Methyltetrazine-PEG13-acid
Methyltetrazine-PEG13-acid is a PEG-based PROTAC linker featuring a methyltetrazine functional group and a terminal carboxylic acid. The PEG13 chain provides a flexible, hydrophilic spacer that can reduce steric interference and help position the reactive warhead for efficient conjugation and productive ternary complex formation. In targeted protein degradation workflows, the methyltetrazine moiety is designed for bioorthogonal inverse-electron-demand Diels–Alder reactivity with strained dienes (commonly trans-cyclooctenes or related motifs), enabling modular assembly of PROTACs by linking an E3 ligase ligand and a target-binding ligand through a defined spacer. The terminal acid supports further synthetic handling and, depending on the overall construct, can improve solubility and facilitate downstream coupling strategies. This linker is valuable for researchers developing chemically precise, modular targeted degradation agents where controllable geometry and efficient conjugation are critical for maintaining degradation potency and cellular performance.
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* For research and manufacturing use only. Not for human or clinical use.
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Methyltetrazine-PEG13-acid is a bifunctional PEG-based linker designed for constructing PROTACs that employ tetrazine-mediated bioorthogonal ligation. Its polyethylene glycol segment promotes solubility and flexible spacing between binding elements, while the methyltetrazine handle enables efficient coupling to compatible partners under mild conditions. The terminal carboxylic acid functionality supports robust conjugation strategies commonly used to assemble targeted protein degradation constructs. The following points describe the structure and reactivity characteristics in detail below.
Structure: The linker comprises a methyltetrazine moiety connected to a long, flexible polyethylene glycol chain terminating in a carboxylic acid. It contains heteroaromatic nitrogen-rich functionality and ether linkages, with a polar, hydrogen-bonding surface that favors aqueous compatibility and conformational mobility.
Reactivity: The methyltetrazine group undergoes inverse-electron-demand Diels–Alder reactions with strained dienes (e.g., trans-cyclooctene derivatives) to form stable conjugates. Typical PROTAC assembly uses mild aqueous or mixed-solvent conditions, controlled pH, and moderate temperature to preserve sensitive ligands. Conjugation to the acid terminus is commonly achieved via amide-forming coupling chemistries using standard activating reagents and compatible bases, without requiring harsh catalysts.
* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C1V1 = C2V2
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