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Paquinimod (ABR 25757) (Synonyms: ABR-25757)

Catalog No.GC31346

Paquinimod (ABR 25757) (ABR 25757) is a specific inhibitor of S100A8/S100A9.

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Paquinimod (ABR 25757) Chemical Structure

Cas No.: 248282-01-1

Size Price Stock Qty
10mM (in 1mL DMSO)
$116.00
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10mg
$105.00
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50mg
$315.00
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100mg
$525.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Tissue experiment [1]:

Tissue

Human synovium

Preparation Method

Incubated osteoarthritis (OA) synovium with human S100A916 and paquinimod and measured the protein release.

Reaction Conditions

350 µM paquinimod;30 min preincubated

Applications

S100A9 clearly upregulated IL-6, IL-8 and TNF-α protein levels in OA synovia, and addition of paquinimodsignificantly inhibited this upregulation for IL-6 and IL-8, but not TNF-α.

Animal experiment [2]:

Animal models

IQAD Tg C57Bl/6 mice

Preparation Method

Mice were treated with 10 mg/kg/day paquinimod, added into the drinking water starting 7 days prior to the addition of DSS and continued during the DSS regimen. Control mice received the same dose of paquinimod for 14 days. In all experiments, water was changed twice a week.

Dosage form

10 mg/kg/day paquinimod;14days;added into the drinking water

Applications

Mice prophylactically treated with paquinimod 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.

References:

[1].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.

[2]. 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.

Background

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.

Chemical Properties

Cas No. 248282-01-1 SDF
Synonyms ABR-25757
Canonical SMILES O=C(C1=C(O)C2=C(C=CC=C2CC)N(C)C1=O)N(CC)C3=CC=CC=C3
Formula C21H22N2O3 M.Wt 350.41
Solubility DMSO : ≥ 125 mg/mL (356.72 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.8538 mL 14.269 mL 28.538 mL
5 mM 0.5708 mL 2.8538 mL 5.7076 mL
10 mM 0.2854 mL 1.4269 mL 2.8538 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 24 reference(s) in Google Scholar.)

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