ARA-290 (cibinetide)
A synthetic 11-amino-acid erythropoietin helix-B-derived peptide studied as a selective ligand of the innate repair receptor (EPOR/CD131 heterocomplex).
Molecular Profile
- Type
- Synthetic linear 11-amino-acid non-erythropoietic helix-B surface peptide
- Molecular formula
- C51H84N16O21
- Molecular weight
- ~1,257.3 g/mol
- CAS number
- 1208243-50-8
- Amino acids
- 11
- Sequence
- pGlu-Glu-Gln-Leu-Glu-Arg-Ala-Leu-Asn-Ser-Ser
- Modification
- N-terminal pyroglutamate (pGlu)
Mechanism & Target Class
ARA-290 is a synthetic peptide derived from the three-dimensional helix-B surface region of erythropoietin (EPO). EPO biology involves two functionally distinct receptor configurations: a homodimeric EPOR/EPOR complex mediating erythropoiesis in erythroid progenitor cells, and a heteromeric EPOR/CD131 (beta-common receptor, βcR) complex — termed the innate repair receptor (IRR) or tissue-protective receptor — that shares the CD131 signaling subunit with the GM-CSF, IL-3, and IL-5 receptors. The foundational EPOR/CD131 heterocomplex characterization was reported by Brines et al. (2004); short tissue-protective helix-B peptide sequences, including the 11-amino-acid precursor of ARA-290, were delimited by Brines et al. (2008). In preclinical cellular systems, IRR engagement is associated with downstream JAK2/STAT3, PI3K/Akt, and ERK pathway activation and with anti-apoptotic transcriptional responses. Mechanistic literature describes IRR expression as locally upregulated in injured, hypoxic, or inflamed tissue rather than constitutively expressed at high levels. ARA-290 has also been reported to interact with TRPV1 channel activity in nociception model systems (Zhang et al., 2016), proposing a direct nociceptor mechanism alongside IRR-mediated anti-inflammatory signaling.
Storage & Handling
- Lyophilized
- Lyophilized powder: −20°C or below; −80°C recommended for long-term archival.
- Handling
- Water-soluble. Avoid repeated freeze-thaw cycles. For research use only.
Primary Database
References (27)
Reviews
1Collino M, Thiemermann C, Cerami A, Brines M. (2015). Pharmacology & Therapeutics
- 2
van Velzen M, Heij L, Niesters M, Cerami A, Dunne A, Dahan A, Brines M. (2014). Expert Opinion on Investigational Drugs
- 3
Brines M, Cerami A. (2012). Molecular Medicine
Clinical
4Lois N, Gardner E, McFarland M, Armstrong D, McNally C, Lavery NJ, Campbell C, Kirk RI, Bajorunas D, Dunne A, Cerami A, Brines M. (2020). Journal of Clinical Medicine
- 5
Culver DA, Dahan A, Bajorunas D, Jeziorska M, van Velzen M, Aarts LPHJ, Tavee J, Tannemaat MR, Dunne AN, Kirk RI, Petropoulos IN, Cerami A, Malik RA, Brines M. (2017). Investigative Ophthalmology & Visual Science
- 6
Brines M, Dunne AN, van Velzen M, Proto PL, Ostenson CG, Kirk RI, Petropoulos IN, Javed S, Malik RA, Cerami A, Dahan A. (2015). Molecular Medicine
- 7
Dahan A, Dunne A, Swartjes M, Proto PL, Heij L, Vogels O, van Velzen M, Sarton E, Niesters M, Tannemaat MR, Cerami A, Brines M. (2013). Molecular Medicine
- 8
Heij L, Niesters M, Swartjes M, Hoitsma E, Drent M, Dunne A, Grutters JC, Vogels O, Brines M, Cerami A, Dahan A. (2012). Molecular Medicine
- 9
ClinicalTrials.gov. ClinicalTrials.gov
- 10
ClinicalTrials.gov. ClinicalTrials.gov
Primary research
11Winicki NM, et al. (2023). Frontiers in Cardiovascular Medicine
- 12
Xu G, Zou T, Deng L, Yang G, Guo T, Wang Y, Niu C, Cheng Q, Yang X, Dong J, Zhang J. (2022). Frontiers in Pharmacology
- 13
Yao M, Domogatskaya A, Ågren N, Watanabe M, Tokodai K, Brines M, Cerami A, Ericzon BG, Kumagai-Braesch M, Lundgren T. (2021). Cell Transplantation
- 14
Nairz M, Haschka D, Dichtl S, et al. (2017). Scientific Reports
- 15
Muller C, Yassin K, Li LS, Palmblad M, Efendic S, Berggren PO, Cerami A, Brines M, Östenson CG. (2016). Molecular Medicine
- 16
Zhang W, Yu G, Zhang M. (2016). Peptides
- 17
Swartjes M, van Velzen M, Niesters M, Aarts L, Brines M, Dunne A, Cerami A, Dahan A. (2014). Molecular Pain
- 18
Collino M, Benetti E, Rogazzo M, Chiazza F, Mastrocola R, Nigro D, Cutrin JC, Aragno M, Fantozzi R, Minetto MA, Thiemermann C. (2014). British Journal of Pharmacology
- 19
Ahmet I, Tae HJ, Brines M, Cerami A, Lakatta EG, Talan MI. (2013). Journal of Pharmacology and Experimental Therapeutics
- 20
van Rijt WG, Nieuwenhuijs-Moeke GJ, van Goor H, Jespersen B, Ottens PJ, Ploeg RJ, Leuvenink HGD. (2013). Journal of Translational Medicine
- 21
van Rijt WG, et al. (2013). Journal of Translational Medicine
- 22
Bohr S, Patel SJ, Shen K, Vitalo AG, Brines M, Cerami A, Berthiaume F, Yarmush ML. (2013). PNAS
- 23
Patel NSA, Nandra KK, Brines M, Collino M, Wong WF, Kapoor A, et al. (2011). Molecular Medicine
- 24
Swartjes M, Morariu A, Niesters M, Brines M, Cerami A, Aarts L, Dahan A. (2011). Anesthesiology
- 25
Ueba H, Brines M, Yamin M, Umemoto T, Ako J, Momomura S, Cerami A, Kawakami M. (2010). PNAS
- 26
Brines M, Patel NSA, Villa P, Brines C, Mennini T, De Paola M, et al. (2008). PNAS
- 27
Brines M, Grasso G, Fiordaliso F, Sfacteria A, Ghezzi P, Fratelli M, Latini R, Xie QW, Smart J, Su-Rick CJ, Pobre E, Diaz D, Gomez D, Hand C, Coleman T, Cerami A. (2004). PNAS
