1. Membrane Transporter/Ion Channel
  2. P2X Receptor
  3. AZD9056 hydrochloride

AZD9056 hydrochloride 

Cat. No.: HY-19427A Purity: 98.16%
Handling Instructions

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

For research use only. We do not sell to patients.

AZD9056 hydrochloride Chemical Structure

AZD9056 hydrochloride Chemical Structure

CAS No. : 345303-91-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 397 In-stock
Estimated Time of Arrival: December 31
1 mg USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 396 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

Clinical Trial
Molecular Weight

455.46

Formula

C₂₄H₃₆Cl₂N₂O₂

CAS No.

345303-91-5

SMILES

O=C(C1=CC(CCCNCCCO)=CC=C1Cl)NCC2(C[[email protected]](C3)C4)C[[email protected]]4C[[email protected]]3C2.Cl

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 34 mg/mL (74.65 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1956 mL 10.9779 mL 21.9558 mL
5 mM 0.4391 mL 2.1956 mL 4.3912 mL
10 mM 0.2196 mL 1.0978 mL 2.1956 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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AZD9056 hydrochloride
Cat. No.:
HY-19427A
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