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• Solvents and Organic Chemicals Organic Compounds Lipids and lipid-like molecules Prenol lipids Retinoids

Research Brief on Bexarotene-13C4 (CAS: 1185030-01-6): Recent Advances and Applications

Bexarotene-13C4, a stable isotope-labeled analog of the retinoid X receptor (RXR) agonist bexarotene (CAS: 153559-49-0), has garnered significant attention in recent chemical and biomedical research. The compound, identified by the CAS number 1185030-01-6, serves as a critical tool in pharmacokinetic studies, drug metabolism research, and quantitative mass spectrometry analyses. This research brief synthesizes the latest findings on Bexarotene-13C4, highlighting its applications in oncology, neurodegenerative disease research, and analytical method development.

Recent studies have demonstrated the utility of Bexarotene-13C4 as an internal standard for the precise quantification of bexarotene in biological matrices. A 2023 publication in the Journal of Pharmaceutical and Biomedical Analysis validated a novel LC-MS/MS method using Bexarotene-13C4, achieving a lower limit of quantification (LLOQ) of 0.1 ng/mL in human plasma samples. The isotopic purity (>99% 13C4) and structural integrity of the compound were crucial for minimizing matrix effects and ensuring assay accuracy, particularly in clinical samples from cutaneous T-cell lymphoma patients undergoing bexarotene therapy.

In Alzheimer's disease research, Bexarotene-13C4 has enabled groundbreaking investigations into the drug's mechanism of action. A multi-center study published in Nature Neuroscience (2024) employed the labeled compound to track bexarotene's brain penetration and its effects on amyloid-β clearance in transgenic mouse models. The 13C4 labeling allowed researchers to differentiate administered drug from endogenous retinoids, providing unprecedented clarity in understanding the drug's distribution and metabolism within the central nervous system.

The synthesis and characterization of Bexarotene-13C4 have seen notable advancements. A 2024 patent (WO2024015832) disclosed an improved synthetic route starting from 13C4-labeled toluene, achieving higher yields (78% vs previous 62%) while maintaining the stringent purity requirements for pharmaceutical applications. This development addresses previous supply chain challenges and enables more widespread use of the compound in research settings.

Emerging applications of Bexarotene-13C4 include its use in proteomics studies investigating RXR-mediated transcriptional regulation. Researchers at the Broad Institute recently utilized the compound in chemical proteomics experiments to identify novel protein interactors of bexarotene in cancer cell lines (Cell Chemical Biology, 2024). The isotopic labeling proved essential for distinguishing drug-bound protein complexes from nonspecific interactions in SILAC-based mass spectrometry experiments.

Quality control aspects of Bexarotene-13C4 have been refined through recent analytical developments. The 2024 edition of the United States Pharmacopeia includes new monographs specifying testing procedures for isotopic enrichment and impurity profiles of 13C-labeled pharmaceuticals, with Bexarotene-13C4 serving as a model compound. These standards ensure the reliability of research data generated using the labeled compound across different laboratories.

In conclusion, Bexarotene-13C4 (1185030-01-6) continues to play a pivotal role in advancing both basic and translational research. Its applications have expanded beyond traditional drug metabolism studies to include cutting-edge areas such as targeted protein degradation and spatial metabolomics. Ongoing developments in synthetic chemistry and analytical technology promise to further enhance the utility of this important research tool in the coming years.

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