CXCR4 antagonist 5 is a potent antagonist targeting the CXCR4 receptor, exhibiting an IC50 value of 8.8 nM. This compound effectively inhibits CXCL12-induced cytosolic calcium influx with an IC50 of 0.02 nM and blocks CXCR4/CXCL12-mediated chemotaxis. Additionally, CXCR4 antagonist 5 demonstrates favorable physicochemical properties along with a moderate safety profile in vitro, showing minimal inhibition of CYP isozymes and hERG channels.
CXCR4 antagonist 5 is a potent antagonist targeting the CXCR4 receptor, exhibiting an IC50 value of 8.8 nM. This compound effectively inhibits CXCL12-induced cytosolic calcium influx with an IC50 of 0.02 nM and blocks CXCR4/CXCL12-mediated chemotaxis. Additionally, CXCR4 antagonist 5 demonstrates favorable physicochemical properties along with a moderate safety profile in vitro, showing minimal inhibition of CYP isozymes and hERG channels.
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