Introduction

tBuO-Ste-Glu(OtBu)-AEEA-AEEA-OSU (CAS 1118767-15-9) is a versatile heterobifunctional linker designed for advanced drug delivery and bioconjugation applications. Combining a hydrophobic stearyl (Ste) chain, tert-butyl (tBu) protecting groups, polyethylene glycol (PEG)-d AEEA spacers, and an N-hydroxysuccinimide (NHS) ester, this compound enables precise covalent conjugation of therapeutic payloads (e.g., proteins, mRNA) to lipid nanoparticles (LNPs) or targeting ligands. Its CAS number, 1118767-15-9, ensures accurate identification in research and industrial workflows. This article explores its structural features, applications, and advantages in modern biopharmaceutical development.

Chemical Structure and Key Components

tBuO-Ste-Glu(OtBu)-AEEA-AEEA-OSU (CAS 1118767-15-9) integrates four functional segments:

1. Stearyl (Ste) Chain: A hydrophobic lipid anchor for ding into lipid membranes or nanoparticles.

2. tBu-Protected Glutamic Acid: Ensures stability during synthesis, with tert-butyl groups removable under acidic conditions.

3. AEEA Spacers: Two aminoethyl-ethoxy-acetyl units enhance hydrophilicity and flexibility, improving biocompatibility.

4. NHS Ester (OSU): Reacts with primary amines (e.g., lysine residues) for controlled bioconjugation.

The CAS registry 1118767-15-9 uniquely identifies this compound, streamlining regulatory compliance and sourcing.

Applications in Drug Development

1. Lipid Nanoparticle (LNP) Functionalization

• Conjugates targeting ligands (e.g., antibodies, peptides) to LNPs for cell-specific mRNA or siRNA delivery.

2. Antibody-Drug Conjugates (ADCs)

• Links cytotoxic drugs to antibodies via pH-labile Glu(OtBu) linkages, enabling tumor-selective drug release.

3. Protein-Polymer Hybrids

• Attaches PEG chains to proteins (e.g., interferons, enzymes) to prolong circulation half-life.

4. Diagnostic Probes

• Couples imaging agents (e.g., fluorescent dyes) to nanoparticles for in vivo tracking.

Advantages Over Conventional Linkers

• Controlled Release: Acid-labile tBu groups allow payload release in acidic environments (e.g., tumor sites).

• Dual Functionality: Combines lipid anchoring (Ste) and amine-reactive (NHS) properties for modular design.

• Enhanced Solubility: AEEA spacers reduce aggregation in aqueous systems.

• Scalability: Compatible with GMP-grade manufacturing for clinical applications.

Synthesis and Handling Guidelines

Synthesis Protocol:

1. Stearyl-Glu(OtBu) Assembly: Stearic acid is coupled to protected glutamic acid.

2. AEEA Spacer Addition: PEG-like spacers are appended via carbodiimide chemistry.

3. NHS Ester Activation: The terminal carboxyl group is converted to an NHS ester.

Storage:

• Store at -20°C under inert gas (e.g., argon) to prevent NHS ester hydrolysis.

• Avoid moisture, light, and primary amines.

Safety and Regulatory Insights

• Handling: Use PPE (gloves, goggles) and work in a fume hood to avoid amine exposure.

• Disposal: Follow local regulations for organic NHS esters.

• Regulatory Status: Listed under CAS 1118767-15-9, classified as non-hazardous.

Global Supplier: Pukang Biotechnology

Pukang Biotechnology supplies high-purity tBuO-Ste-Glu(OtBu)-AEEA-AEEA-OSU (CAS 1118767-15-9) and custom conjugation services. Offerings include:

• GMP-Compliant Production: For ADC and LNP therapeutic development.

• Technical Support: Optimization of linker-drug ratios and stability studies.

• Fast Global Shipping: Ensuring seamless integration into R&D pipelines.

Contact: +86-137-0808-4407 | export@pu-kang.com

Conclusion

tBuO-Ste-Glu(OtBu)-AEEA-AEEA-OSU (CAS 1118767-15-9) bridges drug delivery and bioconjugation, enabling targeted therapies, enhanced diagnostics, and stable nanomedicines. Its modular design, controlled release properties, and scalability make it indispensable for advancing precision medicine. For researchers and developers, CAS 1118767-15-9 offers a robust tool to optimize therapeutic efficacy and safety.