ZK 756326 (hydrochloride)

A non-peptide agonist of CCR8

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库存: 现货

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数量
5mg

￥950.00

760.00

- +
10mg

￥1350.00

1080.00

- +
25mg

￥2950.00

2360.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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Background

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.

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