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Merck
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Key Documents

SML2883

Sigma-Aldrich

Paquinimod

≥98% (HPLC), powder, immunomodulator

Sinônimo(s):

ABR 215757, ABR 25757, ABR-215757, ABR-25757, ABR215757, ABR25757, N,5-Diethyl-1,2-dihydro-4-hydroxy-1-methyl-2-oxo-N-phenyl-3-quinolinecarboxamide, N-Ethyl-N-phenyl-1,2-dihydro-5-ethyl-4-hydroxy-1-methyl-2-oxoquinoline-3-carboxamide, N-Ethyl-N-phenyl-5-ethyl-1,2-dihydro-4-hydroxy-1-methyl-2-oxoquinoline-3-carboxamide

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About This Item

Fórmula empírica (Notação de Hill):
C21H22N2O3
Número CAS:
Peso molecular:
350.41
Número MDL:
Código UNSPSC:
12352200
NACRES:
NA.77

product name

Paquinimod, ≥98% (HPLC)

Nível de qualidade

Ensaio

≥98% (HPLC)

forma

powder

cor

white to beige

solubilidade

DMSO: 2 mg/mL, clear

temperatura de armazenamento

2-8°C

Ações bioquímicas/fisiológicas

Paquinimod (ABR-215757) is an orally active quinoline-3-carboxamide (Q substance) class immunomodulator that targets S100A9 (Calgranulin B; MRP14) via direct binding and blocks its interaction with receptor for advanced glycation end products (RAGE) and Toll-like receptor 4 (IC50 = 26 μM & 23 μM against 100 nM hS100A9 from binding immobilized hRAGE & hTLR4/MD2, respectively). Paquinimod in vivo efficacy is demonstrated in murine models of autoimmune/inflammatory diseases, including liver fibrosis, collagen-induced osteoarthritis, peritonitis, EAE, type 1 diabetes, lupus (0.04-25 mg/kg/day p.o.), and atherosclerosis (10 mg/kg i.p.).

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 3

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable


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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
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
Sahar Tahvili et al.
PloS one, 13(5), e0196598-e0196598 (2018-05-10)
Quinoline-3-carboxamides (Q compounds) are immunomodulatory compounds that have shown efficacy both in autoimmune disease and cancer. We have in here investigated the impact of one such compound, paquinimod, on the development of diabetes in the NOD mouse model for type
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

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