Galacto-RGD | CAS 922175-70-0 | Integrin αvβ3-Selective RGD Tracer for Radiopharmaceutical Research

Description

Product Description

Galacto-RGD is a synthetic derivative of the well-known arginine-glycine-aspartic acid (RGD) motif, engineered for high-affinity targeting of integrin αvβ3 receptors, which are overexpressed in tumor neovasculature and various cancer cell types. This compound incorporates a galactose moiety that enhances hydrophilicity and in vivo pharmacokinetics, making it a superior candidate for radiolabeling and molecular imaging research.

In radiopharmaceutical development, Galacto-RGD serves as a precursor molecule that can be conjugated with positron-emitting isotopes such as ¹⁸F. The resulting labeled derivatives (e.g., [¹⁸F]Galacto-RGD) have been extensively studied in positron emission tomography (PET) imaging of tumor angiogenesis and metastasis.

Biological Relevance and Mechanistic Insight

Integrins are transmembrane receptors mediating cell–extracellular matrix interactions, playing crucial roles in cell adhesion, migration, and signaling. Among them, integrin αvβ3 is a key biomarker of angiogenesis, making it an ideal target for tumor imaging. Galacto-RGD’s RGD sequence binds to the αvβ3 binding pocket with nanomolar affinity, while the galactose substituent improves solubility, clearance, and metabolic stability in vivo.

This dual-functional design has made Galacto-RGD one of the earliest and most reliable RGD-based PET tracers used in translational research and clinical imaging trials.

Research Applications

Galacto-RGD plays a versatile role in molecular imaging and targeted drug discovery. Its main applications include:

• PET imaging agent precursor: For radiolabeling with ¹⁸F via prosthetic groups such as N-succinimidyl-4-(fluoromethyl)benzoate (SFB).

• Integrin-targeted tracer studies: Evaluating αvβ3 expression in angiogenic tissues, tumors, and metastases.

• Radionuclide-drug conjugate (RDC) synthesis: Serving as a targeting moiety for theranostic constructs combining diagnostic and therapeutic isotopes.

• Pharmacokinetic and biodistribution analysis: Studying RGD-peptide transport and clearance in vivo.

By incorporating Galacto-RGD into RDCs or imaging probes, researchers can achieve precise localization and quantification of integrin expression — a key parameter in monitoring tumor progression and therapeutic response.

Product Specifications

Mechanism of Action

Galacto-RGD functions through the RGD–integrin αvβ3 interaction, a well-characterized molecular recognition event. The RGD tripeptide motif binds to the extracellular domain of αvβ3, stabilizing ligand–receptor interaction via ionic and hydrogen bonding with the aspartic acid residue and the metal ion-dependent adhesion site (MIDAS).

When radiolabeled, [¹⁸F]Galacto-RGD binds selectively to αvβ3-expressing cells, allowing non-invasive quantification of receptor density through PET imaging. This specific binding enables researchers to monitor angiogenesis, assess tumor aggressiveness, and evaluate therapeutic efficacy of anti-angiogenic drugs.

The galactose modification improves pharmacokinetic parameters by enhancing hydrophilicity and reducing nonspecific liver uptake, resulting in clearer imaging contrast and faster renal clearance. Consequently, Galacto-RGD represents a benchmark compound for next-generation RGD analogues in nuclear medicine and molecular diagnostics.

Side Effects

In experimental settings, Galacto-RGD demonstrates excellent tolerability and biochemical stability. It exhibits no intrinsic cytotoxicity, as its biological activity is limited to integrin receptor binding without triggering signaling cascades.

Potential laboratory observations may include:

• Minimal nonspecific binding to non-αvβ3 tissues

• Rapid in vivo clearance after radiolabeling

• Low background uptake in non-targeted organs

Nevertheless, as a radiopharmaceutical precursor, all ¹⁸F-labeled derivatives should be handled in compliance with institutional radiation safety procedures and good laboratory practices.

Keywords

Galacto-RGD, 922175-70-0, [¹⁸F]Galacto-RGD precursor, integrin αvβ3 tracer, RGD analogue, radiopharmaceutical peptide, molecular imaging agent, PET tracer precursor, angiogenesis imaging probe, radionuclide-drug conjugate synthesis

Shipping Guarantee

All shipments are handled using validated cold-chain logistics to preserve peptide integrity. Each package is sealed in moisture-proof containers with secondary protective wrapping and continuous temperature monitoring. Products are shipped via express international couriers with full tracking and insurance coverage.

Trade Assurance

We ensure product authenticity, verified ≥99% purity, and compliance with analytical standards (HPLC, MS, and NMR). Each batch is supplied with a Certificate of Analysis (CoA). Our trade assurance policy guarantees replacement or refund for any deviation from listed specifications.

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