GE 2270A (CAS 134861-34-0) | GMP manufacturer

描述

Product Description

GE 2270A (CAS 134861-34-0), also known as MDL 62879, is a cyclic peptide antibiotic belonging to the thiazolyl peptide family, a unique class of antibiotics recognized for their ability to inhibit bacterial protein synthesis. Originally isolated from Actinoplanes species, GE 2270A has drawn scientific interest for its strong activity against gram-positive bacteria and anaerobic pathogens. Its selective mechanism of action and potency make it a valuable molecule for preclinical antimicrobial studies.

Unlike many broad-spectrum antibiotics that target both gram-positive and gram-negative organisms, GE 2270A exhibits high specificity for gram-positive bacteria. This includes clinically significant pathogens such as Staphylococcus aureus, Enterococcus faecalis, and Clostridium difficile. In addition to its antibacterial spectrum, its unique mode of action provides opportunities for researchers investigating new approaches to overcoming antibiotic resistance, particularly resistance mediated by ribosomal mutations or enzymatic modifications.

GE 2270A belongs to the family of thiopeptide antibiotics, which includes molecules like thiostrepton and nocathiacin. These compounds share structural similarities, including macrocyclic frameworks with sulfur-containing heterocycles, which are critical for their biological activity. Thiopeptides typically target protein translation, and GE 2270A is no exception—it binds specifically to the 50S ribosomal subunit, disrupting elongation factor binding and thereby halting bacterial protein synthesis.

Key highlights:

• Antibacterial Spectrum: Effective against gram-positive pathogens and anaerobes.

• Mode of Action: Inhibits bacterial protein synthesis by binding to the ribosome.

• Research Use: Studies on infection models, resistance development, and ribosomal interactions.

• GMP Quality: Supplied under strict manufacturing standards for reproducibility.

By providing an alternative mechanism of action distinct from clinically common antibiotics like ?-lactams or fluoroquinolones, GE 2270A serves as a reference compound for antimicrobial pharmacology. Researchers can utilize it to understand ribosome-targeting antibiotics, explore drug-resistance mutations, and test potential synergies with other antibacterial agents.

Product Specifications

GE 2270A’s physicochemical properties (such as poor water solubility) are typical for cyclic peptide antibiotics, which often require organic solvents for handling in laboratory settings. This property should be carefully considered when preparing stock solutions.

The purity and stability of GE 2270A make it highly suitable for mechanistic studies, including ribosome-binding assays, bacterial culture inhibition tests, and resistance selection experiments.

Mechanism of Action & Research Applications

GE 2270A acts as a ribosome-targeting antibiotic. Specifically, it binds to the 50S ribosomal subunit at the site where elongation factor Tu (EF-Tu) and elongation factor G (EF-G) interact, which are essential for the translation process. By preventing these interactions, GE 2270A halts protein elongation, ultimately blocking bacterial protein synthesis.

Mechanism Details:

1. Target Recognition: GE 2270A recognizes conserved structural motifs within the bacterial ribosome.

2. Binding Action: It stabilizes ribosomal conformations that prevent elongation factors from functioning.

3. Inhibition of Translation: The inability to elongate polypeptides leads to cessation of bacterial growth.

4. Selectivity: GE 2270A does not significantly affect eukaryotic ribosomes, explaining its selective antibacterial activity.

Research Applications:

• Antimicrobial Resistance Studies: GE 2270A is often used in laboratory models to study the emergence of ribosomal mutations and cross-resistance.

• Infection Models: Applied in bacterial culture systems and in vivo infection research to evaluate antibacterial effects.

• Ribosomal Biology: Serves as a probe for ribosome structure and dynamics, helping define binding pockets for drug discovery.

• Comparative Antibiotic Research: Benchmarked against other thiopeptides to explore potency and structural differences.

• Synergistic Studies: Can be combined with other antibiotics (e.g., ?-lactams or macrolides) to study potential additive or synergistic effects.

Because of its unique ribosome-binding mechanism, GE 2270A remains of interest for researchers investigating next-generation antibiotics. Its structure has been used as a scaffold for synthetic analogues, aiming to improve solubility and reduce potential toxicity.

Side Effects (For Reference in Research Models)

In research models, GE 2270A may produce the following side effects or considerations:

• Cytotoxicity at High Concentrations: While selective for bacterial ribosomes, high doses may impact mammalian cell viability.

• Limited Solubility: Handling and formulation challenges due to poor aqueous solubility.

• Resistance Development: Prolonged exposure to bacterial cultures may select for ribosomal mutations.

• Metabolic Stability Issues: Like other peptide antibiotics, may undergo degradation under certain conditions.

Experimental Precautions:

• Ensure correct solvent preparation (e.g., DMSO) for reproducible results.

• Use appropriate bacterial strains for susceptibility testing.

• Monitor for cytotoxic effects in mammalian co-culture experiments.

• Validate controls to differentiate between solvent and drug effects.

Disclaimer

For laboratory research use only. Not for human or veterinary use.

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