Cibinetide acetate
Based on 6 publication(s) in Google Scholar
Cibinetide acetate (ARA290 acetate) is a non-hematopoietic Erythropoietin analog. Cibinetide acetate selectively activates the EPOR/CD131 heteromer IRR without activating EPOR homodimers, and exerts neuroprotective effects through β-common receptor signaling. Cibinetide acetate inhibits Cathepsin K/OSCAR/OC-STAMP/DC-STAMP/NFATC1, increases OPG and Alkaline phosphatase, and decreases CD115. Cibinetide acetate modulates SIRT1/NF-κB/IL-1β signaling, reduces inflammatory infiltration and periapical bone loss, protects pancreatic islets, reduces IBMIR-related platelet consumption, and prolongs graft function. Cibinetide acetate extends healthspan and attenuates age-related cardiac and body weight decline. Cibinetide acetate can be used in research on cerebral ischemic stroke, sarcoidosis-associated small fiber neuropathy, and type 1 diabetes.
For research use only. We do not sell to patients.
- Formula: C51H84N16O21.xC2H4O2
- Molecular Weight:1257.31 (free base)
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Cibinetide acetate
More
Customer Validation & Images
-
IHC
All Cathepsin Isoforms
More
Biological Activity
Description
|
cathepsin K |
SIRT1 |
IL-1β |
In Vitro
Cibinetide (3-300 µM; 48 hours) acetate does not reduce BMDM viability[1].
Cibinetide (150 µM; added on days 0-3; stained on day 4) acetate exhibits the strongest inhibitory effect on osteoclastogenesis when added on day 0 of RANKL-induced BMDM differentiation[1].
Cibinetide (150 µM) acetate inhibits the expression of CTSK, OSCAR, DC-STAMP, OC-STAMP, and NFATC1 in RANKL/M-CSF-stimulated BMDMs[1].
Cibinetide (150 µM; 10 U/mL EPO; LPS on day 2; TRAP staining on day 4) acetate antagonizes LPS- and EPO-enhanced osteoclastogenesis in BMDM cultures[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Cibinetide (300 µg/kg/day; 5 consecutive days; combined with EPO on day 1 and day 4) acetate attenuates EPO-driven expansion of osteoclast progenitor cells and reduces CD115 surface expression on osteoclast precursors in healthy female mice[1].
Cibinetide (30-100 µg/kg; i.p.; once or twice daily; administered at the onset of reperfusion) acetate attenuates cerebral infarction in mice after MCAO at 30 µg/kg twice daily, whereas 30 or 100 µg/kg once daily has no such effect[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:C57BL/6J (C57BL/6J-RccHsd; female; 12 weeks old)[1]
-
Dosage:120 µg/kg
-
Administration:3 times per week; for 4 weeks
-
Result:Hemoglobin levels were unchanged.
Cortical tissue mineral density increased by 5.8%.
Trabecular tissue mineral density increased by 5.2%.
BV/TV was unchanged.
Whole-bone OPG mRNA increased by 52.4%.
RANKL mRNA was unchanged.
The percentages of CD11b−ALP+ preosteoblasts and CD11b−CD115+ preosteoclasts in bone marrow were unchanged.
Surface ALP expression on CD11b− bone marrow cells increased by 25.59%.
Surface CD115 expression decreased by 17.79%.
-
Animal Model:C57BL/6J (C57BL/6J-RccHsd; female; 13 weeks old)[1]
-
Dosage:300 µg/kg/day (alone or with EPO 120 U on days 1 and 4)
-
Administration:daily; for 5 consecutive days; EPO on days 1 and 4
-
Result:EPO alone increased Lin−CD11b−Ly6ChiCD115+ osteoclast progenitors by 81.06%.
Concurrently reduced this population by 42.8% compared with EPO alone.
Osteoblast precursor numbers were unchanged.
Downregulated CD115 surface expression on osteoclast precursors both alone and in combination with EPO; EPO alone had no effect.
Short-term µCT showed no changes in bone parameters in any group.
-
Animal Model:C57BL/6J (male, adult, 22-25 g)[3]
-
Dosage:30 µg/kg (once daily); 30 µg/kg (twice daily); 100 µg/kg (once daily)
-
Administration:i.p.; once daily or twice daily; started at beginning of reperfusion
-
Result:Brain infarction volume was lower in the 30 µg/kg twice-daily group than in the MCAO group.
The 30 µg/kg once-daily and 100 µg/kg once-daily groups did not show this reduction.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
-
Molecular Weight 1257.31 (free base)
-
Formula C51H84N16O21.xC2H4O2
-
SMILES
OC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H]1CCC(N1)=O)=O)CCC(O)=O)=O)CCC(N)=O)=O)CC(C)C)=O)CCC(O)=O)=O)CCCNC(N)=N)=O)C)=O)CC(C)C)=O)CC(N)=O)=O)CO)=O)CO)=O.CC(O)=O.[x]
-
Synonyms
ARA290 acetate
-
Sequence
{Glp}-Glu-Gln-Leu-Glu-Arg-Ala-Leu-Asn-Ser-Ser
-
Sequence Shortening
{Glp}-EQLERALNSS
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (6)
-
Journal Impact Factor
-
Most Recent
-
CNS Neurosci Ther
Erythropoietin-derived peptide ARA290 mediates brain tissue protection through the β-common receptor in mice with cerebral ischemic stroke. [Abstract]2024 Mar;30(3):e14676. PMID: 38488446 -
Int J Mol Sci
2024 Mar 29;25(7):3854. PMID: 38612664 -
Immunology
EPOR activation attenuates colitis via enhancing LC3B-dependent apoptotic cell clearance. [Abstract]2025 Sep;176(1):33-48. PMID: 37204242 -
Toxicol In Vitro
An engineered non-erythropoietic erythropoietin-derived peptide, ARA290, attenuates doxorubicin induced genotoxicity and oxidative stress. [Abstract]2020 Aug:66:104864. PMID: 32335150
Cibinetide acetate purchased from MedChemExpress. Usage Cited in: Toxicol In Vitro. 2020 Aug:66:104864. [Abstract]
Representative photomicrographs demonstrate the results of the TUNEL assay. Alterations in apoptotic cells are assessed using the ratio of green fluorescence. (For interpretation of the references to colour in this figure legend, the reader is referred to the web version of this article.)
-
-
Purity & Documentation
References
[1]. Awida Z, et al. The Non-Erythropoietic EPO Analogue Cibinetide Inhibits Osteoclastogenesis In Vitro and Increases Bone Mineral Density in Mice. International journal of molecular sciences. 2021 Dec 21;23(1):55. [Content Brief]
[3]. Wang RL, et al. Erythropoietin-derived peptide ARA290 mediates brain tissue protection through the β-common receptor in mice with cerebral ischemic stroke. CNS neuroscience & therapeutics. 2024 Mar;30(3):e14676. [Content Brief]
[5]. Gemignani F, et al. Non-length-dependent small fiber neuropathy: Not a matter of stockings and gloves. Muscle & nerve. 2022 Jan;65(1):10-28. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Cibinetide acetate Related Classifications
HY-P0168A Related Classifications
Powered by Bioz
Keywords
- Cibinetide
- ARA290
- ARA 290
- ARA-290
- Erythropoietin Receptor (EpoR)
- Cathepsin
- Nuclear Factor of activated T Cells (NFAT)
- Phosphatase
- Sirtuin
- NF-κB
- Interleukin Related
- c-Fms
- EPOR/CD131
- IBMIR
- SIRT1/NF-κB/IL-1β
- allograft rejection
- erythropoietin analogue
- innate repair receptor
- neuroprotection
- osteoclast differentiation
- β-common receptor
- βCR
- Inhibitor
- inhibitor
- inhibit