Anwendungsbeispiele
Anwendungsbeispiele
Der Liberty Blue Mikrowellen-Peptid-Synthesizer ist der meistverkaufte Peptid-Synthesizer der Welt. Er zeichnet sich durch eine Zykluszeit von 4 Minuten und eine 90%ige Lösemittelreduktion auf Basis der im Jahr 2013 entwickelten High Efficiency Solid Phase Peptide Synthese (HE-SPPS) aus.
Liberty Blue 2.0
Anwendungsbeispiele
- Synthese von Standard- und komplexen Peptiden
- Verzweigte Peptide
- Zyklisierte Peptide
- Disulfidbindung
- Glycopeptide (N/O-verbunden)
- Hochdurchsatz-Synthese
- N-Methyl-Peptide
- Peptid-Thioester
- Peptoide
- Phosphopeptide
- PNA
Cyclic disulfide-bridged peptides can be prepared rapidly with good purity using microwave-enhanced SPPS on the Liberty Blue automated microwave peptide synthesizer. Synthesis of the peptide hormone oxytocin was achieved in under 3 h with 69% purity. Preparation of a peptide agonist of BMP receptor activin-like kinase 3 (Alk3), THR-123, was completed in 3 h with 77% purity. CHEC-7, a neuroprotective peptide inhibitor of amyloidogenesis, was prepared in under 3 h with 80% purity. Finally, a peptide venom from cone snails containing two disulfide bridges (conotoxin-SI) was synthesized in under 4 h with 67% purity.
The Liberty Blue can accomodate a wide range of post-synthetic modifications such as N-terminal acetylation. Microwave-enhanced SPPS on the Liberty Blue produced nonacetylated and acetylated peptides at 78% and 72% respecitivly with a combined time of 2 hr 16 min and a total of < 200 mL of main wash (DMF) consumed.
Glycopeptides containing O-linked glycans can be synthesized quickly with good purity using microwave-enhanced SPPS. Preparation of a peptide substrate of WbwA (a sialic acid glycosyltransferase), was completed in 3 h 10 min with 68% purity on the Liberty Blue automated microwave peptide synthesizer. Synthesis of an analog of APF (antiproliferative factor) conjugated to the TUS nuclear localization sequence was achieved in 1 h 8 min with 73% purity using the Liberty PRIME automated microwave peptide synthesizer.
This application note demonstrates that His(Boc) is a powerful His derivative that can be effectively coupled at 90 °C, providing favorable crude purity while both decreasing coupling time and dramatically reducing epimerization. Fmoc-His(Boc)-OH is widely available as compared to other epimerization suppressing Nπ protected derivatives while maintaining comparable synthetic performance. In summary, the key benefits of Fmoc-His(Boc)-OH are:
- Commercial bulk availability and competitive price relative to Fmoc-His(Trt)-OH.
- Low epimerization levels at elevated temperatures; coupling temperatures of 50 °C and below make Fmoc-His(Boc)-OH applicable for use in the synthesis of active pharmaceutical ingredients and avoiding complex coupling reagents and conditions.
- Excellent solution stability; comparable to Fmoc-His(π-Mbom)-OH and greater than Fmoc-His(Trt)-OH.
This application note demonstrates that His(Boc) is a powerful His derivative that can be effectively coupled at 90 °C, providing favorable crude purity while both decreasing coupling time and dramatically reducing epimerization. Fmoc-His(Boc)-OH is widely available as compared to other epimerization suppressing Nπ protected derivatives while maintaining comparable synthetic performance. In summary, the key benefits of Fmoc-His(Boc)-OH are:
- Commercial bulk availability and competitive price relative to Fmoc-His(Trt)-OH.
- Low epimerization levels at elevated temperatures; coupling temperatures of 50 °C and below make Fmoc-His(Boc)-OH applicable for use in the synthesis of active pharmaceutical ingredients and avoiding complex coupling reagents and conditions.
- Excellent solution stability; comparable to Fmoc-His(π-Mbom)-OH and greater than Fmoc-His(Trt)-OH.