ZK 756326是一种 CCR8(趋化因子受体 8)激动剂,IC50 为 1.8 μM,能够剂量依赖性增加细胞内钙浓度,并交叉脱敏 CCR8 对 CCL1 的反应。
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产品名称 | CXCR1 ↓ ↑ | CXCR2 ↓ ↑ | CXCR4 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Reparixin | ✔ | 99%+ | |||||||||||||||||
SB225002 |
+++
CXCR2, IC50: 22 nM |
99%+ | |||||||||||||||||
Plerixafor |
++
CXCR4, IC50: 44 nM |
99% | |||||||||||||||||
AMD 3465 6HBr | ✔ | 98% | |||||||||||||||||
WZ811 |
++++
CXCR4, EC50: 0.3 nM |
99% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | ZK 756326 effectively blocks the attachment of the CCL1, with an IC50 of 1.8 μM. It acts as a complete agonist for CCR8, inducing a dose-dependent rise in intracellular calcium and diminishing the receptor's responsiveness to CCL1. ZK 756326 also prompts extracellular acidification in cells that express human CCR8. To assess the specificity of ZK 756326 for CCR8, binding competition assays are conducted on a range of other G-protein-coupled receptors. In these tests, ZK 756326, at a concentration of 50 μM, demonstrates more than 28-fold specificity for CCR8 over 26 other GPCRs, which all show IC50 values above 50 μM. However, ZK 756326 exhibits less specificity against serotonergic receptors 5-HT1A, 5-HT2B, 5-HT2C, 5-HT5A, 5-HT6, and the adrenergic receptor α2A, with respective IC50 values of 5.4, 4.4, 34.8, 16, 5.9, and less than 20 μM (with 65% inhibition at 20 μM). Given that ZK 756326 displays no agonist activity at concentrations up to 10 μM on 5-HT1A in a GTPγS binding assay, it is unlikely to act as an agonist on these biogenic amine receptors[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.81mL 0.56mL 0.28mL |
14.03mL 2.81mL 1.40mL |
28.05mL 5.61mL 2.81mL |
CAS号 | 874911-96-3 |
分子式 | C21H28N2O3 |
分子量 | 356.459 |
别名 | ZK756326 2HCl |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 |
溶解方案 | |
动物实验配方 |