Powder: -20°C for 3 years | In solvent: -80°C for 1 year
ZK 756326 是一种选择性的非肽 CCR8 趋化因子受体激动剂(IC50:1.8 μM,在人体内;2.6 μM,在小鼠体内)。对 CCR4/5 和 CXCR3/4 没有活性,比其他 26 种 GPCR 的选择性高 28 倍(对 α2A 和 5-HT 受体的选择性较低)。诱导趋化性并抑制 Env 介导的 (HIV) 细胞-细胞融合。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 279 | 现货 | ||
2 mg | ¥ 393 | 现货 | ||
5 mg | ¥ 659 | 现货 | ||
10 mg | ¥ 1,120 | 现货 | ||
25 mg | ¥ 2,680 | 现货 | ||
50 mg | ¥ 3,970 | 现货 | ||
100 mg | ¥ 5,970 | 现货 |
产品描述 | ZK 756326 is a selective, non-peptide CCR8 chemokine receptor agonist (IC50: 1.8 μM, in human; 2.6 μM, in mouse). Displays no activity at CCR4/5 and CXCR3/4 and shows higher 28-fold selectivity over 26 other GPCRs (less selective at α2A and 5-HT receptors). Induces chemotaxis and inhibits Env-mediated (HIV) cell-cell fusion. |
靶点活性 | in CCR8(mouse):2.6 μM, CCR8(human):1.8 μM |
体外活性 | ZK 756326 stimulated extracellular acidification in cells expressing human CCR8. The ability of ZK 756326 to induce a response was receptor-specific and mediated through Gαi, because it could be blocked by treatment with pertussis toxin. Like CCL1, ZK 756326 inhibited human immunodeficiency virus (HIV) fusion of cells expressing CD4 and CCR8. But unlike mCCL1, ZK 756326 bound to and activated a form of mCCR8 that was mutated to eliminate O-linked sulfation at tyrosines 14 and 15. Therefore, ZK 756326 is most probably not binding in the same manner as CCL1 but can activate the switch mechanism involved in transducing signaling events[1]. |
细胞实验 | Cells are resuspended in RPMI with 1% (w/v) BSA and 25 mM HEPES, pH 7.4 (3 × 105 cells/well), and 100-μl aliquots were loaded into upper inserts. Samples of mCCL1 and ZK 756326 prepared in 600 μl of the same medium were placed in the lower wells. After incubation (2 h at 37°C), inserts were removed, and the migrated cells were counted in an EPICS XL flow cytometer. Duplicate wells were used for each point. A migration index was established as the ratio of the number of cells that had migrated in response to the chemokine or to ZK 756326 divided by the number of cells that had migrated in response to buffer alone. (Only for Reference) |
别名 | ZK756326 2HCl |
分子量 | 356.46 |
分子式 | C21H28N2O3 |
CAS No. | 874911-96-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 90.8 mM
H2O: 181.7 mM
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / H2O | 1 mM | 2.8054 mL | 14.0268 mL | 28.0536 mL | 70.1341 mL |
5 mM | 0.5611 mL | 2.8054 mL | 5.6107 mL | 14.0268 mL | |
10 mM | 0.2805 mL | 1.4027 mL | 2.8054 mL | 7.0134 mL | |
20 mM | 0.1403 mL | 0.7013 mL | 1.4027 mL | 3.5067 mL | |
50 mM | 0.0561 mL | 0.2805 mL | 0.5611 mL | 1.4027 mL | |
H2O | 100 mM | 0.0281 mL | 0.1403 mL | 0.2805 mL | 0.7013 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。
ZK 756326 874911-96-3 Immunology/Inflammation Microbiology/Virology CCR ZK756326 2HCl ZK-756326 ZK756326 Inhibitor inhibitor inhibit