A non-peptide agonist of CCR8; inhibits binding of CCL1 to human CCR8 (IC50 = 1.8 µM); stimulates extracellular acidification in cells expressing human and mouse CCR8 (EC50s = 254 nM and 2.6 µM

ZK 756326 (hydrochloride) – 5 mg

Brand:
Cayman
CAS:
1780259-94-0
Storage:
-20
UN-No:
Non-Hazardous - /

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.{52082} 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.  

 

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Description

A non-peptide agonist of CCR8; inhibits binding of CCL1 to human CCR8 (IC50 = 1.8 µM); stimulates extracellular acidification in cells expressing human and mouse CCR8 (EC50s = 254 nM and 2.6 µM, respectively); exhibits >28-fold selectivity for CCR8 over 26 other GPCRs; binds to the serotonergic receptors 5-HT1A, 5-HT2B, 5-HT2C, and 5-HT5A (IC50s = 5.4, 4.4, 34.8, and 16 µM, respectively); induces Gαi-mediated calcium mobilization, 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

Synonyms: 

Molecular weight: 429.4

CAS: 1780259-94-0

Purity: ≥98%

Formulation: A crystalline solid

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