AZD9056 (hydrochloride)
CAS No. : 345303-91-5
| Size | Price | Stock |
|---|---|---|
| 5mg | $115 | In-stock |
| 10mg | $193 | In-stock |
| 25mg | $430 | In-stock |
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| Cat. No. : | HY-19427A |
| M.Wt: | 455.46 |
| Formula: | C24H36Cl2N2O2 |
| Purity: | >98 % |
| Solubility: | DMSO : 50 mg/mL (ultrasonic);H2O : 1.67 mg/mL (ultrasonic;warming;heat to 60°C) |
AZD9056 hydrochloride 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].
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