Methyltetrazine-propylamine
CAS No.: 1802978-47-7
Cat No.: BP-501472
Purity: 98%
4.5 
Methyltetrazine-propylamine is a bifunctional PROTAC linker building block featuring a tetrazine moiety conjugated through a propylamine spacer. Structurally, it provides an electrophilic tetrazine handle commonly used in inverse-electron-demand Diels–Alder chemistry, enabling rapid and selective ligation to strained dienophiles (e.g., trans-cyclooctene or bicyclononyne derivatives) that are installed on either the targeting ligand or the E3 ligase ligand. The propylamine segment offers a flexible, water-compatible linker region that can support stable amide or urea formation during synthesis and can tune effective spatial positioning between the two recruited components. In targeted protein degradation workflows, this linker facilitates modular assembly of PROTACs by orthogonally connecting functional domains under mild conditions, improving synthetic efficiency and allowing systematic optimization of linker length and geometry to enhance ternary complex formation. It is therefore valuable for researchers developing next-generation, modular degradation constructs and for rapid library generation where consistent conjugation chemistry is required.
Structure of 1802978-47-7
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Methyltetrazine-propylamine is a bifunctional PROTAC linker building block designed to enable efficient conjugation between targeting ligands and protein-recruiting modules. Its tetrazine functionality supports bioorthogonal reactivity with strained partners, while the amine handle facilitates robust coupling strategies. This combination improves synthetic flexibility and can streamline workflows for constructing targeted protein degradation (TPD) constructs. The following sections describe the linker’s structure and practical reactivity considerations in detail.
Structure: The linker contains a methyltetrazine ring connected through a propyl chain to a primary amine. It features heteroaromatic nitrogen-rich functionality and a flexible aliphatic segment, providing suitable spacing and conformational adaptability. The amine enables salt formation and nucleophilic coupling under standard organic conditions.
Reactivity: The methyltetrazine moiety is suited to inverse-electron-demand Diels–Alder-type bioorthogonal ligation with strained dienophiles, typically performed under mild aqueous-compatible conditions. The primary amine can be used for amide bond formation, reductive amination, or carbamate/urea synthesis depending on the activated partner. Common approaches employ coupling reagents and bases in polar aprotic or mixed solvents, with temperature and pH optimized to preserve sensitive targeting ligands.
* 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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