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Merck
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SML2883

Sigma-Aldrich

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

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About This Item

经验公式（希尔记法）:
C21H22N2O3
CAS号:
248282-01-1
分子量:
350.41
MDL编号:
MFCD18633277
UNSPSC代码:
12352200
NACRES:
NA.77

产品名称

Paquinimod, ≥98% (HPLC)

质量水平

100

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
0000317942
0000294949
0000294948
0000287589
0000171018

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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
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
Nina Fransén Pettersson et al.
PloS one, 13(9), e0203228-e0203228 (2018-09-06)
Quinoline-3-carboxamides (Q substances) are small molecule compounds with anti-inflammatory properties. In this study, we used one of these substances, Paquinimod, to treat a novel model for chronic liver inflammation and liver fibrosis, the NOD-Inflammation Fibrosis (N-IF) mouse. We show that
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
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