Ara-290 (Cibinetide) 99% Purity Peptides Improve Neuropathic Pain Improve Metabolism 1208243-50-8

1.  Description

     Chemical Properties: ARA-290 is an EPO-derived peptide compound with the molecular sequence Pyr-Glu-Gln-Leu-Glu-Arg-Ala-Leu-Asn-Ser-Ser (pyrolidone carboxylic acid - glutamic acid - glutamine - leucine - glutamic acid - arginine - alanine - leucine - asparagine - serine - serine). Its core active site is the EPOR₂-βcR₂ receptor binding domain. Chemically stable, resistant to peptidase hydrolysis, stable in neutral to weakly acidic environments, compatible with most biological reagents, and free of erythropoiesis-stimulating side effects.

     Physical Properties: ARA-290 is a white crystalline powder at room temperature, odorless and tasteless, slightly soluble in water, and readily soluble in organic solvents such as dimethyl sulfoxide (DMSO) and methanol. Molecular weight: 1257.33 g/mol. Melting point and boiling point are not publicly reported. Store at 2-8°C in a dry, sealed container protected from light. Avoid contact with strong oxidizing agents and heavy metal ions. Research-grade product purity is typically ≥98% (HPLC detection), with single impurity ≤2.0% and acetate content 5.0%-12.0%.

     Source and Preparation: ARA-290 has no natural occurrence and is synthesized via solid-phase synthesis. Starting from high-purity L-amino acids, the target peptide chain is constructed through multiple reactions including condensation, deprotection, and purification. The final high-purity product is obtained by high-performance liquid chromatography (HPLC) purification. The synthesis process requires precise control of reaction conditions to ensure structural integrity and receptor binding activity of the peptide chain.

2.  Application

      Biomedical Research Field: ARA-290 serves as a core tool reagent for cell protection and inflammation regulation studies, investigating mechanisms in disease models such as neuropathic pain, renal ischemia-reperfusion injury, and organ transplant injury. Through cellular models (e.g., neuronal cells, renal tubular epithelial cells) and animal models, it analyzes its regulatory effects on inflammatory cytokine expression, tissue repair pathways, and pain signaling transmission, providing experimental evidence for developing intervention strategies for related diseases.

     Preclinical Drug Development: Leveraging its potent organ protection and anti-inflammatory activity, ARA-290 serves as a candidate drug in preclinical development for kidney transplantation and ischemic organ injury. In renal ischemia-reperfusion injury models, early administration (1 hour post-reperfusion) significantly improves renal function and reduces inflammatory responses, offering novel directions for clinical interventions against ischemic injury post-transplantation. It is currently undergoing animal-level efficacy validation.

     Potential Health and Rehabilitation Applications: Leveraging its tissue repair and anti-inflammatory properties, ARA-290 holds promise for sports injury recovery and chronic inflammation-related health management. For instance, sports medicine research explores its potential to accelerate muscle injury and tendinitis repair. In geriatric health, studies investigate its regulatory potential for age-related chronic inflammation. However, these applications remain in the theoretical exploration phase and require further clinical validation.

3. Main Efficacy

      Targeted Anti-inflammatory and Immunomodulatory Effects: The core mechanism of ARA-290 involves specific binding to the EPOR₂-βcR₂ receptor complex (innate repair receptor, IRR), activating downstream anti-inflammatory pathways and inhibiting the expression and release of pro-inflammatory factors (such as TNF-α and IL-6). In renal ischemia-reperfusion injury models, early administration significantly reduces renal inflammation levels and decreases neutrophil infiltration, thereby mitigating acute tissue damage.

     Tissue Protection and Repair Effects: By activating the IRR receptor, ARA-290 modulates cell survival signaling pathways (e.g., PI3K/Akt pathway), inhibits damaged cell apoptosis, and promotes cell proliferation and repair. In kidney transplantation studies, ARA290 improves post-ischemic reperfusion renal function indicators (e.g., serum creatinine, blood urea nitrogen levels), reduces tubular necrosis areas, accelerates tissue repair, with more pronounced effects observed with early administration.

    Neuroprotection and Pain Relief Efficacy: In neuropathic pain models, ARA-290 modulates neurogenic inflammatory responses by upregulating IRR receptor expression in the spinal cord, thereby reducing pain signal transmission. It inhibits the activity of pain-related ion channels and decreases excitability of dorsal horn neurons in the spinal cord, alleviating chronic neuropathic pain without the addictive side effects associated with opioid medications.

    Advantage of No Hematopoietic Side Effects: Unlike traditional EPO, ARA-290 does not activate erythropoiesis-related receptor pathways. This avoids potential risks such as polycythemia and thrombosis, offering higher safety. It is suitable for cell protection and anti-inflammatory scenarios where erythropoiesis stimulation is not required.