compound 15 was observed as relatively effective binder to the neuronal voltage-sensitive sodium and L-type calcium channels. Beyond the anticonvulsant properties, 6 compounds diminished the pain responses in the formalin model of tonic pain in mice.