SML2883
Paquinimod
≥98% (HPLC), powder, immunomodulator
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
产品名称
Paquinimod, ≥98% (HPLC)
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
N1(c2c(c(ccc2)CC)C(=O)C(C1=O)C(=O)N(CC)c3ccccc3)C
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/h6-13,18H,4-5H2,1-3H3
InChI key
RBHDLRDFJPBLNO-UHFFFAOYSA-N
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.)。
口服活性S100A9（Calgranulin B；MRP14）阻滞剂在自身免疫性疾病的小鼠模型中具有体内疗效。
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
R F Schelbergen et al.
Annals of the rheumatic diseases, 74(12), 2254-2258 (2015-05-15)
Alarmins S100A8/A9 regulate pathology in experimental osteoarthritis (OA). Paquinimod is an immunomodulatory compound preventing S100A9 binding to TLR-4. We investigated the effect of paquinimod on experimental OA and human OA synovium. Two OA mouse models differing in level of synovial
Per Björk et al.
PLoS biology, 7(4), e97-e97 (2009-05-01)
Despite more than 25 years of research, the molecular targets of quinoline-3-carboxamides have been elusive although these compounds are currently in Phase II and III development for treatment of autoimmune/inflammatory diseases in humans. Using photoaffinity cross-linking of a radioactively labelled
Christina Wache et al.
The Journal of infectious diseases, 212(2), 247-257 (2015-01-22)
Neutrophilic inflammation often persists for days despite effective antibiotic treatment and contributes to brain damage in bacterial meningitis. We propose here that myeloid-related protein 14 (MRP14), an abundant cytosolic protein in myeloid cells, acts as an endogenous danger signal, driving
Sofia Helmersson et al.
The American journal of pathology, 182(5), 1671-1680 (2013-03-20)
Quinoline-3-carboxamide compounds (Q compounds) have demonstrated efficacy in treating autoimmune disease in both humans and mice. However, the mode of action of these compounds is poorly understood. Here, we show that preventive treatment with the Q compound paquinimod (ABR-215757) during
Michael J Kraakman et al.
The Journal of clinical investigation, 127(6), 2133-2147 (2017-05-16)
Platelets play a critical role in atherogenesis and thrombosis-mediated myocardial ischemia, processes that are accelerated in diabetes. Whether hyperglycemia promotes platelet production and whether enhanced platelet production contributes to enhanced atherothrombosis remains unknown. Here we found that in response to
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