| Target Molecule | Ganirelix |
| Synonyms | Orgalutran, Antagon, Fyremadel, RS-26306, Ganirelix Acetate |
| CAS Number | 123246-29-7 (free base); 129311-55-3 (acetate salt) |
| Sequence (3-Letter) | Ac-D-Nal(2)-D-Phe(4-Cl)-D-Pal(3)-Ser-Tyr-D-hArg(Et2)-Leu-hArg(Et2)-Pro-D-Ala-NH₂ |
| Sequence (1-Letter) | Ac-[D-2Nal]-[D-4ClPhe]-[D-3Pal]-S-Y-[D-hArg(Et2)]-L-[hArg(Et2)]-P-[D-Ala]-NH₂ |
| Molecular Formula | C₈₀H₁₁₃ClN₁₈O₁₃ (free base) |
| Molecular Weight | 1570.3 (free base) |
| 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 | Acetate (standard pharmaceutical form), TFA, or custom salt options |
| Synthesis Technology | Solid-Phase Peptide Synthesis (SPPS) for Unnatural and D-Amino Acids |
| Modification Options | Unnatural amino acid incorporation, D-amino acid substitution, C-terminal amidation, stable isotope labeling (13C, 15N), diastereomer impurity standards |
| Available Scale | Milligram (R&D) to Kilogram (Commercial CDMO) |
| Analytical Data | Comprehensive COA, HPLC, MS, and chiral purity confirmation provided per batch |
| Usage | Raw material synthesized strictly for laboratory research, analytical development, and industrial formulation. Not a finished medicine. |
Ganirelix (CAS 123246-29-7) is a synthetic decapeptide functioning as a potent third-generation GnRH antagonist. Its sequence features extensive non-standard modifications, including D-amino acids and unnatural residues such as D-Nal(2), D-Phe(4-Cl), D-Pal(3), and two N,N-diethyl-homoarginine units. We target this sequence to supply high-purity reference materials and raw materials for reproductive endocrinology and oncology research.
Incorporating bulky unnatural building blocks and D-enantiomers alters coupling kinetics and increases the risk of epimerization during solid-phase peptide synthesis (SPPS). Our peptide synthesis platform utilizes specialized coupling cocktails, steric-hindrance-minimizing conditions, and real-time monitoring to prevent deletion sequences and achieve high stereochemical purity.
Yes. We provide extensive peptide modification services for GnRH antagonists. Capabilities include the synthesis of specific diastereomers and deletion sequences as critical impurity reference standards, site-specific stable isotope labeling (13C, 15N) for quantitative LC-MS/MS, and fluorescent labeling.
Our manufacturing infrastructure scales production from milligram-level analytical batches to multigram and kilogram commercial quantities. We optimize preparative HPLC purification and controlled counter-ion exchange (ensuring acetate salt conversion) to guarantee strict batch-to-batch consistency.
We operate as an integrated technical partner providing complete peptide CDMO solutions. Our team manages sequence optimization, impurity profiling, analytical method validation, and regulatory documentation to accelerate complex preclinical and commercial pipelines.
Ganirelix (CAS 123246-29-7), known under trade names such as Orgalutran and Antagon, is a synthetic decapeptide operating as a competitive gonadotropin-releasing hormone (GnRH) receptor antagonist. Defined by the heavily modified sequence Ac-[D-2Nal]-[D-4ClPhe]-[D-3Pal]-S-Y-[D-hArg(Et2)]-L-[hArg(Et2)]-P-[D-Ala]-NH2, it incorporates unnatural residues, D-enantiomers, N-terminal acetylation, and C-terminal amidation. Synpeptide provides comprehensive synthetic solutions for this molecule, showcasing our technical expertise in non-standard amino acid incorporation, stereochemical control, and CDMO manufacturing.
The assembly of Ganirelix presents substantial synthetic obstacles. Bulky non-canonical residues like N,N-diethyl-homoarginine [hArg(Et2)] and halogenated amino acids generate severe steric hindrance, leading to incomplete coupling cycles and on-resin aggregation. Our custom peptide synthesis platform resolves these hurdles using optimized Solid-Phase Peptide Synthesis (SPPS) protocols on low-loading amide resins. By utilizing targeted activating reagents and strictly regulated coupling parameters, we suppress deletion fragments and epimerization, delivering raw materials with rigorous purity specifications (typically ≥95% or ≥98% via HPLC).
Due to multiple chiral centers and unnatural residues, Ganirelix requires comprehensive analytical validation. Diastereomeric impurities arising from partial racemization can compromise biological activity. Through our peptide modification services, we synthesize deliberate diastereomeric variants and deletion sequences as reference standards for stability-indicating assays. We also offer site-specific stable isotope labeling (13C, 15N) for pharmacokinetic mass spectrometry and fluorescently tagged analogues for receptor-binding studies.
Moving a heavily modified decapeptide from exploratory R&D to multi-gram or commercial volume demands robust downstream process engineering. The unique hydrophobic and basic properties of the non-standard residues require customized chromatographic isolation. We execute large-scale peptide synthesis for Ganirelix by optimizing preparative HPLC purification and controlled lyophilization. Our infrastructure accommodates demands from milligram batches to kilogram commercial lots, ensuring consistent counter-ion exchange (providing the pharmaceutical acetate salt form) across all production volumes.
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 analytical documentation—including COA, HPLC purity traces, and exact mass confirmation—ensuring regulatory alignment for downstream therapeutic programs.
