ZK 756326 (hydrochloride)

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. 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.Formal Name: 2-[2-[4-[(3-phenoxyphenyl)methyl]-1-piperazinyl]ethoxy]-ethanol, dihydrochloride. CAS Number: 1780259-94-0. Molecular Formula: C21H28N2O3 . 2HCl. Formula Weight: 429.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: 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.