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TAK-220  ≥98%

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包装规格：1mg 5mg 10mg in glass bottle
溶解性：溶于DMSO（≥ 50 mg/mL)
产品描述：基本信息 产品编号： T10598 产品名称： TAK-220 CAS: 333994-00-6   储存条件 粉末 -20℃ 四年     分子式： C31H41ClN4O3 溶于液体 -80℃ 6个月 分子量 553.14- -20℃ 1个月 化学名：  1-acetyl-N-[3-[4-[(4-carbamoylphenyl)methyl]piperidin-1-yl]propyl]-N-(3-chloro-4-methylphenyl)piperidine-4-carboxamide Solubility (25°C)：   体外:   DMSO   Ethanol   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 1.8079mL 9.0393mL 18.0786mL 5mM 0.3616mL 1.8079mL 3.6157mL 10mM 0.1808mL 0.9039mL 1.8079mL   生物活性 产品描述 一种选择性的，可口服的 CCR5 拮抗剂，能够抑制 RANTES，MIP-1α 与 CCR5 结合，IC50 值分别为 3.5nM 和 1.4nM。 靶点 CCR HIV   体外研究 TAK-220 is a selective CCR5 antagonist,with IC50s of 3.5nM and 1.4nM for inhibition on the binding of RANTES and MIP-1α to CCR5 in CHO cells,respectively,but shows no effect on the binding to CCR1,CCR2b,CCR3,CCR4,or CCR7.TAK-220 (0-1000nM) interacts with CCR5 but not with RANTES and inhibits the CCR5-mediated Casup>2+signaling.TAK-220 inhibits R5 HIV-1 (JR-FL) envelope-mediated membrane fusion,with an IC50 value of 0.42nM,but does not alter X4 HIV-1 (HXB2) envelopemediated membrane fusion. TAK-220 also selectively inhibits HIV-1,with EC50s of 1.2nM (HIV-1 KK),0.72nM (HIV-1 CTV),1.7nM (HIV-1 HKW),1.7nM (HIV-1 HNK),0.93nM (HIV-1 HTN),and 0.55nM (HIV-1 HHA),and EC90s of 12nM (HIV-1 KK),5nM (HIV1 CTV),12nM (HIV-1 HKW),28nM (HIV-1 HNK),15nM (HIV-1 HTN),and 4nM (HIV-1 HHA) in PBMCs.TAK-220 shows potent inhibitory activity against the R5 isolates,with IC50s of 3.12nM against HIV-1 R5-08,13.47nM against HIV-1 R5-06,and 2.26nM against HIV-1 R5-18.TAK-220 (>100nM) has no toxicity in uninfected PBMCs.   推荐实验方法(仅供参考) 动物实验:   PHA-stimulated PBMCs are inoculated with 1,000 to 1,400 CCID50s of R5 HIV-1 (JR-FL) or X4 HIV-1 (IIIB) or with 13 to 55ng of p24 of HIV-1 clinical isolates per 4×106 cells and incubated for 4h.The cells are washed to remove unadsorbed viral particles and seeded into a 96-well plate (2×105 cells/well) with culture medium containing various concentrations of TAK220.The effects of high concentrations of human serum (HS) on the anti-HIV-1 activity of TAK-220 are examined with RPMI 1640 medium supplemented with either 20% FBS alone or 40% human type AB serum plus 10% FBS,100 U/mL recombinant human interleukin 2,and antibiotics.On day 4 after infection,the cells are subcultured at 1:2 with culture medium containing the same concentrations of the test compounds.On day 7 after infection,the culture supernatants are collected and their p24 antigen levels are determined with a p24 antigen enzyme-linked immunosorbent assay kit.
保存条件：-20℃

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