ZK 756326

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ZK 756326 是一种选择性非肽 CCR8 趋化因子受体激动剂（IC50：1.8 μM，人；2.6 μM，小鼠）。

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.

ZK 756326 inhibits the binding of the CCR8 ligand I-309 (CCL1), with an IC50 value of 1.8 μM. ZK 756326 is a full agonist of CCR8, dose-responsively eliciting an increase in intracellular calcium and cross-desensitizing the response of the receptor to CCL1. ZK 756326 stimulates extracellular acidification in cells expressing human CCR8. Binding competition assays are performed on a series of other G-protein-coupled receptors to determine whether the interaction of ZK 756326 is specific for CCR8. In these assays, ZK 756326 is tested at 50 μM for inhibition of radiolabeled ligand binding. At this concentration, ZK 756326 shows >28 fold specificity for CCR8 compared with 26 other GPCRs, all with IC50 values of >50 μM. There is less selectivity when ZK 756326 is tested against the serotonergic receptors 5-HT1A, 5-HT2B, 5-HT2C, 5-HT5A, 5-HT6, and the adrenergic receptor α2A, in which IC50 values of 5.4, 4,4, 34.8, 16, 5.9, and <20 μM (at 20 μM 65% inhibition), respectively, are observed. The compound is unlikely to be an agonist on these biogenic amine receptors, because when tested at concentrations up to 10 μM on a representative receptor, 5-HT1A, it shows no agonist activity in a GTPγS binding assay.

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Cell Cycle/DNA Damage

GPR

CCR8

Others-Field

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874911-96-3

429.38

C21H28N2O3·2HCl

>98% (HPLC)

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C1CN(CCN1CCOCCO)CC2=CC(=CC=C2)OC3=CC=CC=C3.Cl.Cl

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(-20℃)

With Ice Pack

≥ 2 years