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Cibinetide
Cat. No. CY-070
Structure:
Glp-Glu-Gln-Leu-Glu-Arg-Ala-Leu-Asn-Ser-Ser-OH (Glp is pyroglutamic acid)
Other Names:
ARA 290, Pyroglutamate Helix B Surface Peptide, pHBSP
Activity:
Erythropoietin/CD131 heteroreceptor agonist
Cibinetide is a linear nonhematopoietic peptide that mimics the three-dimensional structure of the helix B surface domain of erythropoietin (EPO). Cibinetide binds selectively to the non-hematopoietic EPO receptor (the innate repair receptor, IRR), which is a heterodimer of the EPO receptor and the cytokine family beta common receptor (βCR, CD131). The IRR becomes locally upregulated following tissue injury and its activation initiates a local anti-inflammatory response, inhibition of death signal and anti-apoptosis, preventing overt tissue damage. Cibinetide produces effective and long-term pain relief following peripheral nerve damage, an effect mediated by its anti-inflammatory and immunomodulatory functions, and the IRR is thought to be a point of integration between the immune system and pain signalling via nociception. Cibinetide possesses analgesic and tissue protective effects in many diseases such as diabetes and cancer.
Brines et al (2008) Nonerythropoietic, tissue-protective peptides derived from the tertiary structure of erythropoietin. Proc Natl Acad Sci U S A 105(31) 10925 PMID: 18676614
Swartjes et al (2014) ARA 290, a peptide derived from the tertiary structure of erythropoietin, produces long-term relief of neuropathic pain coupled with suppression of the spinal microglia response. Mol Pain 10 13 PMID: 24529189
Zhang and Zhang (2016) ARA 290 relieves pathophysiological pain by targeting TRPV1 channel: Integration between immune system and nociception. Peptides 76 73 PMID: 26774587
Ghassemi-Barghi et al (2023) Mechanistic Approach for Protective Effect of ARA290, a Specific Ligand for the Erythropoietin/CD131 Heteroreceptor, against Cisplatin-Induced Nephrotoxicity, the Involvement of Apoptosis and Inflammation Pathways. Inflammation 46(1)342 PMID: 36085231
Guide to Pharmacology - Cibinetide
Related areas
All peptides >
All cytokine receptor modulators >
All immunology research categories >
All pain research categories >
Technical Data
| Structure | Glp-Glu-Gln-Leu-Glu-Arg-Ala-Leu-Asn-Ser-Ser-OH (Glp is pyroglutamic acid) |
| CAS Number | 1208243-50-8 |
| Molecular Weight | 1257.31 |
| Formula | C51H84N16O21 |
| Sequence | XEQLERALNSS |
| Modifications | X is pyroglutamic acid |
Solubility and Storage
| Solubility | > 50 mg per ml in water |
| Appearance | Freeze dried solid |
| Storage | Store dry, frozen and in the dark |
Batch Specific Data
| Purity | >95% by hplc |
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