5-(2,6-二氯苯基)-2-((2,4-二氟苯基)硫基)-6H-嘧啶并[1,6-b]哒嗪-6-酮

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5-(2,6-二氯苯基)-2-((2,4-二氟苯基)硫基)-6H-嘧啶并[1,6-b]哒嗪-6-酮

5-(2,6-二氯苯基)-2-((2,4-二氟苯基)硫基)-6H-嘧啶并[1,6-b]哒嗪-6-酮

编号ABP000251 化学名称VX-745,VX745/ CAS209410-46-8 MDL: MFCD09834070 分子式C19H9Cl2F2N3OS 分子量436.268 纯度 >98%

化学名称 : 5-(2,6-二氯苯基)-2-((2,4-二氟苯基)硫基)-6H-嘧啶并[1,6-b]哒嗪-6-酮

CAS : 209410-46-8

英文名称: VX-745,VX745/

英文同义词: 5-(2,6-DICHLOROPHENYL)-2-((2,4-DIFLUOROPHENYL)THIO)-6H-PYRIMIDO[1,6-B]PYRIDAZIN-6-ONE

溶解度:Soluble to 100 mM in DMSO

储存条件:Store at -20°C

生物活性

VX-745 is a lead anti-inflammatory candidate, p38 MAPK inhibitor (IC50=10 nM) for the treatment of Rheumatoid arthritis (RA). p38 MAPK is a specific enzyme that regulates the production of IL-1,  IL-2, IL-6, TNFα, chemokines and nitric oxide (NO), as part of acute and chronic inflammatory responses.In vitro, VX-745 was selective for p38 MAPK compared to a large panel of kinases (IC50≥20µM). VX-745 selectively inhibited p38α MAPK (IC50=10 nM), p38β MAPK (IC50 =220 nM) [368149], but not p38γ MAPK (IC50≥20 µM). In addition, cell data for VX-745 provided IC50 values of 56 and 52 nM for IL-1β and TNFα, respectively, and VX-745 blocked IL-6 and IL-8 production induced by IL-1 and TNFα. In a human whole blood assay, IC50 values were 152 and 177 nM for IL-1β and TNFα inhibition, respectively.

参考文献

[1] Haddad JJ. Curr Opin Investig Drugs. 2001 Aug;2(8):1070-6

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