84088-42-6
84088-42-6 structure
- Name: Roquinimex
- Chemical Name: 4-hydroxy-N,1-dimethyl-2-oxo-N-phenylquinoline-3-carboxamide
- CAS Number: 84088-42-6
- Molecular Formula: C18H16N2O3
- Molecular Weight: 308.331
- Catalog: Signaling Pathways Apoptosis TNF Receptor
- Create Date: 2018-06-30 10:50:24
- Modify Date: 2024-01-09 20:44:14
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Roquinimex (Linomide; PNU212616; ABR212616) is a quinoline derivative immunostimulant which increases NK cell activity and macrophage cytotoxicity; inhibits angiogenesis and reduces the secretion of TNF alpha.IC50 value:Target: TNF alphaProphylactic administration of DSS-treated mice with roquinimex significantly reduced clinical signs of colitis, MDS and the CH-reduction. Moreover, in roquinimex treated animals, the MPO activity was significantly reduced by more than 50% compared to DSS control mice. Notably, therapeutic administration of roquinimex in DSS-treated mice also significantly inhibited the MDS, CH-reduction and MPO activity [2]. Linomide, a synthetic immunomodulator, at concentrations effective in vivo reduces the number of MBP-reactive TNF-alpha and increases MBP-reactive IL-10 and TGF-beta mRNA expressing MNC from MS patients' blood when analysed in vitro. Compared to dexamethasone, Linomide up-regulated levels of blood MNC expressing mRNA of TGF-beta after culture in presence of MBP [3].
| Name | 4-hydroxy-N,1-dimethyl-2-oxo-N-phenylquinoline-3-carboxamide |
|---|---|
| Synonyms |
Roquinimex
LS-2616 1,2-Dihydro-4-hydroxy-N,1-dimethyl-2-oxo-N-phenyl-3-quinolinecarboxamide 4-Hydroxy-N,1-dimethyl-2-oxo-N-phenyl-1,2-dihydro-3-quinolinecarboxamide FCF-89 Linomide 4-hydroxy-N,1-dimethyl-2-oxo-N-phenyl-1,2-dihydroquinoline-3-carboxamide N-phenyl-N-methyl-1,2-dihydro-4-hydroxy-1-methyl-2-oxoquinoline-3-carboxamide 3-Quinolinecarboxamide, 1,2-dihydro-4-hydroxy-N,1-dimethyl-2-oxo-N-phenyl- N-phenyl-N-methyl-1,2-dihydro-4-hydroxy-1-methyl-2-oxo-quinoline-3-carboxamide |
| Description | Roquinimex (Linomide; PNU212616; ABR212616) is a quinoline derivative immunostimulant which increases NK cell activity and macrophage cytotoxicity; inhibits angiogenesis and reduces the secretion of TNF alpha.IC50 value:Target: TNF alphaProphylactic administration of DSS-treated mice with roquinimex significantly reduced clinical signs of colitis, MDS and the CH-reduction. Moreover, in roquinimex treated animals, the MPO activity was significantly reduced by more than 50% compared to DSS control mice. Notably, therapeutic administration of roquinimex in DSS-treated mice also significantly inhibited the MDS, CH-reduction and MPO activity [2]. Linomide, a synthetic immunomodulator, at concentrations effective in vivo reduces the number of MBP-reactive TNF-alpha and increases MBP-reactive IL-10 and TGF-beta mRNA expressing MNC from MS patients' blood when analysed in vitro. Compared to dexamethasone, Linomide up-regulated levels of blood MNC expressing mRNA of TGF-beta after culture in presence of MBP [3]. |
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| Related Catalog | |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Boiling Point | 436.2±45.0 °C at 760 mmHg |
| Melting Point | 204 °C(dec.) |
| Molecular Formula | C18H16N2O3 |
| Molecular Weight | 308.331 |
| Flash Point | 217.6±28.7 °C |
| Exact Mass | 308.116089 |
| PSA | 62.54000 |
| LogP | 1.65 |
| Vapour Pressure | 0.0±1.1 mmHg at 25°C |
| Index of Refraction | 1.686 |
| Hazard Codes | Xn: Harmful; |
|---|---|
| Risk Phrases | R22 |
| Safety Phrases | S36/37 |
| RIDADR | UN 2811 |
| HS Code | 2933790090 |
|
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| Literature: Sjoevall, Sven; Hansen, Lars; Granquist, Bo Organic Process Research and Development, 2004 , vol. 8, # 5 p. 802 - 807 |
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| Literature: Joensson, Stig; Andersson, Gunnar; Fex, Tomas; Fristedt, Tomas; Hedlund, Gunnar; Jansson, Karl; Abramo, Lisbeth; Fritzson, Ingela; Pekarski, Olga; Runstroem, Anna; Sandin, Helena; Thuvesson, Ingela; Bjoerk, Anders Journal of Medicinal Chemistry, 2004 , vol. 47, # 8 p. 2075 - 2088 |
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| Literature: Journal of Medicinal Chemistry, , vol. 47, # 8 p. 2075 - 2088 |
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| Literature: Journal of Medicinal Chemistry, , vol. 47, # 8 p. 2075 - 2088 |
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| Literature: Journal of Medicinal Chemistry, , vol. 47, # 8 p. 2075 - 2088 |
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| Literature: Bioorganic and Medicinal Chemistry Letters, , vol. 11, # 4 p. 451 - 452 |
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~49%
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| Literature: Khan, Saeed R.; Mhaka, Annastasiah; Pili, Roberto; Isaacs, John T. Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 4 p. 451 - 452 |
| Precursor 7 | |
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| DownStream 0 | |
| HS Code | 2933790090 |
|---|---|
| Summary | 2933790090. other lactams. VAT:17.0%. Tax rebate rate:9.0%. . MFN tariff:9.0%. General tariff:20.0% |