DOTA.SA.FAPi (TFA) combines a fibroblast-activation-protein-targeting motif with a DOTA chelator, allowing coordination of radiometals or lanthanides. The peptide moiety directs binding to FAP-expressing environments in model systems, while the macrocycle controls metal complexation. Researchers study its thermodynamic stability and receptor affinity. Applications include targeted-imaging ligand development, coordination chemistry, and peptide-chelator optimization.
DOTA.SA.FAPi (TFA) is a synthetic peptide conjugate that integrates a fibroblast activation protein inhibitor (FAPi) motif with a DOTA chelator, provided as a trifluoroacetate (TFA) salt. This compound is specifically engineered for advanced biochemical and molecular imaging research, where selective targeting of fibroblast activation protein (FAP) is essential. The DOTA chelator enables subsequent radiometal labeling, making the construct highly versatile for applications in tracer development, target validation, and in vitro or in vivo studies of FAP-expressing biological systems. Its modular design and specificity have established it as a valuable tool in the expanding field of tumor microenvironment research and fibroblast biology.
Radiolabeling Development: The DOTA component of DOTA.SA.FAPi (TFA) supports robust chelation of a wide range of radiometals, including gallium-68, lutetium-177, and indium-111, facilitating the synthesis of radiolabeled probes for molecular imaging and biodistribution studies. Researchers utilize this peptide conjugate to generate radiotracers that enable the precise visualization and quantification of FAP expression in cell cultures, tissue sections, or animal models. Its high chelation efficiency and structural stability help ensure reliable incorporation of radioisotopes, which is critical for the development and optimization of novel imaging agents.
Fibroblast Activation Protein Targeting: The FAPi motif confers selective binding affinity toward fibroblast activation protein, a serine protease overexpressed in cancer-associated fibroblasts and certain pathological tissue environments. By leveraging this specificity, the compound is widely employed in studies aiming to investigate the distribution, density, and functional role of FAP in tumor stroma or fibrotic tissues. Its application extends to the screening and validation of FAP-targeted diagnostics, allowing researchers to evaluate ligand-receptor interactions, assess target engagement, and explore FAP's contributions to disease mechanisms.
Tumor Microenvironment Characterization: DOTA.SA.FAPi (TFA) serves as a molecular probe in the detailed analysis of the tumor microenvironment, particularly in the context of stromal remodeling and tumor-stroma interactions. By enabling targeted delivery of imaging agents or functional payloads, it supports investigations into the spatial and temporal dynamics of fibroblast activation, extracellular matrix remodeling, and cellular crosstalk within tumors. Such studies are instrumental in elucidating the role of stromal components in tumor progression, metastasis, and resistance to therapy.
Peptide-Driven Imaging Agent Research: The synthetic peptide backbone of this conjugate allows for the exploration of structure-activity relationships and optimization of peptide-based imaging agents. Researchers employ DOTA.SA.FAPi (TFA) as a scaffold for modifying peptide sequence, linker chemistry, or chelator selection, thereby tuning pharmacokinetics, binding affinity, and in vivo stability. This flexibility is invaluable in the iterative process of developing next-generation imaging probes or targeted delivery systems for preclinical research.
In Vitro Assay Development: The well-defined structure and FAP specificity of the compound make it suitable for use in a variety of in vitro assay formats. It is frequently applied in binding assays, competitive displacement studies, and cell-based functional assays to quantify FAP expression or activity. These applications provide critical data for the screening of novel inhibitors, the assessment of compound selectivity, and the validation of FAP as a biomarker or therapeutic target in diverse biological models.
1. Myotropic activity of allatostatins in tenebrionid beetles
2. SERS spectrum of the peptide thymosin‐β4 obtained with Ag nanorod substrate
4. Cationic cell-penetrating peptides are potent furin inhibitors
5. Emerging applications of nanotechnology for diagnosis and therapy of disease: a review
If you have any peptide synthesis requirement in mind, please do not hesitate to contact us at . We will endeavor to provide highly satisfying products and services.
Creative Peptides is a trusted CDMO partner specializing in high-quality peptide synthesis, conjugation, and manufacturing under strict cGMP compliance. With advanced technology platforms and a team of experienced scientists, we deliver tailored peptide solutions to support drug discovery, clinical development, and cosmetic innovation worldwide.
From custom peptide synthesis to complex peptide-drug conjugates, we provide flexible, end-to-end services designed to accelerate timelines and ensure regulatory excellence. Our commitment to quality, reliability, and innovation has made us a preferred partner across the pharmaceutical, biotechnology, and personal care industries.
Read More