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Tetrazine-containing Bifunctional Reagents

Tetrazine-containing reagents are suitable for the introduction of

  • a functional group (e.g. Amine or NHS Ester) to Cyclooctene-labeled molecules via Cu-free Click Chemistry
  • an Tetrazine group to various targets e.g. via NHS Ester- or Maleimide-based chemistry

Two Tetrazine versions with different reactivities and stability characteristics are available to meet specific application requirements. Tetrazine reagents are the ideal choice if a rapid reaction kinetic is the key aspect whereas 6-Methyl-Tetrazine reagents are ideally suited if an improved chemical stability is required[1].


Table 1: Available Tetrazine-containing Bifunctional Reagents

Reactive Group6-Methyl-TetrazineTetrazine
NHS ester6-Methyl-Tetrazine-PEG5-NHS esterTetrazine-PEG5-NHS ester
Amine (-NH2)6-Methyl-Tetrazine-AmineTetrazine-Amine

Selected References

[1] Karver et al. (2011) Synthesis and Evaluation of a Series of 1,2,4,5-Tetrazines for Bioorthogonal Conjugations. Am. Chem. Soc. 22:2263.