2017年12月3日星期日

AZD9056 hydrochloride|cas 345303-91-5

AZD9056 hydrochloride|cas 345303-91-5

DC Chemicals, Website: www.dcchemicals.com

Product Name: AZD9056 hydrochloride|Cas Number: 345303-91-5| Catalog Number: DC10425|Other Nmaes: AZD-9056 hydrochloride; AZD 9056 hydrochloride

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

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].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].

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