Fluorescent Probe to Confirm Drug Binding to Site I on HSA

Dansylamide (D5405) is a fluorescent probe that selectively interacts with drug binding site I on human serum albumin (HSA).¹)²) It is used in albumin binding assays to confirm drug binding to site I, as well as in drug discovery, R&D and metabolic toxicity assays. Its activity is not significantly different between fatty acid-free (FA-) and FA+ HSA. In an inhibition assay using 80 µM probe, 5 µM HSA (FA-), 1% DMSO in 10 mM phosphate buffer pH 7.2–7.5 at 20–25 °C for 30 minutes, with excitation/emission at 365/480 nm on a plate reader, displacement of the probe indicates binding to site I. Phenylbutazone inhibited dansylamide binding to site I in the brochure testing, while warfarin is often used as a positive control for site I. Combined with dansylglycine (D5406) for site II, dansylamide helps characterize the two drug binding sites on HSA, which is essential for pharmacokinetic and pharmacological studies.¹)²)

Related products

• TCI D5405 1431-39-6 Dansylamide [for Albumin binding assay]
• TCI D5406 1091-85-6 Dansylglycine [for Albumin binding assay]
• TCI D4898 1201643-08-4 BD140 [for Albumin binding assay]
• TCI I0415 15687-27-1 Ibuprofen
• TCI P1686 50-33-9 Phenylbutazone
• TCI F0371 5104-49-4 Flurbiprofen
• TCI T0451 88-82-4 2,3,5-Triiodobenzoic Acid
• TCI I0655 53-86-1 Indomethacin

References

1. Fluorescent Dye Cocktail for Multiplex Drug-Site Mapping on Human Serum Albumin. J. C. Er, M. Vendrell, M. K. Tang, D. Zhai, Y.-T. Chang, ACS Comb. Sci. 2013, 15, 452. doi:10.1021/co400060b
2. Structural Basis of the Drug-binding Specificity of Human Serum Albumin. J. Ghuman, P. A. Zunszain, I. Petitpas, A. A. Bhattacharya, M. Otagiri, S. Curry, J. Mol. Biol. 2005, 353, 38. doi:10.1016/j.jmb.2005.07.075
3. Study on Binding of Drug to Serum Protein. Y. Otagiri, YAKUGAKU ZASSHI 2009, 129, 413. doi:10.1248/yakushi.129.413
4. Structural and functional insights into S-thiolation of human serum albumins. F. Nakashima, T. Shibata, K. Uchida, et al., Sci. Rep. 2018, 8, 932. doi:10.1038/s41598-018-19610-9
5. Binding modes of environmental endocrine disruptors to human serum albumin: insights from STD-NMR, ITC, spectroscopic and molecular docking studies. H. Yang, Y. Huang, J. Liu, et al., Sci. Rep. 2017, 7, 11126. doi:10.1038/s41598-017-11604-3
6. 8‐Prenylnaringenin tissue distribution and pharmacokinetics in mice and its binding to human serum albumin and cellular uptake in human embryonic kidney cells. Y. Tanaka, H. Okuyama, R. Mukai, et al., Food Sci. Nutr. 2022, 10, 1070. doi:10.1002/fsn3.2733

Download TCI brochure Fluorescent Probes for the Characterization of Two Specific Drug Binding Sites on HSA (PDF)

Source

• TCI Product Highlights: www.tcichemicals.com/ID/en/product/tci-topics/ProductHighlights_20200323
• TCI product page D5405: tcichemicals.com/ID/en/p/D5405
• TCI product page D5406: tcichemicals.com/ID/en/p/D5406
• TCI product page D4898: tcichemicals.com/ID/en/p/D4898
• TCI brochure LL062: Fluorescent Probes for the Characterization of Two Specific Drug Binding Sites on HSA

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