Pinealon [Peptide]

Description

What is Pinealon?

Pinealon is a synthetic tripeptide composed of the amino acid sequence glutamic acid-aspartate-arginine (Glu-Asp-Arg), and is classified as a short-chain peptide bioregulator. First characterized in research programs focused on pineal gland tissue extracts, the compound belongs to a broader class of cytomedine-derived ultrashort regulatory peptides developed at the Saint Petersburg Institute of Bioregulation and Gerontology.

In research settings, Pinealon has been investigated for its involvement in neuronal signaling, reactive oxygen species (ROS) modulation, and gene expression regulation in in vitro and in vivo preclinical systems. It has been studied primarily as a molecular tool in models relevant to neurodegenerative processes, including Alzheimer’s disease pathogenesis, oxidative stress-induced neuronal injury, and age-related neuronal morphology changes.

Pinealon is not approved by the Food and Drug Administration for human use. It is intended strictly for laboratory and research purposes, is not a dietary supplement, and is not approved for veterinary or clinical use in its research-grade form.

Chemical Properties

Property	Detail
Product Type	Synthetic Tripeptide Bioregulator
Product Name	Pinealon
Application	Scientific / Research Use Only
CAS Number	175175-23-2
Molar Mass	418.41 g/mol
Chemical Formula	C15H26N6O8
Sequence	Glu-Asp-Arg (H-Glu-Asp-Arg-OH)
IUPAC Name	(2S)-2-[[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]-4-[[(1S)-1-carboxymethyl-2-(2-amino-2-oxoethyl)…]succinate chain; systematic name: L-glutamyl-L-aspartyl-L-arginine
Synonyms	EDR peptide; Glu-Asp-Arg
Physical Form	Lyophilized white to off-white powder
Solubility	Soluble in water and physiological saline; solubility also observed in dilute aqueous buffer systems at neutral to slightly alkaline pH
Storage (Lyophilized)	Store at −20°C in a sealed, light-protected container with desiccant; protect from repeated temperature fluctuations
Storage (Reconstituted)	Store at 4°C; use within 48–72 hours of reconstitution; discard any solution that appears turbid, discolored, or shows particulate matter
PubChem CID	10273502
Purity	≥98% (HPLC verified, independent third-party laboratory analysis; COA available per batch)
WADA Status	Pinealon (EDR) does not appear by name on the current WADA Prohibited List. However, as a peptide bioregulator, it may fall under the S2 category (Peptide Hormones, Growth Factors, Related Substances and Mimetics) depending on classification context. Researchers engaged in sport-adjacent studies should verify the current status at GlobalDRO.com before use.

How Does Pinealon Work?

Pinealon is a short-chain peptide bioregulator that has been investigated for its interactions with intracellular signaling systems, gene expression machinery, and the cellular redox environment. Research at the receptor and cellular level suggests at least three mechanistic axes relevant to preclinical neuronal models.

Reactive Oxygen Species Suppression and Antioxidant Enzyme Induction

In isolated cerebellar granule cell preparations, neutrophil cultures, and PC12 pheochromocytoma cell models, dose-dependent restriction of ROS accumulation was observed following Pinealon application under conditions of receptor-dependent and receptor-independent oxidative challenge. In rat cerebellar neuron cell culture systems, the compound has been associated with upregulation of antioxidant enzyme synthesis, including superoxide dismutase 2 (SOD2) and glutathione peroxidase 1 (GPX1). These observations suggest a cellular-level antioxidant capacity that may operate through transcriptional modulation of endogenous defense mechanisms rather than direct radical scavenging alone.

MAPK/ERK Signaling Pathway Modulation

In rodent cerebellar granule cell preparations and PC12 cell systems, Pinealon application was associated with a delayed time course of ERK1/2 phosphorylation activation. At concentrations above those required to reduce ROS accumulation, the compound appeared to interact with cell cycle progression, suggesting a direct genomic interaction distinct from antioxidant activity alone. The MAPK/ERK cascade has been identified in computational and in vitro models as a probable downstream target of EDR-mediated intracellular action, with proposed modulation of proapoptotic proteins including caspase-3 and p53 in neuronal cell systems.

Epigenetic Regulation and Gene Expression

Computational modeling and molecular docking studies have proposed that EDR (Pinealon) enters cells and interacts with histone proteins and/or ribonucleic acids, thereby influencing chromatin-level regulation. In silico analyses suggest the peptide may bind to specific oligonucleotide sequences in the DNA minor groove, with the proposed consequence of altering transcription factor activity including PPARA and PPARG. These proposed epigenetic mechanisms remain at a hypothesis stage supported by molecular modeling and limited in vitro data; independent replication is required.

Dendritic Spine Morphology and Neuroplasticity Markers

In fibroblast-derived induced cortical neuron preparations from aged human donors, EDR application was associated with arborization of the dendritic tree, including increases in both primary process number and total dendrite length. EDR was also observed to reduce oxidative DNA damage markers in induced neurons derived from elderly donor fibroblasts under the same model system. In Alzheimer’s disease model preparations using cultured neurons from transgenic mice, EDR application was associated with reduced elimination of dendritic spines, though the mechanistic basis for this observation is not fully characterized.

Key Research Findings

• ROS suppression in neuronal cells: Dose-dependent restriction of reactive oxygen species accumulation observed in cerebellar granule cell, neutrophil, and PC12 cell preparations under oxidative stress conditions; associated with reduced necrotic cell death by propidium iodide assay. [Khavinson et al., 2011]

• ERK1/2 signaling modulation: Delayed ERK1/2 activation time course characterized in cerebellar granule cell preparations following Pinealon treatment; higher-dose cell cycle modification observed, indicating a probable direct genomic interaction. [Khavinson et al., 2011]

• Dendritic arborization in aged induced neurons: EDR promoted increases in primary process number and total dendrite length in fibroblast-derived induced cortical neurons from elderly human donors; oxidative DNA damage reduction observed in the same model. [Kraskovskaya et al., 2024]

• MAPK/ERK and apoptotic protein regulation (proposed): Computational and review-level analysis proposed EDR modulation of MAPK/ERK pathway activity, caspase-3, p53, SOD2, and GPX1 in neuronal systems relevant to Alzheimer’s disease pathogenesis. [Khavinson et al., 2020]

• Anabolic and neuroprotective markers in aging models: Pinealon administration in a small clinical observation study of patients with organic brain syndrome in remission was associated with anabolic activity markers and improvements in central nervous system functional indicators; prooxidant activity was also noted via chemiluminescence. [Meshchaninov et al., 2015]

All findings listed above are derived from preclinical or in vitro data, or limited observational study designs with small sample sizes. No conclusions regarding human therapeutic efficacy can be drawn from these observations. These findings do not constitute evidence of safety or efficacy in any human condition or organism.

What are the Potential Research Applications of Pinealon?

Neuronal Oxidative Stress and ROS Biology

Pinealon has been applied in in vitro systems as a molecular tool for investigating ROS accumulation dynamics in neuronal and immune cell preparations. Its dose-dependent effects on oxidative challenge in cerebellar granule cells and PC12 models make it a candidate reagent for studies examining antioxidant enzyme induction pathways, cell viability under oxidative conditions, and the relationship between ROS levels and downstream signaling cascades. These are observed in preclinical and in vitro contexts only.

MAPK/ERK Signaling in Neuronal Systems

The compound’s observed effects on ERK1/2 activation kinetics in cerebellar granule cell preparations position it as a research tool for probing MAPK pathway modulation in neuronal contexts. Research groups investigating the role of ERK1/2 phosphorylation timing in cell survival, proliferation, and apoptotic regulation may find EDR useful as a mechanistic reference compound in these pathway studies. These applications are limited to laboratory and preclinical model systems.

Alzheimer’s Disease Preclinical Models

Pinealon has been applied in Alzheimer’s disease model systems, including cell cultures derived from transgenic mice overexpressing AD-associated mutations, to investigate dendritic spine dynamics and neuroplasticity markers. It has also been studied in fibroblast-derived induced neuron models to characterize age-related neuronal morphology changes and the effects of short peptides on dendritic tree structure. These observations are derived from preclinical and in vitro contexts only and do not constitute claims of efficacy or safety in any organism.

Epigenetic and Gene Expression Studies

Computational models and in vitro findings support investigation of Pinealon as a probe for epigenetic regulatory mechanisms in neuronal cell systems. Proposed interactions with histone proteins, DNA minor groove binding sites, and downstream transcription factor activity (PPARA, PPARG) are subjects of ongoing research at the molecular modeling level. These hypotheses have not been independently replicated at the genomic level and are derived from preclinical and computational contexts only.

Aging and Biological Age Markers

Pinealon has been included in small-scale observational research on aging biomarkers and cellular indicators associated with biological age in human subjects with polymorbidity, alongside other short synthetic peptide bioregulators. These observations are preliminary, involve small sample sizes, and should not be extrapolated to therapeutic conclusions. These are observed in preclinical and limited observational study contexts only and do not constitute claims of efficacy or safety in any organism.

What are the Potential Side Effects of Pinealon?

• Prooxidant activity was detected via chemiluminescence assay in an observational study involving human subjects with organic brain syndrome administered Pinealon over a defined period; this finding was not uniform and requires further mechanistic investigation before interpretation.

• Decrease of CD34+ positive hematopoietic stem cell markers in peripheral blood was observed in a small human observational study; significant inhibition of hematopoietic activity was noted, suggesting the compound may affect stem cell compartment dynamics at assessed doses.

• At higher concentrations in PC12 and cerebellar granule cell preparations, cell cycle modification extending beyond antioxidant saturation concentrations was observed, indicating possible direct genomic interactions not yet fully characterized.

• No specific dose-limiting organ toxicity data are available from controlled animal studies for Pinealon; the absence of such data does not imply safety, as comprehensive toxicological profiling in standard preclinical models has not been published in peer-reviewed literature.

No human safety or tolerability data pertaining to research-grade Pinealon has been established. These observations are derived from experimental systems and limited observational designs and should not be extrapolated to human or animal outcomes.

Risk & Handling

Handling Precautions

Pinealon should be handled exclusively by trained laboratory personnel familiar with peptide handling procedures. Minimum personal protective equipment includes nitrile gloves, laboratory coat, and eye protection. Lyophilized powder reconstitution should be performed in a manner that minimizes aerosol generation; use of a biosafety cabinet or laminar flow hood is recommended. Pinealon is a biologically active peptide with demonstrated cellular-level activity; standard laboratory procedures appropriate for pharmacologically active agents apply. No compound-specific extreme hazard precautions (such as those required for cytotoxic chimeric peptides) have been identified in published literature; however, researchers should exercise care consistent with handling a bioactive regulatory peptide.

Exposure Risks

Risk Tier: LOW-MODERATE

Pinealon is a short, naturally occurring amino acid sequence tripeptide. No acute lethality or dose-limiting organ toxicity has been documented in standard animal models in published literature. At research-relevant concentrations, no systemic cardiovascular, renal, or hepatic toxicity has been characterized. Cell-level activity, including ROS modulation and ERK1/2 signaling effects, has been observed in vitro at nanomolar concentrations, indicating biological potency appropriate to a bioregulatory peptide. A small human observational study noted prooxidant activity and hematopoietic marker suppression, indicating that systemic biological effects are possible at assessed doses. Plasma half-life data for Pinealon in standard preclinical rodent models has not been established in published peer-reviewed sources; rapid degradation consistent with unprotected tripeptides in biological fluids is expected. No human safety data has been established for research-grade Pinealon.

Storage

• Lyophilized form: Store at −20°C in a sealed, light-protected container with desiccant
• Reconstituted form: Store at 4°C; use within 48–72 hours of reconstitution
• Limit freeze-thaw cycles; repeated cycling degrades peptide integrity and reduces assay reproducibility
• Do not store in the presence of strong oxidizing or reducing agents
• Discard any reconstituted solution that appears turbid, discolored, or shows particulate matter

FAQs

Q: What is Pinealon and what is it investigated for in research? A: Pinealon (EDR; Glu-Asp-Arg) is a synthetic tripeptide bioregulator investigated in preclinical and in vitro models for neuroprotective mechanisms, reactive oxygen species modulation, MAPK/ERK signaling in neuronal cells, and gene expression regulation relevant to neurodegenerative disease models. It is supplied by RCDbio for laboratory research use only and is not intended for human or veterinary use.

Q: What is the half-life of Pinealon in preclinical models? A: Published pharmacokinetic data specifically characterizing the plasma half-life of Pinealon in rodent or other standard preclinical models is not available in peer-reviewed literature. As an unmodified tripeptide, rapid hydrolysis by plasma peptidases and renal clearance are expected based on the behavior of comparable short peptides in biological systems. In vitro stability under low-temperature aqueous conditions is expected to exceed in vivo stability. These figures are derived from general peptide pharmacokinetic principles and do not represent established pharmacokinetic data for research-grade Pinealon.

Q: How should Pinealon be stored to maintain stability? A: Lyophilized Pinealon should be stored at −20°C in a sealed, light-protected container with desiccant. Once reconstituted, store at 4°C and use within 48–72 hours. Minimize freeze-thaw cycling, as repeated temperature transitions degrade peptide integrity. Discard any reconstituted solution that appears turbid or discolored.

Q: What toxicity observations have been reported in preclinical studies? A: Comprehensive controlled toxicology studies for Pinealon in standard animal models have not been published. A small observational study in human subjects noted prooxidant activity via chemiluminescence and a reduction in CD34+ hematopoietic stem cell markers in peripheral blood. Cell cycle modification at higher concentrations was observed in in vitro neuronal preparations. No acute lethality or organ-specific dose-limiting toxicity has been reported in available literature. No human safety data has been established for research-grade Pinealon.

Q: What is Pinealon typically reconstituted with in laboratory research? A: Based on its aqueous solubility profile, Pinealon is typically reconstituted in sterile water for injection, physiological saline (0.9% NaCl), or dilute phosphate-buffered saline at neutral to slightly alkaline pH. The specific reconstitution vehicle should be selected based on the requirements of the experimental system in which the compound will be applied.

Q: How does Pinealon relate to the broader class of peptide bioregulators? A: Pinealon belongs to a class of ultrashort synthetic peptide bioregulators, several of which (including Epithalon/AEDG and Livagen/KED) have been derived from or inspired by tissue-specific peptide extract research programs. These compounds share a short amino acid sequence structure (two to four residues) and have been investigated as modulators of gene expression and cellular homeostasis in aging and neurodegeneration research contexts. The mechanistic framework proposed for this compound class involves interactions with chromatin regulatory elements rather than classical receptor-ligand pharmacology.

Q: Is Pinealon the same compound as the pharmaceutical preparation sold under that brand name in some regions? A: Research-grade Pinealon supplied by RCDbio shares the same amino acid sequence (Glu-Asp-Arg) as the compound referenced in pharmaceutical bioregulator research literature. It is not a pharmaceutical preparation, has not undergone clinical regulatory review, and is not approved for human use in any formulation supplied by RCDbio. Researchers should note that any pharmaceutical preparations bearing this name in certain jurisdictions represent separately regulated products not associated with research-grade material supplied for laboratory use.

Related Research Compounds

Epithalon (AEDG) Peptide — A tetrapeptide bioregulator (Ala-Glu-Asp-Gly) from the same ultrashort peptide class as Pinealon, investigated in preclinical models for telomerase activation, epigenetic aging markers, and pineal gland-associated regulatory mechanisms.

Livagen Peptide — A tetrapeptide bioregulator (Lys-Glu-Asp-Ala) investigated in preclinical models for chromatin decondensation activity and immunomodulatory effects in aging cell systems; shares structural and mechanistic research context with EDR-class compounds.

Semax Nasal Spray — A synthetic heptapeptide analog of ACTH 4–10 investigated in preclinical models for BDNF-related neurotrophin pathway activity and neuroprotective mechanisms in rodent ischemia and stress models.

References

Khavinson V, Ribakova Y, Kulebiakin K, Vladychenskaya E, Kozina L, Arutjunyan A, Boldyrev A. Pinealon increases cell viability by suppression of free radical levels and activating proliferative processes. Rejuvenation Research. 2011;14(5):535–541. doi:10.1089/rej.2011.1172. PMID: 21978084. https://pubmed.ncbi.nlm.nih.gov/21978084/ 

Khavinson V, Linkova N, Kozhevnikova E, Trofimova S. EDR Peptide: Possible Mechanism of Gene Expression and Protein Synthesis Regulation Involved in the Pathogenesis of Alzheimer’s Disease. Molecules. 2020;26(1):159. doi:10.3390/molecules26010159. PMID: 33396470. https://pubmed.ncbi.nlm.nih.gov/33396470/ 

Kraskovskaya N, Linkova N, Sakhenberg E, Krieger D, Polyakova V, Medvedev D, Krasichkov A, Khotin M, Ryzhak G. Short Peptides Protect Fibroblast-Derived Induced Neurons from Age-Related Changes. International Journal of Molecular Sciences. 2024;25(21):11363. doi:10.3390/ijms252111363. PMID: 39518916. https://pubmed.ncbi.nlm.nih.gov/39518916/ 

Meshchaninov VN, Tkachenko EL, Zharkov SV, Gavrilov IV, Katyreva IuE. Effect of Synthetic Peptides on Aging of Patients with Chronic Polymorbidity and Organic Brain Syndrome of the Central Nervous System in Remission. Advances in Gerontology. 2015;28(1):62–67. PMID: 26390612. https://pubmed.ncbi.nlm.nih.gov/26390612/ 

Disclaimer

Pinealon is exclusively for laboratory research purposes. RCDbio products are not intended to diagnose, prevent, treat, or cure any disease or medical condition.

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