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ZK-756326 dihydrochloride is a potent, selective and non-peptide CCR8 chemokine receptor agonist. ZK756326 dihydrochloride inhibited the binding of the CCR8 ligand I-309 (CCL1), with an IC(50) value of 1.8 muM. ZK-756326 2HCl was a full agonist of CCR8, dose-responsively eliciting an increase in intracellular calcium and cross-desensitizing the response of the receptor to CCL1. 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.
| Molecular Weight | 429.38 |
| Formula | C21H30Cl2N2O3 |
| CAS Number | 1780259-94-0 |
| Solubility (25°C) | Water 25 mg/mL DMSO 15 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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