生物活性 | |||
---|---|---|---|
描述 | AZD-2098 is a selective CCR4 receptor antagonist with pIC50 value of 7.8. It is a candidate drug for asthma indications. AZD-2098 inhibited the cellular responses mediated by the hCCR4 receptor with pIC50 values of 7.5, 6.3 and 6.3 for inhibition of CCL22 Ca2+ response (measured by MDC-induced Ca2+ flux in CHO cells transfected with the human CCR4 receptor), inhibition of Th2 cell CCL22 driven chemotaxis in 0.3% HAS (measured by MDC-induced chemotaxis) and inhibition of Th2 cell CCL17 driven chemotaxis in 0.3% HAS (measured by TARC-induced chemotaxis). Oral administration of AZD-2098 at dose>0.75µmol/kg 1 hour prior to antigen challenge (then every 12 hours thereafter prior to termination 96 hours post challenge) reduced alveolitis and leukocyte trafficking in the microvasculature of sensitized rats. |
实验方案 | |||
---|---|---|---|
1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.99mL 0.60mL 0.30mL |
14.96mL 2.99mL 1.50mL |
29.92mL 5.98mL 2.99mL |
参考文献 |
---|