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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化学信息
| 名称 | Paquinimod |
|---|---|
| Iupac 化学名称 | N,5-diethyl-4-hydroxy-1-methyl-2-oxo-N-phenyl-1,2-dihydroquinoline-3-carboxamide |
| 同义词 | ABR‑215757; ABR 215757; ABR215757; Paquinimod. |
| 英文同义词 | ABR‑215757; ABR 215757; ABR215757; Paquinimod. |
| 分子式 | C21H22N2O3 |
| 分子量 | 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号 | 248282-01-1 |
| 相关CAS号 |
订购信息
| 包装 | 价格 | 库存 | 纯度 | 备货期 |
|---|---|---|---|---|
| 大货 | 询价 | 询价 | 询价 |
| 外观性状 | 固体粉末 |
|---|---|
| 纯度 | 98% Min. |
| 存储 | 短期（几天到几周）为0-4摄氏度，长期（几个月）为-20摄氏度 |
| 可溶性 | 可溶于DMSO |
| 处理方式 | |
| 运输条件 | 作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周 |
| 海关编码 |
| Targets | |
|---|---|
| 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.
