| Identification | Back Directory | [Name]
Paquinimod | [CAS]
248282-01-1 | [Synonyms]
ABR25757
ABR-25757
ABR 25757
ABR?215757
Paquinimod
ABR?215757; ABR 215757; ABR215757; PAQUINIMOD.
ABR 25757;ABR-25757;ABR25757;PAQUINIMOD;248282-01-1
N,5-diethyl-4-hydroxy-1-methyl-2-oxo-N-phenylquinoline-3-carboxamide
N,5-diethyl-4-hydroxy-1-methyl-2-oxo-N-phenyl-1,2-dihydroquinoline-3-carboxamide
3-Quinolinecarboxamide, N,5-diethyl-1,2-dihydro-4-hydroxy-1-methyl-2-oxo-N-phenyl- | [Molecular Formula]
C21H22N2O3 | [MDL Number]
MFCD18633277 | [MOL File]
248282-01-1.mol | [Molecular Weight]
350.41 |
| Chemical Properties | Back Directory | [Boiling point ]
487.3±45.0 °C(Predicted) | [density ]
1.267±0.06 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,2-8°C | [solubility ]
DMSO:15.0(Max Conc. mg/mL);42.8(Max Conc. mM) | [form ]
A solid | [pka]
4.50±1.00(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Paquinimod is a S100A9 inhibitor preventing S100A9 binding to TLR-4. Paquinimod reduces pathology in experimental collagenase-induced osteoarthritis. Paquinimod treatment of collagenase-induced OA (CIOA) resulted in significantly reduced synovial thickening (57%), osteophyte size at the medial femur (66%) and cruciate ligaments (67%) and cartilage damage at the medial tibia (47%) and femur (75%; n=7, untreated n=6). Paquinimod reduces leukocyte recruitment during sterile inflammation. Paquinimod also reduced priming of proinflammatory effector CD4(+) T cells. | [Biological Activity]
Paquinimod (ABR-215757) is an orally active quinoline-3-carboxamide (Q substance) class immunomodulator th at 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/MD2respectively). Paquinimod in vivo efficacy is demonstrated in murine models of autoimmune/inflammatory diseasesincluding liver fibrosiscollagen-induced osteoarthritisperitonitisEAEtype 1 diabeteslupus (0.04-25 mg/kg/day p.o.)and atherosclerosis (10 mg/kg i.p.). |
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| Company Name: |
ChemCell Biomedicine Co.,Ltd.
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020-13556033878 2965585218 13556033878 |
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https://www.chemicalbook.com/ShowSupplierProductsList15061/0.htm |
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