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1129435-60-4

1129435-60-4 structure
1129435-60-4 structure
  • Name: Gevokizumab
  • Chemical Name: IMMunoglobulin G2
  • CAS Number: 1129435-60-4
  • Molecular Formula:
  • Molecular Weight:
  • Catalog: Signaling Pathways Immunology/Inflammation Interleukin Related
  • Create Date: 2018-06-04 06:50:37
  • Modify Date: 2024-01-09 14:18:04
  • Gevokizumab is a potent anti-IL-1β antibody, negatively modulates IL-1β signaling through an allosteric mechanism. Gevokizumab selectively decreases the binding affinity of IL-1β for the IL-1 receptor type I (IL-1RI) signaling receptor instead of IL-1 counter-regulatory decoy receptor (IL-1 receptor type II)[1][2].

Name IMMunoglobulin G2
Description Gevokizumab is a potent anti-IL-1β antibody, negatively modulates IL-1β signaling through an allosteric mechanism. Gevokizumab selectively decreases the binding affinity of IL-1β for the IL-1 receptor type I (IL-1RI) signaling receptor instead of IL-1 counter-regulatory decoy receptor (IL-1 receptor type II)[1][2].
Related Catalog
In Vitro Gevokizumab (5 nM; 16 h) shows inhibitory effects of IL-1β-mediated NF-kB activation caused by the soluble receptors, sIL-1RI and sIL-1RII in HeLa cells[1]. Gevokizumab (1.85, 5.55, 16.66, and 50 nM) is a selective negative allosteric modulator which reduces the binding affinity of sIL-1RI to IL-1β[1].
In Vivo Gevokizumab (1 mg/kg; i.v.; once daily for 3 d) improves endothelial regrowth and reduces neointima formation in rats following carotid denudation[2]. Animal Model: Rat carotid denudation model in Sprague-Dawley rats (3-month0-old, 330-360 g)[2] Dosage: 1, 10 and 50 mg/kg Administration: Intravenous injection; once daily for 3 days Result: Decreased carotid intima-media thickness (IMT) in the proximal part of the denuded artery at day 28, and improved endothelial regrowth at 1 mg/kg. 
References

[1]. Issafras H, et al. Detailed mechanistic analysis of gevokizumab, an allosteric anti-IL-1β antibody with differential receptor-modulating properties. J Pharmacol Exp Ther. 2014 Jan;348(1):202-15. 

[2]. Roubille F, et al. The interleukin-1β modulator gevokizumab reduces neointimal proliferation and improves reendothelialization in a rat carotid denudation model. Atherosclerosis. 2014 Oct;236(2):277-85.

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