tcsc6172 AZD9056 (hydrochloride)

AZD9056 is a selective orally active inhibitor of P2X7 which plays a significant role in inflammation and pain-causing diseases.

In Vitro: The antagonist AZD9056 blocks P2X7 receptors with an IC₅₀ of 11.2 nM in HEK-hP2X7 cell line, indicating a high selectivity of the antagonist for the P2X7 receptor. The P2X7-receptor antagonist AZD9056 has a clear inhibitory effect (IC₅₀=1-3 μM) in mouse microglia BV2 cells^[1]. AZD9056 is an inhibitor of BCRP and weakly inhibits BCRP-mediated transport of methotrexate (IC₅₀=92 μM)^[2].

In Vivo: Treatment with AZD9056 exerts pain-relieving and anti-inflammatory effects. The upregulated expression of interleukin (IL)-1β, IL-6, tumor necrosis factor-α (TNF-α), matrix metalloproteinase-13 (MMP-13), substance P (SP) and prostaglandin E2 (PGE2) which is induced by MIA in cartilage tissues is reversed by AZD9056^[3].