Date published: 2026-2-2

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IL-1R Antagonist (CAS 566914-00-9)

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Alternate Names:
BB-loop Mimic; Hydrocinnamoyl-L-valyl Pyrrolidine
Application:
IL-1R Antagonist is a specific inhibitor of TIR domain-mediated MyD88/IL1-RI interaction
CAS Number:
566914-00-9
Purity:
≥95%
Molecular Weight:
302.41
Molecular Formula:
C18H26N2O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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IL-1R Antagonist is a cell-permeable, end protected L-valyl derivative modeled on the MyD88-binding sequence of the TIR domain BB-loop of IL-1RI. It specifically inhibits TIR domain-mediated MyD88/IL1-RI interaction without affecting TLR4/MyD88 interaction. Has shown to activate the MAP kinase signaling cascades in murine lymphocytes and EL4 thymoma cells in vitro. IL-1R Antagonist, also known as Interleukin-1 receptor antagonist or IL-1Ra, is a naturally occurring protein that regulates inflammation and immune responses in the body. It belongs to the interleukin-1 family of cytokines, which are immune and inflammatory mediators. IL-1R Antagonist is produced by various cells, including macrophages, monocytes, and lymphocytes, and it plays a role in controlling inflammatory and immune processes.


IL-1R Antagonist (CAS 566914-00-9) References

  1. A low molecular weight mimic of the Toll/IL-1 receptor/resistance domain inhibits IL-1 receptor-mediated responses.  |  Bartfai, T., et al. 2003. Proc Natl Acad Sci U S A. 100: 7971-6. PMID: 12799462
  2. MyD88-dependent and -independent signaling by IL-1 in neurons probed by bifunctional Toll/IL-1 receptor domain/BB-loop mimetics.  |  Davis, CN., et al. 2006. Proc Natl Acad Sci U S A. 103: 2953-8. PMID: 16477040
  3. IL-1beta induces a MyD88-dependent and ceramide-mediated activation of Src in anterior hypothalamic neurons.  |  Davis, CN., et al. 2006. J Neurochem. 98: 1379-89. PMID: 16771830
  4. Design, synthesis, and in vitro activity of peptidomimetic inhibitors of myeloid differentiation factor 88.  |  Fantò, N., et al. 2008. J Med Chem. 51: 1189-202. PMID: 18275134
  5. The TIR/BB-loop mimetic AS-1 protects the myocardium from ischaemia/reperfusion injury.  |  Cao, Z., et al. 2009. Cardiovasc Res. 84: 442-51. PMID: 19586942
  6. The TIR/BB-loop mimetic AS-1 prevents cardiac hypertrophy by inhibiting IL-1R-mediated MyD88-dependent signaling.  |  Zhu, Y., et al. 2011. Basic Res Cardiol. 106: 787-99. PMID: 21533832
  7. A small molecule that mimics the BB-loop in the Toll interleukin-1 (IL-1) receptor domain of MyD88 attenuates staphylococcal enterotoxin B-induced pro-inflammatory cytokine production and toxicity in mice.  |  Kissner, TL., et al. 2011. J Biol Chem. 286: 31385-96. PMID: 21693701
  8. [Effect of hydrocinnamoyl-L-valyl pyrrolidine on healing quality of deep partial-thickness scald wound in mice].  |  Yang, ML., et al. 2016. Zhonghua Shao Shang Za Zhi. 32: 658-666. PMID: 27894387
  9. A novel reporter for real-time, quantitative imaging of AKT-directed K63-poly-ubiquitination in living cells.  |  Nyati, S., et al. 2018. Oncotarget. 9: 11083-11099. PMID: 29541398
  10. The TIR/BB-loop mimetic AS-1 prevents Ang II-induced hypertensive cardiac hypertrophy via NF-κB dependent downregulation of miRNA-143.  |  Song, J., et al. 2019. Sci Rep. 9: 6354. PMID: 31015570
  11. Downregulation of the inflammatory network in senescent fibroblasts and aging tissues of the long-lived and cancer-resistant subterranean wild rodent, Spalax.  |  Odeh, A., et al. 2020. Aging Cell. 19: e13045. PMID: 31605433
  12. Role of MyD88 in IL-1β and Ethanol Modulation of GABAergic Transmission in the Central Amygdala.  |  Bajo, M., et al. 2019. Brain Sci. 9: PMID: 31817854
  13. Toxoplasma gondii Rhoptry Protein 7 (ROP7) Interacts with NLRP3 and Promotes Inflammasome Hyperactivation in THP-1-Derived Macrophages.  |  Zhu, L., et al. 2022. Cells. 11: PMID: 35626667

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

IL-1R Antagonist, 10 mg

sc-221747
10 mg
$167.00

IL-1R Antagonist, 25 mg

sc-221747A
25 mg
$312.00