TAK 799 ;TAK 779
中文名称 | TAK 799 ;TAK 779 |
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中文同义词 | 化合物TAK-779;N,N-二甲基-N-(4-(2-(对甲苯基)-6,7-二氢-5H-苯并[7]环庚烯-8-甲酰胺基)苄基)四氢-2H-吡喃-4-铵氯化物 |
英文名称 | Tak 799 |
英文同义词 | 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;N,N-Dimethyl-N-(4-(((2-(4-methylphenyl)-6,7-dihydro-5H-benzocyclohepten-8-yl)carbonyl)amino)benzyl)tetrahydro-2H-pyran-4-aminium chloride;Tak 799;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;TAK779;TAK 799;TAKEDA 779 |
CAS号 | 229005-80-5 |
分子式 | C33H39N2O2.Cl |
分子量 | 531.136 |
EINECS号 | |
相关类别 | 标准品 |
Mol文件 | 229005-80-5.mol |
结构式 |
TAK 799 ;TAK 779 性质
储存条件 | 2-8°C |
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溶解度 | 在水中的溶解度为性3mg/mL,澄清(加热) |
形态 | 粉末 |
颜色 | 白色至米色 |
MIP-1α-CCR5 1 nM (IC 50 , in CHO/CCR5 cells) |
MIP-1β-CCR5 1 nM (IC 50 , in CHO/CCR5 cells) |
RANTES-CCR5 1.4 nM (IC 50 , in CHO/CCR5 cells) |
MCP-1-CCR2b 27 nM (IC 50 , in CHO/CCR5 cells) |
R5 HIV-1 (Ba-L) 1.2 nM (EC 50 , in MAGI-CCR5 cells) |
R5 HIV-1 (Ba-L) 5.7 nM (EC90, in MAGI-CCR5 cells) |
R5 HIV-1 (Ba-L) 3.7 nM (EC 50 , in PBMCs) |
R5 HIV-1 (Ba-L) 12.8 nM (EC90, in PBMCs) |
R5 HIV-1 (KK) 1.6 nM (EC 50 , in PBMCs) |
R5 HIV-1 (KK) 20.8 nM (EC90, in PBMCs) |
R5 HIV-1 (HHA) 3.2 nM (EC 50 , in PBMCs) |
R5 HIV-1 (HHA) 7.5 nM (EC90, in PBMCs) |
R5 HIV-1 (CTV) 3.5 nM (EC 50 , in PBMCs) |
R5 HIV-1 (CTV) 27 nM (EC90, in PBMCs) |
mCXCR3 369 nM (IC 50 , in PBMCs) |
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.
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).
安全信息
WGK Germany | 3 |
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更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2023/01/06 | S0438 | TAK 799 ;TAK 779 TAK-779 | 229005-80-5 | 25mg | 6871.41元 |