Paquinimod
Paquinimod, also known as ABR‑215757, is a S100A9 inhibitor preventing S100A9 binding to TLR-4. Paquinimod reduces pathology in experimental collagenase-induced osteoarthritis. Paquinimod treatment of collagenase-induced OA (CIOA) resulted in significantly reduced synovial thickening (57%), osteophyte size at the medial femur (66%) and cruciate ligaments (67%) and cartilage damage at the medial tibia (47%) and femur (75%; n=7, untreated n=6). Paquinimod reduces leukocyte recruitment during sterile inflammation. Paquinimod also reduced priming of proinflammatory effector CD4(+) T cells.
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Chemical Information
| Name | Paquinimod |
|---|---|
| Iupac Chemical Name | N,5-diethyl-4-hydroxy-1-methyl-2-oxo-N-phenyl-1,2-dihydroquinoline-3-carboxamide |
| Synonyms | ABR‑215757; ABR 215757; ABR215757; Paquinimod. |
| Molecular Formula | C21H22N2O3 |
| Molecular Weight | 350.42 |
| Smile | O=C(C1=C(O)C2=C(N(C)C1=O)C=CC=C2CC)N(CC)C3=CC=CC=C3 |
| InChiKey | DIKSYHCCYVYKRO-UHFFFAOYSA-N |
| InChi | InChI=1S/C21H22N2O3/c1-4-14-10-9-13-16-17(14)19(24)18(20(25)22(16)3)21(26)23(5-2)15-11-7-6-8-12-15/h6-13,24H,4-5H2,1-3H3 |
| CAS Number | 248282-01-1 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Solid powder |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Solubility | Soluble in DMSO |
| Handling | |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| HS Code |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: Schelbergen RF, Geven EJ, van den Bosch MH, Eriksson H, Leanderson T, Vogl T, Roth J, van de Loo FA, Koenders MI, van der Kraan PM, van den Berg WB, Blom AB, van Lent PL. 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. PubMed PMID: 25969431.
2: Wache C, Klein M, Ostergaard C, Angele B, Häcker H, Pfister HW, Pruenster M, Sperandio M, Leanderson T, Roth J, Vogl T, Koedel U. 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. PubMed PMID: 25605866.
3: Deronic A, Helmersson S, Leanderson T, Ivars F. The quinoline-3-carboxamide paquinimod (ABR-215757) reduces leukocyte recruitment during sterile inflammation: leukocyte- and context-specific effects. Int Immunopharmacol. 2014 Feb;18(2):290-7. doi: 10.1016/j.intimp.2013.12.008. Epub 2013 Dec 23. PubMed PMID: 24370393.
4: Helmersson S, Sundstedt A, Deronic A, Leanderson T, Ivars F. 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. PubMed PMID: 23506849.
5: Yan L, Bjork P, Butuc R, Gawdzik J, Earley J, Kim G, Hofmann Bowman MA. Beneficial effects of quinoline-3-carboxamide (ABR-215757) on atherosclerotic plaque morphology in S100A12 transgenic ApoE null mice. Atherosclerosis. 2013 May;228(1):69-79. doi: 10.1016/j.atherosclerosis.2013.02.023. Epub 2013 Feb 28. PubMed PMID: 23497784; PubMed Central PMCID: PMC3640742.
6: Bengtsson AA, Sturfelt G, Lood C, Rönnblom L, van Vollenhoven RF, Axelsson B, Sparre B, Tuvesson H, Ohman MW, Leanderson T. Pharmacokinetics, tolerability, and preliminary efficacy of paquinimod (ABR-215757), a new quinoline-3-carboxamide derivative: studies in lupus-prone mice and a multicenter, randomized, double-blind, placebo-controlled, repeat-dose, dose-ranging study in patients with systemic lupus erythematosus. Arthritis Rheum. 2012 May;64(5):1579-88. doi: 10.1002/art.33493. PubMed PMID: 22131101.
Chemical Structure
