A non-peptide agonist of CCR8
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ZK 756326 (hydrochloride)

Item No. 28454

Technical Information
Formal Name
2-[2-[4-[(3-phenoxyphenyl)methyl]-1-piperazinyl]ethoxy]-ethanol, dihydrochloride
CAS Number
1780259-94-0
Molecular Formula
C21H28N2O3 • 2HCl
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
PBS (pH 7.2): 10 mg/ml
SMILES
OCCOCCN(CC1)CCN1CC2=CC=CC(OC3=CC=CC=C3)=C2.Cl.Cl
InChi Code
InChI=1S/C21H28N2O3.2ClH/c24-14-16-25-15-13-22-9-11-23(12-10-22)18-19-5-4-8-21(17-19)26-20-6-2-1-3-7-20;;/h1-8,17,24H,9-16,18H2;2*1H
InChi Key
MPACCEKWFGWZHS-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    ZK 756326 is a non-peptide agonist of the CC chemokine receptor CCR8. It inhibits binding of CCL1 to human CCR8 (IC50 = 1.8 µM) and induces Gai-mediated calcium-mobilization in U87 cells expressing the receptor.1 It exhibits greater than 28-fold selectivity for CCR8 over 26 other GPCRs but also binds to the serotonin (5-HT) receptor subtypes 5-HT1A, 5-HT2B, 5-HT2C, and 5-HT5A with IC50 values of 5.4, 4.4, 34.8, and 16 µM, respectively. ZK 756326 stimulates extracellular acidification in cells expressing human and mouse CCR8 (EC50s = 254 nM and 2.6 µM, respectively). ZK 756326 induces ERK phosphorylation, exhibits leukocyte chemotactic activity, and inhibits HIV fusion of cells expressing CD4 and CCR8.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Haskell, C.A., Horuk, R., Liang, M., et alIdentification and characterization of a potent, selective nonpeptide agonist of the CC chemokine receptor CCR8. Mol. Pharmacol. 69(1), 309-316 (2005).