Synthesis of tritium labeled 30‐KDa PEG and conjugation to form [ 3 H]Pegbelfermin
Autor: | Yuan Tian, Richard C. Burrell, John A. Easter, Yang Hong, Samuel J. Bonacorsi |
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Rok vydání: | 2021 |
Předmět: |
education.field_of_study
FGF21 Chemistry Organic Chemistry Population Type 2 diabetes Metabolism Pharmacology medicine.disease Biochemistry Analytical Chemistry Drug Discovery PEG ratio medicine Radiology Nuclear Medicine and imaging Specific activity Animal studies Steatohepatitis education Spectroscopy |
Zdroj: | Journal of Labelled Compounds and Radiopharmaceuticals. 64:477-481 |
ISSN: | 1099-1344 0362-4803 |
Popis: | Non-alcoholic steatohepatitis (NASH) is the most chronic liver condition in the western population and is fueled by the obesity and type 2 diabetes epidemic. Pegbelfermin (1), a PEGylated human fibroblast growth factor 21 (FGF21) analogue, has previously been shown to improve markers of metabolism and liver fibrosis in obese patients with type 2 diabetes. Radiolabeled Pegbelfermin was needed to access the accumulation of intact drug and metabolized PEG. In an effort to accomplish both goals with one labeled synthesis, the isotopic label was positioned in the PEG. A total of 21 mCi of tritium labeled Pegbelfermin was synthesized having a specific activity of 21.6 Ci/mmol for use in animal studies. |
Databáze: | OpenAIRE |
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