中文名 | Paquinimod |
英文名 | Paquinimod |
别名 | 帕奎莫德 化合物PAQUINIMOD N,5-二乙基-4-羟基-1-甲基-2-氧代-N-苯基-1,2-二氢喹啉-3-甲酰胺 |
英文别名 | ABR25757 ABR 25757 ABR-25757 PAQUINIMOD ABR?215757 Paquinimod ABR215757 248282-01-1 ABR 215757 PAQUINIMOD. N,5-diethyl-4-hydroxy-1-methyl-2-oxo-N-phenyl-1,2-dihydroquinoline-3-carboxamide |
CAS | 248282-01-1 |
化学式 | C21H22N2O3 |
分子量 | 350.41 |
密度 | 1.267±0.06 g/cm3(Predicted) |
沸点 | 487.3±45.0 °C(Predicted) |
溶解度 | DMSO : ≥ 125 mg/mL (356.72 mM) |
酸度系数 | 4.50±1.00(Predicted) |
存储条件 | 2-8°C |
体内研究 | S100A9 is a calcium-binding protein of the S100 family. Paquinimod is an immunomodulatory compound preventing S100A9 binding to TLR-4. Prophylactic treatment with S100A9 inhibitor Paquinimod reduces pathology in experimental collagenase-induced osteoarthritis. Paquinimod is a potent inhibitor of insulitis and diabetes development in the NOD mouse. To assess the preventive efficacy of Paquinimod on diabetes development in female NOD mice, groups of mice are treated with daily doses of 0.04, 0.2, 1, and 5 mg/kg/day of Paquinimod from week 10 of age until week 20 of age. Glycosuria is analyzed on a weekly basis from 10 weeks of age until the endpoint of the experiment at 40 weeks of age. There is a clear dose-dependent reduction in diabetes development in the Paquinimod-treated mice. |
上游原料 | 1,2-DIHYDRO-4-HYDROXY-5-ETHYL-1-METHYL-2-OXO-QUINOLINE-3-CARBOXYLIC ACID METHYL ESTER 2-氨基-6-乙基苯甲酸 |
参考资料 展开查看 | 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.854 ml | 14.269 ml | 28.537 ml |
5 mM | 0.571 ml | 2.854 ml | 5.707 ml |
10 mM | 0.285 ml | 1.427 ml | 2.854 ml |
5 mM | 0.057 ml | 0.285 ml | 0.571 ml |
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