Biological Activity |
AZD2098 is a potent and selective CC-chemokine receptor 4 (CCR4) inhibitor with pIC50s of 7.8, 8.0, 8.0 and 7.6 for human, rat, mouse and dog respectively, used for asthma research[1][2]. IC50 & Target: pIC50: 7.8 (hCCR4), 8.0 (rat CCR4), 8.0 (mouse CCR4), 7.6(dog CCR4)[1] In Vitro: AZD2098 potently inhibits chemokine-induced cellular responses, with pIC50 of 7.5 and 6.3 against CCL22-induced Ca2+ influx in hCCR4-expressing CHO cells and CCL17- or CCL22-induced chemotaxis of primary human Th2 cells respectively[1]. In Vivo: AZD2098 (0.22-7.5 umol/kg; p.o.; 1 hour before and every 12 hours after antigen challenge) exhibits efficacy against antigen-induced inflammatory response among ovalbumin-sensitized rats, and the changes are first visible at a dose of 0.22 umol/kg and maximal at 7.5 umol/kg[1]. |