Premium
[ 125 I]‐ and [ 14 C]‐labelling of the long‐acting insulin derivative NN304
Author(s) -
Kristensen Jesper B.,
Müller Lars K.,
Larsen Ulla D.,
Hansen Louis B.,
Foged Christian
Publication year - 2000
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/1099-1344(200006)43:7<671::aid-jlcr352>3.0.co;2-l
Subject(s) - chemistry , labelling , insulin , human insulin , yield (engineering) , human serum albumin , lactoperoxidase , conjugate , biochemistry , tyrosine , peptide , chromatography , enzyme , peroxidase , medicine , mathematical analysis , materials science , mathematics , metallurgy
Lys ϵB29 Tetradecanoyl des(B30) human insulin, Novo Nordisk code no NN304, is a long‐acting human insulin derivative that differs from human insulin by being more than 98% albumin bound in plasma. The syntheses of [ 125 I]Tyr A14 N ϵ ‐Lys ϵB29 Tetradecanoyl des (B30) human insulin ([ 125 I]NN304) and Lys ϵB29 [I‐ 14 C]‐Tetradecanoyl des (B30) human insulin ([ 14 C]NN304) used for absorption, distribution, metabolism and excretion (ADME) studies are described. NN304 was radio‐iodinated using the lactoperoxidase/hydrogen peroxide method, and the product was isolated using RP‐HPLC. Radio‐peptide mapping confirmed the [ 125 I] labelling position at Tyrosine 14 in the A‐chain. The radio‐chemical yield was 30% with a radiochemical purity of >98%. [ 14 C]NN304 was synthesised in two steps starting from 1‐[ 14 C] myristic acid and subsequently purified by HPLC. The overall radiochemical yield was 15% with a radiochemical purity >98%. Copyright © 2000 John Wiley & Sons, Ltd.