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Pharmaceutical Intermediate Peptides Information

Pharmaceutical Intermediate Peptides Information

Model:1627580-64-6 137525-51-0 175175-23-2
MOTS‑c, BPC‑157, Epitalon, Pinealon, TB‑500, and GHK‑Cu are synthetic peptides investigated for regenerative and metabolic effects. MOTS‑c, a mitochondrial‑derived peptide, modulates glucose metabolism. BPC‑157, a gastric pentadecapeptide, has shown wound‑healing potential in early clinical trials. Epitalon, a tetrapeptide from Russian research, was once granted FDA orphan status for retinitis pigmentosa. Pinealon, a neuroprotective tripeptide, has undergone Phase III trials in Russia. TB‑500, an active fragment of thymosin β4, promotes angiogenesis and is mainly used in veterinary studies. GHK‑Cu, a copper‑bound tripeptide, is clinically proven as a cosmetic anti‑aging agent. All are for research use only; none are approved for human therapy except as cosmetics.



MOTS-C

CAS: 1627580-64-6
Molecular formula: C₁₀₁H₁₅₂N₂₈O₂₂S₂
Molecular weight: 2174.62



MOTS-c (human) is one type of Mitochondrial-Derived Peptides (MDPs). Its primary physiological function is to facilitate the biosynthesis of AICAR, an endogenous AMP analog, thereby activating AMP-activated protein kinase (AMPK). Meanwhile, it can boost cellular glucose uptake and improve insulin sensitivity. As a pharmaceutical raw material, it serves as a potential weight-loss peptide ingredient and also exhibits prominent anti-aging effects.

Original Research Background
MOTS-c was discovered through fundamental scientific research rather than developed by a single enterprise.

Current R&D Status:Hudson Biotech is the leading institution advancing its clinical development.

Clinical Trials
A Phase 2a clinical trial is currently underway, yet no large-scale, peer-reviewed published results are available. 

MOTS-c remains in the research stage and has not obtained marketing approval from major regulatory authorities such as the U.S. FDA for clinical therapeutic use.

Synthesis Method
MOTS-c is manufactured via standard Solid-Phase Peptide Synthesis (SPPS).




BPC-157

CAS: 137525-51-0
Molecular formula: C₆₂H₉₈N₁₆O₂₂
Molecular weight: 1419.54



BPC 157 (pentadecapeptide) is an intestinal peptide with free radical scavenging activity in clinical settings. Unlike other peptides, BPC 157 exerts biological effects without a delivery carrier. As a stable gastric peptide, it displays anti-ulcer activity and accelerates wound and fistula healing.

Original Research Background
Original research on BPC-157 was conducted by a scientific research team from Croatia.
Core Research Institutions
Nearly all existing research data for BPC-157 originates from the same Croatian research team.

  • Early clinical trials were partially carried out by Croatian pharmaceutical firm PLIVA in the 2000s.
  • Slovenian pharmaceutical company Lek Pharmaceuticals d.d. participated in synthetic research on its analogs.


Clinical Trials

Limited low-quality clinical trials have been conducted, which fail to meet the recognition standards of mainstream medical communities. No completed large-scale human clinical trial data is available to date.


Synthesis Method

Solid-Phase Peptide Synthesis (SPPS) with either Fmoc or Boc protecting group strategies is applicable.




Pinealon

CAS: 175175-23-2
Molecular formula: C₁₅H₂₆N₆O₈

Molecular weight: 418.4


Pinealon is a tripeptide short-chain peptide. Research literature identifies it as an antioxidant polypeptide. Due to its low molecular weight, this small-molecule peptide can directly interact with cellular genomes.


Original Research Background

Pinealon was developed by a Russian research team led by Professor Vladimir Khavinson. It is an outcome of Russia’s "Peptide-Gene Regulation" research program, developed by the St. Petersburg Institute of Bioregulation and Gerontology. Pinealon is one of a series of short-peptide biological regulators developed by Professor Khavinson’s group.


Clinical Trials

Small-scale clinical trials have been performed, lacking high-quality independent validation data.
Regulatory Status
Pinealon has not obtained U.S. FDA approval for any medical indications and is only marketed as a research chemical.


Synthesis Method

Standard Solid-Phase Peptide Synthesis (SPPS).




Epitalon

CAS: 307297-39-8
Molecular formula: C₁₄H₂₂N₄O₉

Molecular weight: 390.35


Epitalon is an artificially synthesized polypeptide known as "vitamin for epithelial tissue". Initially isolated from bovine pineal gland extracts, it is a well-documented anti-aging agent and widely incorporated into cosmetic formulations.


Original Research Background

Epitalon was developed by the Russian research team of Professor Vladimir Khavinson at the St. Petersburg Institute of Bioregulation and Gerontology. Its molecular design was derived from amino acid composition analysis of Epithalamin, an extract from bovine pineal glands.


Clinical Trials

Clinical research has been initiated, though supporting evidence remains limited:
  1. Phase 2 clinical trials in Russia for diabetic macular edema;
  2. Small-scale clinical studies evaluating telomere length and sleep quality in elderly populations.


Synthesis Methods

  1. Primary route: Solid-Phase Peptide Synthesis (SPPS);
  2. Alternative route: Liquid-Phase Peptide Synthesis (LPPS);
  3. Emerging green synthesis: Enzymatic synthesis under research exploration.




TB-500

CAS: 885340-08-9
Molecular formula: C₃₈H₆₈N₁₀O₁₄

Molecular weight: 889.02


TB-500 acts as a globular actin (G-actin) binding peptide that binds monomeric G-actin to inhibit actin polymerization. It exerts diverse biological activities including promoting angiogenesis, wound healing, corneal repair, anti-inflammation, and regulating tumor metastasis.


Original Research Background

TB-500 is an artificially synthesized short peptide corresponding to amino acid residues 17–23 of Tβ4. It was designed to retain core biological activity while delivering a smaller, more stable molecular structure for research applications. It is a product of fundamental scientific research with no single proprietary pharmaceutical developer, supplied as a research chemical by biotech companies worldwide.


Clinical Trials

No human clinical trials of TB-500 have been registered or approved by mainstream pharmaceutical regulatory authorities including the U.S. FDA.


Synthesis Method

Standard Solid-Phase Peptide Synthesis (SPPS).




GHK-Cu

CAS: 89030-95-5
Molecular formula: C₁₄H₂₁CuN₆O₄

Molecular weight: 400.91


GHK-Cu is a complex formed by copper ions and the tripeptide GHK. The copper(II) ion endows this copper peptide with a distinctive blue hue. It is the first polypeptide discovered with cosmetic efficacy. Its low molecular weight enables facile skin penetration and absorption.


Original Research Background

GHK-Cu was discovered by American scientist Dr. Loren Pickart. Subsequent studies uncovered its tissue repair activity. ProCyte Corporation was founded in 1986 to develop GHK-Cu applications in tissue repair, anti-aging, and hair growth.


Clinical Trials

Phase 2 clinical trials have been completed.
Synthetic Process (Two-Step Procedure)
  1. Synthesis of GHK tripeptide: Mature Solid-Phase Peptide Synthesis (SPPS) or liquid-phase synthesis technology;
  2. Copper complexation reaction: Purified GHK tripeptide reacts with copper salts (e.g., copper acetate, copper hydroxide) in aqueous solution. GHK tripeptide exhibits high affinity for Cu²⁺ to spontaneously form stable GHK-Cu complexes. The final product is purified via filtration and lyophilization.




Sermorelin

CAS: 86168-78-7
Molecular formula: C₁₄₉H₂₄₆N₄₄O₄₂S

Molecular weight: 3357.89


Sermorelin is an artificially synthesized 29-amino-acid polypeptide, an N-terminal fragment of endogenous Growth Hormone-Releasing Hormone (GHRH) with prominent growth-regulating effects. Neuropeptides, neurotransmitters, hormones and cytokines serve as the "common signaling mediators" for crosstalk between the nervous, endocrine and immune systems. Beyond intrinsic fine regulatory mechanisms, immune function is modulated by the neuro-endocrine-immune network.


Original Research Background

Sermorelin was originally developed by Swedish pharmaceutical enterprises. Kabi Pharmacia first launched the product commercially in 1988, with subsequent intellectual property transferred to U.S.-based EMD Serono, Inc., marketed under the brand name Geref®.


Clinical Trials

Sermorelin completed required clinical trials and previously obtained U.S. FDA marketing approval, though it has since been withdrawn from the market.


Synthesis Method

Solid-Phase Peptide Synthesis (SPPS) for the 29-amino-acid peptide, with two mainstream protecting group strategies:
  1. Boc strategy: Uses tert-butyloxycarbonyl (Boc) as amino acid N-terminal protecting group; drawback: corrosive hydrogen fluoride (HF) required for final resin cleavage, posing operational hazards;
  2. Fmoc strategy: The dominant modern approach, utilizing 9-fluorenylmethoxycarbonyl (Fmoc) for N-terminal amino protection.




Melanotan-II (MT-II)

CAS: 121062-08-6
Molecular formula: C₅₀H₆₉N₁₅O₉

Molecular weight: 1024.18


Melanotan-II (MT-II) is an artificially synthesized cyclic heptapeptide, an analog of α-melanocyte-stimulating hormone (α-MSH).


Original Research Background

MT-II was developed by the research team at the University of Arizona, USA.


Clinical Trials

Early-phase clinical trials were conducted, yet pivotal Phase 3 trials were never completed. No global regulatory authority has approved MT-II for human therapeutic use.


Synthesis Methods

  1. Solid-Phase Peptide Synthesis (SPPS): The preferred efficient manufacturing route. Linear peptide chains are assembled via sequential amino acid coupling on solid resin, followed by on-resin side-chain cyclization to form lactam bridges, optimizable with automated peptide synthesizers;
  2. Liquid-Phase Synthesis: Suitable for large-scale production.
  • Convergent fragment condensation approach: Overall yield ~2.6%;
  • Ajiphase® technology: Claims 72% total yield for gram-scale production.




Semax

CAS: 80714-61-0
Molecular formula: C₃₇H₅₁N₉O₁₀S

Molecular weight: 813.92


Semax, a cognitive peptide consisting of seven amino acids, is an ACTH analog. Its physiological functions include upregulating neurotrophin transcription, exerting neuroprotective effects and enhancing cognitive performance.


Original Research Background

Semax was developed by a Russian research team.


Clinical Trials

Semax is approved as a clinical pharmaceutical in Russia, though high-quality standardized clinical trial evidence remains limited.


Synthesis Method

Standard laboratory Solid-Phase Peptide Synthesis (SPPS).




Ipamorelin

CAS: 170851-70-4
Molecular formula: C₃₈H₄₉N₉O₅
Molecular weight: 711.85


Ipamorelin is a pharmaceutical raw material classified as a peptide hormone and synthetic Growth Hormone-Releasing Hormone analog. It can stimulate gastrointestinal motility, induce growth hormone secretion, enhance lipolysis and physical strength, and causes water retention without hepatotoxicity.


Original Research Background

Ipamorelin was originally developed by Danish pharmaceutical giant Novo Nordisk.


Clinical Trials

Ipamorelin advanced to Phase 2 clinical trials, yet development was terminated due to insufficient therapeutic efficacy.


Synthesis Method

Standard laboratory Solid-Phase Peptide Synthesis (SPPS).




Selank

CAS: 129954-34-3
Molecular formula: C₃₃H₅₇N₁₁O₉

Molecular weight: 751.87


Selank, a heptapeptide with the sequence THR-LYS-PRO-ARG-PRO-GLY-PRO, is a synthetic analog of the human tetrapeptide tuftsin. Clinical studies demonstrate sustained nootropic and anxiolytic activity, with potential applications for generalized anxiety disorder (GAD).


Original Research Background

Selank was developed by Russian research institutions: primary developer is the Institute of Molecular Genetics of the Russian Academy of Sciences, with collaborative research from the V.V. Zakusov Research Institute of Pharmacology.


Clinical Trials

Selank completed clinical trials and obtained clinical approval in Russia, lacking high-quality independent international validation data.


Synthesis Method

Standard laboratory Solid-Phase Peptide Synthesis (SPPS).




Thymosin Alpha-1

CAS: 62304-98-7
Molecular formula: C₁₂₉H₂₁₅N₃₃O₅₅

Molecular weight: 3108.28


Thymosin Alpha-1 is a therapeutic peptide indicated for chronic hepatitis B and boosting immune responsiveness. This highly conserved polypeptide is primarily localized in thymic epithelial cells, with additional expression in lymphoid tissues (spleen, lymph nodes) and non-lymphoid organs (lung, kidney, brain). Its secretion and release are not regulated by exogenous hormones or releasing factors.


Original Research Background

Thymosin Alpha-1 was first isolated from bovine thymic extract Thymic Fraction V. Global commercial development and promotion were led by U.S.-based SciClone Pharmaceuticals, which acquired global patent and commercial rights (excluding the U.S. and Europe) in the early 1990s. Multiple domestic manufacturers conduct R&D and production of this peptide in China.


Clinical Trials

Thymosin Alpha-1 is among the most extensively researched peptide therapeutics with abundant clinical trial datasets.


Synthesis Method

Two Primary Production Routes
  1. Chemical Synthesis (Mainstream): Solid-Phase Peptide Synthesis (SPPS) with Fmoc protection and DIC coupling reagents, delivering purity exceeding 98%. Optimized technologies including fragment condensation and PEG resin anchoring are developed to mitigate synthetic complexity;
  2. Biosynthesis (Recombinant Expression): Genetic engineering technology inserts the thymosin alpha-1 gene into host strains (e.g., Escherichia coli) for protein expression. Suitable for mass production, yet rigorous purification is required to remove host cell proteins and endotoxin impurities.




GHRP-6

CAS: 87616-84-0
Molecular formula: C₄₆H₅₆N₁₂O₆

Molecular weight: 873.02


GHRP-6 (Growth Hormone Releasing Peptide-6) is an artificially synthesized hexapeptide belonging to the Growth Hormone Secretagogue (GHS) family.


Original Research Background

GHRP-6 is a product of fundamental scientific research rather than proprietary development by a single enterprise. The GHRP peptide class was first synthesized in 1977, and GHRP-6 is the first member identified with potent in vivo biological activity.


Clinical Trials

Human clinical trials have been initiated, primarily investigating its neuroprotective efficacy for acute ischemic stroke.


Synthesis Method

Standard laboratory Solid-Phase Peptide Synthesis (SPPS).

Export Instructions

This full English translation covers all peptide data including CAS number, molecular formula, molecular weight, biological functions, original research background, clinical trial status and synthetic techniques, formatted for direct copy export to Word/Excel/TXT documents.



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