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AZD9056 hydrochloride

CAS No. : 345303-91-5

MCE 国际站：AZD9056 hydrochloride

产品活性：AZD9056 hydrochloride 是具有口服活性的P2X7选择性抑制剂，其在炎症和引起疼痛的疾病中起重要作用。

研究领域：Membrane Transporter/Ion Channel

作用靶点：P2X Receptor

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. AZD9056 is an inhibitor of BCRP and weakly inhibits BCRP-mediated transport of methotrexate (IC₅₀=92 μM).

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.

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