TAK-779
TAK-779(TAK-779)
CAS: 229005-80-5
化学式: C33H39N2O2.Cl
| 中文名 | TAK-779 |
| 英文名 | TAK-779 |
| 别名 | 化合物TAK-779 |
| 英文别名 | TAK779 Tak 799 TAK-779 TAK 779 TAK 799 TAK 799 Takeda 779 TAKEDA 779 TAK 799 TAK 779 N,N-Dimethyl-N-[4-[[[2-(4-methylphenyl)-6,7-dihydro-5H-benzohepten-8-yl]carbonyl]amino]benzyl]tetrahydro-2H-pyran-4-aminium chloride N,N-Dimethyl-N-(4-(((2-(4-methylphenyl)-6,7-dihydro-5H-benzocyclohepten-8-yl)carbonyl)amino)benzyl)tetrahydro-2H-pyran-4-aminium chloride 2H-Oyran-4-aminium, N-((4-(((6,7-dihydro-2-(4-methylphenyl)-5H-benzocyclohepten-8-yl)carbonyl)amino)phenyl)methyl)tetrahydro-N,N-dimethyl- 2H-Pyran-4-aminium, N,N-dimethyl-N-(4-(((2-(4-methylphenyl)-6,7-dihydro-5H-benzocyclohepten-8-yl)carbonyl)amino)benzyl)tetrahydro-, chloride |
| CAS | 229005-80-5 |
| 化学式 | C33H39N2O2.Cl |
| 分子量 | 531.136 |
| 溶解度 | H2O: 可溶物3mg/mL，澄清 (温热) |
| 存储条件 | 2-8°C |
| 外观 | 粉末 |
| 颜色 | white to beige |
| 体外研究 | TAK-779 is a potent and selective nonpeptide antagonist of CCR5, with a K i of 1.1 nM, and effectively and selectively inhibits R5 HIV-1, with EC 50 and EC 90 of 1.2 nM and 5.7 nM, respectively, in MAGI-CCR5 cells. TAK-779 less potently blocks the binding of [ 125 I]-monocyte chemotactic protein 1 to CCR2b in CHO/CCR2b cells, with an IC 50 for CCR2b of 27 nM. TAK-779 also completely inhibits the binding of [ 125 I]-RANTES to CHO/CCR5 cells with an IC 50 of 1.4 nM. TAK-779 (20 nM) selectively inhibits CCR5-mediated Ca 2+ -signaling. In addition, TAK-779 shows no inhibition on X4 HIV-1 strains. TAK-779 is an antagonist of CXCR3, and inhibits the migration of T cells but not T cell proliferation. |
| 体内研究 | TAK-779 (10 mg/kg per day, s.c.) significantly prolongs the allograft survival of the rat intestinal transplantation model. TAK-779 also decreases the number of CD4 + as well as CD8 + T cells in spleen, blood and recipient mesenteric lymph nodes (MLN). TAK-779 (150 µg per mouse, s.c.) supppresses the development of experimental autoimmune encephalomyelitis (EAE) in myelin oligodendrocyte glycoprotein (MOG)-immunized C57BL/6 mice. TAK-779 decreases the infiltration of CXCR3 and CCR5 bearing leukocytes into the spinal cord. TAK-779 does not alter myelin oligodendrocyte glycoprotein (MOG)-specific immune responses or affect the potential of MOG-specific T cells to transfer experimental autoimmune encephalomyelitis (EAE). |
| WGK Germany | 3 |
TAK-779 - 配置溶液浓度参考
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.883 ml | 9.414 ml | 18.828 ml |
| 5 mM | 0.377 ml | 1.883 ml | 3.766 ml |
| 10 mM | 0.188 ml | 0.941 ml | 1.883 ml |
| 5 mM | 0.038 ml | 0.188 ml | 0.377 ml |
最后更新：2024-01-02 23:10:35
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