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TAK-779  ≥98%

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包装规格：1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO（≥ 25 mg/mL)
产品描述：基本信息 产品编号： T10597 产品名称： TAK-779 CAS: 229005-80-5   储存条件 粉末 2-8℃ 四年 分子式： C33H39ClN2O2 溶于液体 -80℃ 6个月 分子量 531.13 -20℃ 1个月 化学名：  dimethyl-[[4-[[3-(4-methylphenyl)-8,9-dihydro-7H-benzo[7]annulene-6-carbonyl]amino]phenyl]methyl]-(oxan-4-yl)azanium;chloride Solubility (25°C)：   体外:   DMSO   Ethanol 'mg/mL Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 1.8828mL 9.4139mL 18.8278mL 5mM 0.3766mL 1.8828mL 3.7656mL 10mM 0.1883mL 0.9414mL 1.8828mL   生物活性 产品描述 一种有效的，选择性的，非肽类 CCR5 和 CXCR3 拮抗剂，对 CCR5 的 Ki 值为 1.1nM，同时可以有效地，选择性地抑制 R5 HIV-1，在 MAGI-CCR5 细胞中，EC50 和 EC90 值分别为 1.2nM 和 5.7nM。 靶点 CCR HIV CXCR   体外研究 TAK-779 is a potent and selective nonpeptide antagonist of CCR5,with a Ki of 1.1nM,and effectively and selectively inhibits R5 HIV-1,with EC50 and EC90 of 1.2nM and 5.7nM,respectively,in MAGI-CCR5 cells.TAK-779 less potently blocks the binding of [125I]-monocyte chemotactic protein 1 to CCR2b in CHO/CCR2b cells,with an IC50 for CCR2b of 27nM.TAK-779 also completely inhibits the binding of [125I]-RANTES to CHO/CCR5 cells with an IC50 of 1.4nM.TAK-779 (20nM) selectively inhibits CCR5-mediated Ca2+-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 (10mg/kg per day,s.c.) significantly prolongs the allograft survival of the rat intestinal transplantation model.TAK779 also decreases the number of CD4+as well as CD8+T cells in spleen,blood and recipient mesenteric lymph nodes (MLN).TAK-779 (150µg 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 MOGspecific T cells to transfer experimental autoimmune encephalomyelitis (EAE).   推荐实验方法(仅供参考) 细胞实验:   The anti-HIV-1 activities of the test compounds (TAK-779,etc.) are based on the inhibition of virus-induced infectious focus formation in MAGI-CCR5 cells and the reduction of p24 antigen production in PBMCs.In brief, MAGI-CCR5 cells (1×104 cells per well) are cultured in a microtiter tray. After a 24-h incubation at 37℃,the culture supernatants are replaced with fresh culture media containing the virus (≈300 focus forming units per well) and various concentrations of the test compounds (TAK-779,etc.).After a 2-day incubation,the cells are fixed and stained with 5-bromo-4-chloro-3-indolyl-β-dgalactosidase.The number of infected (blue) cells is counted microscopically.For the PBMC assays, phytohemagglutininstimulated PBMCs (2.5×105 cells per 500μl) are infected with HIV-1 in the presence of various concentrations of the test compounds (TAK-779,etc.).The amounts of the virus used for infection are, depending on the replicability of each strain,generally 1-10ng of p24 per 2.5×105 cells. After an overnight incubation at 37℃,the cells are washed extensively to remove unadsorbed viral particles and are incubated further with culture media containing the same concentrations of the compounds as those used during viral adsorption.On day 6 after viral infection,the culture supernatants are collected and determined for their p24 antigen levels with a sandwich ELISA kit.The cytotoxicities of the compounds are evaluated in parallel with their antiviral activities.They are based on the viability and proliferation of mock-infected cells.   动物实验:   Mice The mice are immunized with MOG and are treated s.c.with TAK-779 or vehicle.The mice (N=10) are injected s.c.with 150µg TAK-779 (dissolved in 5% mannitol solution) in a volume of 100µL,once daily after MOG immunization.TAK-779 injection is started from day 0 after immunization and continued once daily for 22 days.The dose of 150µg is determined based on the observations in prior experiments that the dose of 50µg per mouse can not produce inhibition,and a dose of more than 100µg per mouse is required to produce significant inhibition.The dose of 150µg per mouse has also been used in other mouse experimental models,and approximately the same dose is used in allograft rejection and asthma models.As a control,an equal volume of PBS containing 5% mannitol is injected daily in the control mice (N=10).
保存条件：2-8℃

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