Paquinimod (ABR 25757) (Synonyms: ABR-25757) |
| رقم الكتالوجGC31346 |
Paquinimod (ABR 25757) (ABR 25757) هو مثبط محدد لـ S100A8 / S100A9.
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Cas No.: 248282-01-1
Sample solution is provided at 25 µL, 10mM.
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Paquinimod (ABR-215757) binds S100A9 and inhibits its interaction with TLR4/MD2 and RAGE[1-2].
The addition of paquinimod(350 µM paquinimod;30 min preincubated) significantly inhibited the up-regulated levels of IL-6 and IL-8 protein in synovium due to S100A9, but had no inhibitory effect on TNF-α[7].
Mice prophylactically treated with paquinimod(10 mg/kg/day;14days;added into the drinking water) exhibited detectable but mitigated signs of colitis, as determined by a reduced trend in weight loss, reduced colonic shortening and inflammation in the colons compared to DSS-only treated mice. Paquinimod treatment also prevented the upregulation of Lcn2 and S100A8/A9 in the brain in DSS-treated mice[3]. In a meningitis model, MRP14-deficient mice showed a better resolution of inflammation during antibiotic therapy. Treatment with the MRP14 antagonist paquinimod(10 mg/kg) reduced inflammation and disease severity significantly, reaching levels comparable to those achieved after genetic depletion of MRP14[4]. Preventive treatment with the paquinimod (ABR-215757) (25 mg/kg;5days;added into the drinking water) during the first 5 days after induction of experimental autoimmune encephalomyelitis is sufficient to significantly ameliorate disease symptoms[5]. Paquinimod treatment can significantly inhibit progression of insulitis to T1D in the NOD mouse[6].
References:
[1]. BjÖrk P, BjÖrk A,et,al. Identification of human S100A9 as a novel target for treatment of autoimmune disease via binding to quinoline-3-carboxamides. PLoS Biol. 2009 Apr 28;7(4):e97. doi: 10.1371/journal.pbio.1000097. PMID: 19402754; PMCID: PMC2671563.
[2]. Gong H, Su WJ, et,al.Hippocampal Mrp8/14 signaling plays a critical role in the manifestation of depressive-like behaviors in mice. J Neuroinflammation. 2018 Sep 4;15(1):252. doi: 10.1186/s12974-018-1296-0. PMID: 30180864; PMCID: PMC6122683.
[3]. Talley S, Valiauga R, et,al.DSS-induced inflammation in the colon drives a proinflammatory signature in the brain that is ameliorated by prophylactic treatment with the S100A9 inhibitor paquinimod. J Neuroinflammation. 2021 Nov 10;18(1):263. doi: 10.1186/s12974-021-02317-6. PMID: 34758843; PMCID: PMC8578918.
[4]. Wache C, Klein M, et,al.Myeloid-related protein 14 promotes inflammation and injury in meningitis. J Infect Dis. 2015 Jul 15;212(2):247-57. doi: 10.1093/infdis/jiv028. Epub 2015 Jan 20. PMID: 25605866.
[5]. Helmersson S, Sundstedt A, et,al.Amelioration of experimental autoimmune encephalomyelitis by the quinoline-3-carboxamide paquinimod: reduced priming of proinflammatory effector CD4(+) T cells. Am J Pathol. 2013 May;182(5):1671-80. doi: 10.1016/j.ajpath.2013.01.032. Epub 2013 Mar 16. PMID: 23506849.
[6]. Tahvili S, TÖrngren M, et,al. Paquinimod prevents development of diabetes in the non-obese diabetic (NOD) mouse. PLoS One. 2018 May 9;13(5):e0196598. doi: 10.1371/journal.pone.0196598. PMID: 29742113; PMCID: PMC5942776.
[7]. Schelbergen RF, Geven EJ, et,al.Prophylactic treatment with S100A9 inhibitor paquinimod reduces pathology in experimental collagenase-induced osteoarthritis. Ann Rheum Dis. 2015 Dec;74(12):2254-8. doi: 10.1136/annrheumdis-2014-206517. Epub 2015 May 12. PMID: 25969431.
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