Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TAK-220 is a selective and orally bioavailable CCR5 antagonist (IC50s: 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5, respectively).
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 1,820 | 5日内发货 | ||
5 mg | ¥ 2,890 | 5日内发货 | ||
25 mg | ¥ 9,620 | 6-8周 | ||
50 mg | ¥ 12,500 | 6-8周 | ||
100 mg | ¥ 17,500 | 6-8周 | ||
1 mL * 10 mM (in DMSO) | ¥ 3,180 | 5日内发货 |
产品描述 | TAK-220 is a selective and orally bioavailable CCR5 antagonist (IC50s: 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5, respectively). |
靶点活性 | HIV-1 (HHA):0.55 nM (EC50)(in PBMCs), HIV-1 (HTN):0.93 nM (EC50)(in PBMCs), HIV-1 (KK):1.2 nM (EC50)(in PBMCs), HIV-1 (KK):12 nM (EC90)(in PBMCs), MIP-1α-CCR5:1.4 nM (in CHO cells), HIV-1 (HHA):4 nM (EC90)(in PBMCs), HIV-1 (HKW):1.7 nM (EC50)(in PBMCs), HIV-1 (HKW):12 nM (EC90)(in PBMCs), HIV-1 (HNK):1.7 nM (EC50)(in PBMCs), HIV-1 (HTN):15 nM (EC90)(in PBMCs), X4 HIV-1 (CTV):0.72 nM (EC50)(in PBMCs), X4 HIV-1 (CTV):5 nM (EC90)(in PBMCs), RANTES-CCR5:3.5 nM (in CHO cells), HIV-1 (HNK):28 nM (EC90)(in PBMCs) |
体外活性 | TAK-220 inhibits R5 HIV-1 (JR-FL) envelope-mediated membrane fusion (IC50: 0.42 nM). TAK-220 shows potent inhibitory activity against the R5 isolates, with IC50s of 3.12 nM against HIV-1 R5-08, 13.47 nM against HIV-1 R5-06, and 2.26 nM against HIV-1 R5-18. TAK-220 (>100 nM) has no toxicity in uninfected PBMCs. TAK-220 (0-1000 nM) interacts with CCR5 but not with RANTES and inhibits the CCR5-mediated Casup>2+ signaling. TAK-220 also selectively inhibits HIV-1, with EC50s of 1.2 nM (HIV-1 KK), 0.72 nM (HIV-1 CTV), 1.7 nM (HIV-1 HKW), 1.7 nM (HIV-1 HNK), 0.93 nM (HIV-1 HTN), and 0.55 nM (HIV-1 HHA), and EC90s of 12 nM (HIV-1 KK), 5 nM (HIV-1 CTV), 12 nM (HIV-1 HKW), 28 nM (HIV-1 HNK), 15 nM (HIV-1 HTN), and 4 nM (HIV-1 HHA) in PBMCs [1][2]. |
分子量 | 553.14 |
分子式 | C31H41ClN4O3 |
CAS No. | 333994-00-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (90.39 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.8079 mL | 9.0393 mL | 18.0786 mL | 45.1965 mL |
5 mM | 0.3616 mL | 1.8079 mL | 3.6157 mL | 9.0393 mL | |
10 mM | 0.1808 mL | 0.9039 mL | 1.8079 mL | 4.5197 mL | |
20 mM | 0.0904 mL | 0.452 mL | 0.9039 mL | 2.2598 mL | |
50 mM | 0.0362 mL | 0.1808 mL | 0.3616 mL | 0.9039 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
TAK-220 333994-00-6 Microbiology/Virology Proteases/Proteasome HIV Protease TAK 220 TAK220 Inhibitor inhibitor inhibit