Direct manufacturer pricing, multi-gram to multi-kilogram commercial capacity, HPLC purity ≥ 98.5%, and regulatory documentation.
Unraveling the biophysical properties, cellular energetics restoration, and therapeutic dynamics of the benchmark Szeto-Schiller peptide series.
SS-31 (Elamipretide, CAS No. 736992-21-5), structurally denoted as D-Arg-2',6'-Dmt-Lys-Phe-NH2, is an engineered aromatic-cationic tetrapeptide designed to overcome classic bio-membrane permeability barriers. With a molecular weight of 639.80 g/mol (free base), its synthetic structure alternates aromatic residues with basic amino acids, preventing premature enzymatic degradation by standard aminopeptidases.
The strategic inclusion of 2',6'-dimethyltyrosine (Dmt) confers exceptional scavenging capabilities against reactive oxygen species (ROS) while maintaining an optimal 3+ electrostatic charge at physiological pH 7.4. This allows for rapid cellular internalization independent of active transporters or receptor-mediated endocytosis pathways.
Unlike conventional small-molecule antioxidants that diffuse nonspecifically, SS-31 selectively concentrates >1,000-fold in the inner mitochondrial membrane (IMM). Its primary pharmacological target is cardiolipin, a unique dimeric phospholipid essential for maintaining cristae curvature and organizing the electron transport chain (ETC) supercomplexes.
Under oxidative stress and cellular aging, cardiolipin undergoes pathological peroxidation, leading to respiratory uncoupling, loss of mitochondrial membrane potential (ΔΨm), and release of cytochrome c. SS-31 penetrates the phosphate headgroups of cardiolipin via electrostatic and hydrophobic interactions, re-stabilizing cristae infrastructure and optimizing ATP synthesis.
Global pharmaceutical pipelines focus heavily on SS-31 for treating rare and orphan genetic mitochondrial disorders, most prominently Barth Syndrome, Primary Mitochondrial Myopathy (PMM), and Friedreich's Ataxia. In addition, its cardiac and renal protective features have positioned it as a cornerstone molecule for ischemia-reperfusion injury and acute kidney injury (AKI).
Recent commercial interest spans ophthalmology (Dry Age-Related Macular Degeneration / Geographic Atrophy) and neurodegenerative paradigms where neuroinflammation and bioenergetic collapse precipitate progressive cellular apoptosis.
| Analytical Parameter | Enterprise Quality Standard | Testing Methodology | Therapeutic Significance |
|---|---|---|---|
| Chemical Name | D-Arginyl-2',6'-dimethyl-L-tyrosyl-L-lysyl-L-phenylalaninamide | IUPAC Reference Validation | Ensures sequence purity & correct optical activity |
| CAS Number | 736992-21-5 (Free Base) / 1261596-73-9 (Acetate Salt) | Registry Cross-Check | Commercial traceability and customs clearance |
| Chromatographic Purity | ≥ 98.5% (Pharmaceutical) / ≥ 99.2% (Reference API) | RP-HPLC (UV detection at 220nm) | Minimizes isomeric and deletion peptide impurities |
| Single Max Unknown Impurity | ≤ 0.5% (ICH Q3A Guideline Compliance) | High-Resolution LC-MS / MS | Prevents immunogenicity in downstream formulation |
| Bacterial Endotoxins | ≤ 5.0 EU/mg (Parenteral Grade API) | LAL Kinetic Chromogenic Assay | Mandatory threshold for clinical injectables |
| Net Peptide Content | ≥ 80.0% to 88.0% (w/w) | Elemental Nitrogen / AAA (Amino Acid Analysis) | Crucial for exact dosage equivalence in formulations |
| Counter-Ion Content | Acetate (5.0% - 12.0%) or TFA (≤ 0.25% in desalted lot) | Ion Chromatography (IC) / 19F-NMR | Guarantees physiological tolerability and solubility |
Deconstructing synthesis economics, bulk tier volume discounts, raw material volatility, and cost-containment strategies for enterprise procurement leaders.
The manufacturing cost structure of SS-31 is heavily influenced by the availability of specialized building blocks, specifically Fmoc-2',6'-dimethyl-L-tyrosine (Fmoc-Dmt-OH). Unlike standard canonical amino acids, Dmt requires an 8-step chiral synthesis, positioning it as the single largest contributor (approx. 42-48%) to total raw material expenditure.
Secondarily, the resin matrix selected for Solid-Phase Peptide Synthesis (SPPS)—such as Sieber Amide Resin or Rink Amide-MBHA—dictates loading capacity and initial coupling yield. Thinheal optimizes this via high-load, low-swelling polymeric supports that substantially cut resin expenses per kilogram batch.
Procurement teams navigate three primary commercial pricing regimes based on lifecycle maturity:
Total Cost of Ownership (TCO) in peptide procurement extends far beyond spot FOB quotes. Experienced supply chain directors prioritize suppliers capable of providing comprehensive Drug Master File (DMF) support, residual solvent control (eliminating toxic class 1 & 2 solvents), and reproducible counter-ion exchange (converting TFA to pharmaceutical-grade acetate).
Working with integrated producers like Thinheal reduces late-phase regulatory auditing expenses and eliminates the 25-35% project delays commonly encountered when changing raw peptide suppliers before Phase III trials.
Exploring the state-of-the-art chemical engineering routes, purification advancements, green chemistry initiatives, and future synthetic roadmaps.
While standard Solid-Phase Peptide Synthesis (SPPS) using Fmoc chemistry is ideal for clinical batches, scaling SS-31 to hundreds of kilograms requires innovative Liquid-Phase / Hybrid Segment Condensation. The tetrapeptide backbone allows for a modular [2+2] convergent synthesis, coupling D-Arg(Pbf)-Dmt-OH with H-Lys(Boc)-Phe-NH2 in homogeneous solution.
This hybrid methodology drastically curbs solvent consumption (DMF/NMP) by up to 55%, optimizes coupling kinetics, reduces overall reaction cycle times, and mitigates the generation of deletion tripeptides that are notoriously difficult to resolve during chromatographic purification.
Downstream processing forms the key quality bottleneck. Utilizing industrial DAC (Dynamic Axial Compression) columns loaded with spherical 10μm C18 bonded silica, our process achieves baseline resolution between SS-31 and critical impurities, such as D-Arg-Tyr-Lys-Phe-NH2 (the des-methyl artifact).
Secondary orthogonal chromatography facilitates salt metathesis, replacing residual trifluoroacetate ions with pharmaceutically accepted acetate. Cryogenic, large-scale tray lyophilizers are then operated under automated primary and secondary drying cycles to secure a crystalline-like cake with water content strictly below 5.0%.
The peptide industry faces increasing environmental pressures under REACH and EPA standards regarding hazardous solvents (DCM, DMF, Piperidine). Thinheal implements Machine Learning (ML) algorithmic predictive modeling to simulate peptide folding and aggregation states prior to synthesis.
By transitioning to green solvents like 2-Methyltetrahydrofuran (2-MeTHF) and Cyrene, coupled with continuous PAT (Process Analytical Technology) monitoring inline NIR spectra, we enhance batch yield consistency while simultaneously lowering carbon footprints across our multi-ton synthesis base.
How international pharmaceutical purchasers navigate international regulatory frameworks, cold-chain customs clearance, and quality qualification.
To support Investigational New Drug (IND) and New Drug Applications (NDA), Thinheal supplies complete Module 3 Common Technical Documents (CTD) covering Section 3.2.S. This includes comprehensive synthetic route descriptions, characterization via high-field NMR (1H, 13C), HRMS, FTIR, and detailed validation of analytical procedures according to ICH Q2(R1).
In addition, stress testing datasets (thermal, photolytic, acid/base hydrolysis, oxidative degradation) are pre-packaged to assist sponsors in defending stability protocols during FDA, EMA, or PMDA inquiries.
Peptide APIs in lyophilized form exhibit relative stability, but improper transit handling can prompt hygroscopic degradation, aggregation, or counter-ion detachment. Every global consignment leaving Hangzhou is secured in temperature-monitored, validated dry-ice or +2°C to +8°C insulated vacuum shippers equipped with real-time GPS and temperature dataloggers.
Our experienced customs team manages biological import declarations, TSCA declarations in the US, and REACH declarations in the European Union, preventing customs holds and guaranteeing sample integrity upon arrival.
Recognizing the urgency of international clinical trial schedules, Thinheal deploys specialized regional desks covering North America & Western Europe, Russia & CIS, the Middle East, and the Asia-Pacific region. Our technical sales engineers operate on overlapping time zones, offering real-time bilingual consultation.
From initial sequence verification and CoA review to formal vendor qualification questionnaires and on-site cGMP facility audit arrangements, procurement teams experience direct, professional, and friction-free project governance.
Clear, direct answers regarding specifications, minimum order quantities, lead times, regulatory files, and formulation handling.
Thinheal manufactures both High-Purity Research Grade (≥ 98.0% HPLC purity) for assay development and early preclinical studies, and full Pharmaceutical / Parenteral Grade (≥ 98.5% to ≥ 99.2% purity) synthesized under strict cGMP protocols. Our parenteral batches feature verified bacterial endotoxin levels ≤ 5.0 EU/mg, controlled bioburden, and thoroughly documented residual solvent profiling adhering to ICH Q3C limits.
Because Fmoc-2',6'-dimethyl-L-tyrosine (Dmt) is the key chiral monomer of SS-31, we run an in-house qualification program verifying optical purity (> 99.5% enantiomeric excess via chiral HPLC) and identity via high-field NMR before releasing it to synthesis lines. This prevents the formation of diastereomeric peptide impurities (e.g., L-Arg or D-Dmt variants) that exhibit identical molecular weight and cannot be separated downstream.
Our standard pharmaceutical catalog product is provided as the acetate salt, which is widely recognized as biologically neutral and safe for in vivo injection formulations. For non-clinical R&D or specific crystallization research, TFA (trifluoroacetate) salt lots are available. We also offer custom salt conversions including hydrochloride (HCl) or custom organic salts upon request with full ion chromatography verification.
Standard inventory quantities (10g, 50g, 100g, 500g) are available for immediate dispatch within 48 to 72 hours under cold-chain packaging. Custom kilogram-scale or multi-kilogram commercial campaigns typically require 4 to 6 weeks from purchase order to final QC sign-off and issuance of complete release documentation (CoA, MS, HPLC traces, Karl Fischer water determination, residual solvent GC data).
Yes. Thinheal supports global pharmaceutical clients with Drug Master File (DMF) submissions, Certificates of Suitability (CEP) readiness, open-part access, and comprehensive Letter of Authorization (LoA) documentation. Our regulatory affairs team collaborates directly with sponsor QA teams to resolve regulatory authority deficiency letters rapidly.
Lyophilized SS-31 peptide powder should be maintained at -20°C in a tightly sealed container protected from moisture and light. Under these conditions, the product demonstrates proven chemical stability for at least 24 months. Prior to reconstitution, containers should be allowed to equilibrate to room temperature inside a desiccator cabinet to prevent condensation of atmospheric moisture onto the hygroscopic cake.
Explore therapeutic peptides, metabolic regulators, and advanced cosmetic actives manufactured under verified batch release systems.
Connect directly with our senior peptide synthesis chemists and regional supply desk. Receive an itemized pricelist, batch-specific CoA, chromatograms, and a technical feasibility report for your project within 24 hours.
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