所有图片(1)
别名:
ABR 215757, ABR 25757, ABR-215757, ABR-25757, ABR215757, ABR25757, N,5-二乙基-1,2-二氢-4-羟基-1-甲基-2-氧基-N-苯基-3-喹啉甲酰胺, N-乙基-N-苯基-1,2-二氢-5-乙基-4-羟基-1-甲基-2-羟基喹啉-3-甲酰胺, N-乙基-N-苯基-5-乙基-1,2-二氢-4-羟基-1-甲基-2-羟基喹啉-3-甲酰胺
经验公式（希尔记法）:
C21H22N2O3
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生化/生理作用
Paquinimod (ABR-215757)是一种口服活性喹啉-3-甲酰胺（Q物质）类免疫调节剂，靶向S100A9（Calgranulin B；MRP14），并阻断其与晚期糖基化终产物受体(RAGE)和Toll样受体4的相互作用（IC50 = 26 μM & 23 μM对100 nM hS100A9， 分别结合固定化hRAGE & hTLR4/MD2）。Paquinimod在自身免疫性/炎症性疾病的小鼠模型中证明了体内疗效，包括肝纤维化、胶原诱导的骨关节炎、腹膜炎、EAE、1型糖尿病、狼疮(0.04-25 mg/kg/day p.o)和动脉粥样硬化(10 mg/kg i.p.)。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Hong Gong et al.
Journal of neuroinflammation, 15(1), 252-252 (2018-09-06)
Depression is one of the most common mental disorders characterized mainly by low mood and loss of interest or pleasure. About a third of patients with depression do not respond to classic antidepressant treatments. Recent evidence suggests that Mrp8/14 (myeloid-related
Stig Jönsson et al.
Journal of medicinal chemistry, 47(8), 2075-2088 (2004-04-02)
Roquinimex-related 3-quinolinecarboxamide derivatives were prepared and evaluated for treatment of autoimmune disorders. The compounds were tested in mice for their inhibitory effects on disease development in the acute experimental autoimmune encephalomyelitis model and selected compounds in the beagle dog for
Hans Carlsten et al.
International immunopharmacology, 4(12), 1515-1523 (2004-09-08)
Autoimmune, lupus-prone MRL lpr/lpr mice were treated orally with oxo-quinoline-3-carboxamide (ABR-25757), a newly developed immunomodulator. Treatment was initiated in one set of experiment at the age of 10 weeks, before the onset of clinically apparent disease, and in another set
Ling Yan et al.
Atherosclerosis, 228(1), 69-79 (2013-03-19)
There is an emerging widespread interest in the role of damage-associated molecular pattern molecules (DAMP) S100A8, S100A9 and S100A12 in cardiovascular and other diseases. In this study we tested the efficacy of ABR-215757, a S100 protein binding immuno-modulatory compound to
Adnan Deronic et al.
International immunopharmacology, 18(2), 290-297 (2013-12-29)
Quinoline-3-carboxamides (Q-compounds) are currently in clinical development for both autoimmune disease and cancer. We have previously shown that the Q-compound paquinimod (ABR-215757) significantly ameliorates disease symptoms in several mouse models of human inflammatory disease. Considering that recruitment of inflammatory cells
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