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ZK-756326 dihydrochloride

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ZK-756326 dihydrochloride
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Cat #: V28513 CAS #: 1780259-94-0 Purity ≥ 99%

Description: ZK-756326 is a novel, selective, potent and non-peptide agonist of CCR8 chemokine receptor with an IC(50) value of 1.8 muM.

References: 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.

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Molecular Weight (MW)429.38
Molecular FormulaC21H30Cl2N2O3
CAS No.1780259-94-0
ProtocolIn VitroZK 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
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.3289 mL11.6447 mL23.2894 mL46.5788 mL
5mM0.4658 mL2.3289 mL4.6579 mL9.3158 mL
10mM0.2329 mL1.1645 mL2.3289 mL4.6579 mL
20mM0.1164 mL0.5822 mL1.1645 mL2.3289 mL
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%DMSO + % + %Tween 80 + %ddH2O

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Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
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