Advanced Macrocyclization Linker Library
| Cat. No. : CS-L951 |
|---|
| （505） |
| Library Contents: |
| Macrocyclic scaffolds are increasingly valued in modern drug discovery for their exceptional activity against undruggable targets (proteases, kinases, PPIs). 2026 marks a key commercial breakthrough for oral macrocyclic peptides: enlicitide, the world’s first oral PCSK9 macrocyclic peptide, has received FDA approval. Macrocyclic candidates targeting KRAS and other classic undruggable targets have also entered clinical development, validating macrocyclization as an effective strategy to overcome druggability barriers. Two core R&D directions lead current macrocyclic drug design: AI-driven de novo generation and structural optimization of small-molecule macrocycles, and macrocyclic peptides based on sequence design and conformational engineering. Macrocycle druggability hinges on embedded linkers, which determine cyclization efficiency, final conformation and drug-like properties. Bifunctional reaction orthogonality is the core linker selection criterion. Our linker library enables stepwise intramolecular cyclization with suppressed side reactions, accommodates varied ring sizes, and covers three key reaction systems: amide condensation, nucleophilic substitution and CuAAC click chemistry. Built on classical macrocyclization systems, the library is processed through reaction classification, bifunctional orthogonality evaluation, novelty clustering and redundancy removal, with PROTAC long-chain and ADC cleavable linkers explicitly excluded. Featuring rigid, semi-rigid and flexible scaffolds, it is widely applicable to small-molecule macrocycle synthesis and linear peptide cyclization. |
| Size (Pre-dissolved DMSO or Solid) | Stock | Price |
|---|---|---|
| In-stock | Get quote |
Products are for research use only. Not for human use. We do not sell to patients.
Bulk Inquiry
CollapseYour information is safe with us. * Required Fields
Data Sheet
Description & Advantages
Composition
| Storage: | -80°C |
|---|
• A curated collection of bifunctional linkers for efficient synthesis of macrocyclic small molecules and cyclic peptides.
• Screened by reaction orthogonality, skeleton rigidity and span grading, covering three mainstream macrocyclization systems.
• All compounds are available off the shelf.
• All compounds are validated by LC-MS or NMR to ensure high purity and quality.
Browsing History
| Tags:Advanced Macrocyclization Linker Library supplier, Advanced Macrocyclization Linker Library purchase, Advanced Macrocyclization Linker Library manufacturer, Advanced Macrocyclization Linker Library sigma, Advanced Macrocyclization Linker Library distributor, cost, Advanced Macrocyclization Linker Library buy, Advanced Macrocyclization Linker Library for sale |