| Target Molecule | Pasireotide (SOM230) |
| Synonyms | SOM230, Signifor, Pasireotide diaspartate |
| CAS Number | 396091-73-9 (free base); 820232-50-6 (diaspartate salt) |
| Sequence (3-Letter) | cyclo[-(4R)-4-(2-aminoethylcarbamoyloxy)-Pro-Phg-D-Trp-Lys-Tyr(Bzl)-Phe-] |
| Sequence (1-Letter) | cyclo[Hyp*-Phg-(D-Trp)-K-Tyr(Bzl)-F] |
| Molecular Formula | C₅₈H₆₆N₁₀O₉ (free base) |
| Molecular Weight | 1047.2 (free base); diaspartate salt ≈ 1313.4 |
| Service Category | Custom Peptide Synthesis / CDMO Manufacturing |
| Synthesis Purity | Customizable (e.g., ≥95%, ≥98% via HPLC) |
| Appearance | White to off-white lyophilized powder |
| Counter Ion | Diaspartate (standard pharmaceutical salt), acetate, or custom options |
| Synthesis Technology | Solid-Phase Peptide Synthesis (SPPS) and Head-to-Tail Macrolactamization |
| Modification Options | Backbone cyclization, unnatural amino acid incorporation, stable isotope labeling (13C, 15N), linear precursor impurity standards |
| Available Scale | Milligram (R&D) to Kilogram (Commercial CDMO) |
| Analytical Data | Comprehensive COA, HPLC, MS, and cyclization verification provided per batch |
| Usage | Raw material synthesized strictly for laboratory research, analytical development, and industrial formulation. Not a finished medicine. |
Pasireotide (SOM230, CAS 396091-73-9) is a synthetic cyclic hexapeptide somatostatin analogue containing four unnatural residues. We target this sequence to supply high-purity reference materials and raw materials for endocrine, oncology, and metabolic disease research.
Unlike disulfide-bridged analogues, Pasireotide requires head-to-tail amide bond macrolactamization. Our peptide synthesis platform utilizes low-loading resins and optimized solution-phase or on-resin cyclization protocols under high-dilution conditions, suppressing intermolecular dimer/oligomer formation to isolate the monomeric cyclic peptide.
Yes. Pasireotide incorporates phenylglycine, D-tryptophan, O-benzyl-tyrosine, and modified hydroxyproline. Our peptide modification services synthesize these specialized building blocks with verified chiral purity, and we intentionally prepare uncyclized linear precursors and diastereomeric variants as impurity reference standards.
Our manufacturing infrastructure scales production from milligram analytical batches to multigram and kilogram commercial quantities. We utilize continuous-flow cyclization systems, high-capacity preparative HPLC, and controlled counter-ion exchange (providing diaspartate or acetate forms) to guarantee consistent lot-to-lot profiles.
We operate as an integrated technical partner providing complete peptide CDMO solutions. Our team manages sequence optimization, macrolactamization verification, impurity profiling, analytical method validation, and regulatory documentation to support complex clinical-stage development.
Pasireotide (SOM230, CAS 396091-73-9), commercialized as Signifor in its diaspartate salt form, is a synthetic cyclic hexapeptide engineered as a broad-spectrum somatostatin receptor agonist. Defined by the sequence cyclo[Hyp*-Phg-(D-Trp)-K-Tyr(Bzl)-F], it incorporates four distinct unnatural building blocks and head-to-tail backbone cyclization. Synpeptide delivers comprehensive custom synthesis solutions for this molecule, showcasing our technical capabilities in homodetic macrolactamization, unnatural amino acid assembly, and CDMO manufacturing.
Synthesizing a head-to-tail cyclic hexapeptide composed of sterically congested, non-canonical residues presents severe synthetic challenges. The combination of bulky side chains, such as O-benzyl-tyrosine and 4-(2-aminoethylcarbamoyloxy)proline, reduces coupling rates during solid-phase elongation. Our custom peptide synthesis platform resolves these hurdles using optimized Solid-Phase Peptide Synthesis (SPPS) protocols on specialized orthogonal resins. By applying high-efficiency coupling reagents and controlled macrolactamization regimes, we suppress truncated linear sequences and epimerization, delivering raw materials with rigorous purity specifications (typically ≥95% or ≥98% via HPLC).
The unique receptor selectivity of Pasireotide relies on its exact three-dimensional conformation, governed by D-Trp and L-phenylglycine (Phg). The phenylglycine residue is particularly prone to racemization during peptide activation. Through our peptide modification services, we implement mild, low-racemization coupling methods to preserve chiral purity. We also synthesize uncyclized linear precursors, polymeric oligomers, and specific diastereomeric variants as critical reference standards for stability-indicating analytical assays, alongside stable isotope-labeled analogues (13C, 15N) for pharmacokinetic bioanalysis.
Transitioning an intramolecularly cyclized hexapeptide from laboratory screening to commercial production requires specialized chemical engineering. High-dilution conditions required to prevent oligomerization generate massive liquid volumes during scale-up. We execute large-scale peptide synthesis for Pasireotide utilizing continuous-flow liquid-phase cyclization and high-capacity preparative HPLC purification. Our facilities accommodate requirements from milligram research batches to kilogram commercial lots, ensuring uniform counter-ion exchange to produce the exact diaspartate or acetate salt forms required by pharmaceutical manufacturers.
We deliver comprehensive technical support as a fully integrated peptide CDMO. Our development specialists assist pharmaceutical partners with process optimization, stability testing, impurity identification, and analytical method validation. Every batch is released with complete documentation—including COA, HPLC purity traces, and exact mass confirmation by high-resolution MS—ensuring regulatory alignment for downstream therapeutic programs.
