229005-80-5
基本信息
Tak 799
Takeda 779
TAK-779(Cl)
TAK 799
TAK 779
TAK-779 >=98% (HPLC)
TAK-779
TAK 779
TAK779
TAK779
TAK 799
TAKEDA 779
TAK-779 Chemical Structure
N,N-Dimethyl-N-[4-[[[2-(4-methylphenyl)-6,7-dihydro-5H-benzohepten-8-yl]carbonyl]amino]benzyl]tetrahydro-2H-pyran-4-aminium chloride
物理化学性质
| 储存条件 | 2-8°C |
| 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 |
安全数据
| WGK Germany | 3 |
TAK 799 ;TAK 779价格(试剂级)
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2023/01/06 | S0438 | TAK 799 ;TAK 779 TAK-779 | 229005-80-5 | 25mg | 6871.41元 |
常见问题列表
|
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).