MedChemExpress - Model AZD9056 hydrochloride -345303-91-5
AZD9056 hydrochloride is a selective orally active inhibitor of P2X7 which plays a significant role in inflammation and pain-causing diseases.MCE products for research use only. We do not sell to patients.
AZD9056 hydrochloride
MCE China：AZD9056 hydrochloride
Brand：MedChemExpress (MCE)
Cat. No.HY-19427A
CAS：345303-91-5
Purity：98.18%
Storage：4°C, sealed storage, away from moisture *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Shipping：Room temperature in continental US; may vary elsewhere.
Description：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].
Animal Administration：Rats: To reveal the molecular mechanisms of action of P2X7R in articular cartilage in OA-induced pain and inflammation, the antagonist of P2X7R AZD9056 is used. Wistar rats are administered (by intra-articular injection) monosodium iodoacetate (MIA), and the rats with OA are then treated with the P2X7R antagonist, AZD9056[3].
Cell Assay：AZD9056 is used as a stock solution in DMSO. Final DMSO concentrations in experiments does not exceed 1.0% (v/v). The effect of agonists on cell viability is assessed in parental HEK293 cells and HEK–hP2X7 cells using the CellTiter-Blue assay. For inhibition experiments, AZD9056 is added to the cells at concentrations up to 10 μmol/L 5 min prior to the addition of ATP (2.5 mM) or BzATP (0.25 mM). After incubation for 30 min at 37°C, an aliquot (20 μL) of the prewarmed CellTiter-Blue reagent is added. Samples are incubated for 1 h at 37°C. Fluorescence signals are measured[1].
IC50 & Target：P2X7 Receptor
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References：
[1]. Seeland S, et al. ATP-induced cellular stress and mitochondrial toxicity in cells expressing purinergic P2X7 receptor. Pharmacol Res Perspect. 2015 Mar;3(2):e00123. [Content Brief]
[2]. Elsby R, et al. In vitro risk assessment of AZD9056 perpetrating a transporter-mediated drug-drug interaction with methotrexate. Eur J Pharm Sci. 2011 May 18;43(1-2):41-9. [Content Brief]
[3]. Hu H, et al. Blocking of the P2X7 receptor inhibits the activation of the MMP-13 and NF-κB pathways in the cartilage tissue of rats with osteoarthritis. Int J Mol Med. 2016 Dec;38(6):1922-1932. [Content Brief]
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