Adarulatide Tetraxetan (CAS No. 1246013-02-4) – Copper-Labeled Diagnostic Imaging Agent

Description

Product Description

Adarulatide tetraxetan (CAS No. 1246013-02-4), also known as Copper adarulatidum tetraxetanum, is a synthetic peptide conjugate that functions as a chelator-based diagnostic imaging agent. It incorporates the macrocyclic chelating group tetraxetan (DOTA derivative), which allows stable coordination with radiometals such as copper-64, gallium-68, or lutetium-177. This structural feature makes Adarulatide tetraxetan a highly valuable molecular imaging probe precursor.

Background and Development

Radiolabeled peptides play a critical role in modern diagnostic oncology. They combine high target selectivity (from peptide ligands) with the quantifiable imaging capabilities of radioactive isotopes. Adarulatide tetraxetan belongs to a new generation of radiopharmaceutical precursors that integrate targeting peptides with robust chelators to enable Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) imaging.

The DOTA-tetraxetan moiety ensures excellent thermodynamic stability and kinetic inertness when complexed with radiometals, which minimizes transchelation in vivo and provides high-quality imaging contrast. When labeled with copper isotopes such as Cu-64, Adarulatide tetraxetan demonstrates reliable biodistribution, target retention, and renal clearance, essential properties for diagnostic accuracy and safety.

Diagnostic Applications

Adarulatide tetraxetan is primarily applied in molecular imaging for cancer diagnostics. It binds to specific receptors expressed on tumor cells, allowing real-time visualization and quantification of receptor density using PET or SPECT.

Key research applications include:

• Radiometal chelation and radiolabeling studies

• PET imaging of tumor-associated receptors

• Biodistribution and pharmacokinetic profiling

• Preclinical evaluation of novel peptide tracers

• Development of theranostic agents (diagnostic + therapeutic hybrids)

Advantages of Adarulatide Tetraxetan

• High Radiometal Affinity: Strong coordination with Cu, Ga, Lu, and Y isotopes.

• Excellent Stability: Resistant to demetallation in physiological environments.

• High Target Selectivity: Enables precise imaging of receptor-overexpressing tissues.

• Versatile Platform: Can be adapted for both diagnostic and therapeutic labeling.

• Biocompatible Design: Minimal toxicity and predictable metabolic clearance.

Product Specifications

Mechanism of Action

The mechanism of Adarulatide tetraxetan lies in radiometal chelation and receptor-mediated targeting for imaging applications.

1. Chelation Chemistry

   • The tetraxetan (DOTA-like) macrocycle forms a highly stable coordination complex with radiometals.

   • This ensures that the radiometal remains tightly bound during circulation and imaging, reducing background signal.

2. Receptor Targeting

   • The peptide portion of Adarulatide specifically binds to receptors (e.g., somatostatin, integrin, or prostate-specific membrane antigen, depending on the analog).

   • This allows selective uptake in receptor-overexpressing tissues, enhancing imaging contrast.

3. Radiolabeling with Copper Isotopes

   • Commonly used isotopes include Cu-64 (β+ emitter) for PET imaging.

   • Copper-labeled Adarulatide demonstrates predictable pharmacokinetics and renal excretion.

4. In Vivo Imaging Pathway

   • After intravenous administration, the compound circulates systemically, accumulates in receptor-rich tissues, and emits gamma or positron radiation.

   • This radiation is detected by imaging instruments to reconstruct real-time molecular maps of receptor distribution.

5. Theranostic Potential

   • When labeled with therapeutic isotopes like Lu-177, Adarulatide tetraxetan can transition from diagnostic to therapeutic use, providing a unified “theranostic” platform.

     

Side Effects

As a diagnostic imaging research compound, Adarulatide tetraxetan generally exhibits minimal toxicity in experimental settings. However, potential side effects in animal or in vitro studies include:

• Mild Cytotoxicity: At high concentrations in non-target tissues.

• Transient Radiation Exposure: Depending on the isotope used for labeling.

• Renal Accumulation: As common with peptide-based tracers, though reversible.

• Immunogenic Response: Minimal, due to synthetic peptide origin and neutral charge.

• Metal Complex Stability: Poor labeling procedures may lead to unbound radiometal presence.

Proper handling, labeling optimization, and biosafety protocols are essential during research use.

Disclaimer

For research use only. Not intended for human or veterinary use, diagnosis, or treatment.

Keywords

Adarulatide tetraxetan, CAS 1246013-02-4, copper adarulatide, DOTA conjugate, radiometal chelator, Cu-64 PET imaging agent, peptide-based diagnostic tracer, molecular imaging probe, radiopharmaceutical precursor, receptor-targeted imaging

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