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ZK 756326

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Chemical Structure| 874911-96-3 同义名 : ZK756326 2HCl
CAS号 : 874911-96-3
货号 : A592527
分子式 : C21H28N2O3
纯度 : 99%+
分子量 : 356.459
MDL号 : MFCD09038571
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
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].
实验方案
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
参考文献

[1]Haskell CA, et al. Identification and characterization of a potent, selective nonpeptide agonist of the CC chemokine receptor CCR8. Mol Pharmacol. 2006 Jan;69(1):309-16.