AZD9056 hydrochloride

Name: AZD9056 hydrochloride
Brand: MedChemExpress
SKU: HY-19427A
Rating: 5.0 (2 reviews)

Cat. No.: HY-19427A Purity: 98.82%: FAQs
Data Sheet SDS COA Handling Instructions

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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

CAS No. : 345303-91-5

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 127	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 127	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 115	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 193	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 430	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 720	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1220	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of AZD9056 hydrochloride:

AZD9056 Get quote

2 Publications Citing Use of MCE AZD9056 hydrochloride

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P2X1 Receptor P2X2 Receptor P2X3 Receptor P2X4 Receptor P2X7 Receptor

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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

IC₅₀ & Target

P2X7 Receptor

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.23 nM Compound: 2; AZD9056	Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced EtBr uptake measured after 2 hrs by fluorescence analysis Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced EtBr uptake measured after 2 hrs by fluorescence analysis	[PMID: 27427902]
J774.A1	IC₅₀	11.8 μM Compound: 5, AZD9056	Antagonist activity at P2X7 receptor in LPS-primed mouse J774.A1 cells assessed as inhibition of ATP-induced IL-1beta release after 30 mins by ELISA Antagonist activity at P2X7 receptor in LPS-primed mouse J774.A1 cells assessed as inhibition of ATP-induced IL-1beta release after 30 mins by ELISA	[PMID: 25597334]
MDA-MB-231	IC₅₀	8.699 μM Compound: 2; AZD9056	Antiinvasive activity against human MDA-MB-231 cells measured after 48 hrs by transwell invasion assay Antiinvasive activity against human MDA-MB-231 cells measured after 48 hrs by transwell invasion assay	[PMID: 27427902]
THP-1	IC₅₀	0.06 nM Compound: 2; AZD9056	Antagonist activity at human P2X7 receptor in LPS/IFN-gamma-differentiated human THP-1 cells assessed as suppression of BzATP-stimulated IL-1beta release per-incubated for 30 mins before BzATP addition and measured after 30 mins by ELISA Antagonist activity at human P2X7 receptor in LPS/IFN-gamma-differentiated human THP-1 cells assessed as suppression of BzATP-stimulated IL-1beta release per-incubated for 30 mins before BzATP addition and measured after 30 mins by ELISA	[PMID: 27427902]

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].

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

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].

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

Clinical Trial

Molecular Weight

455.46

Formula

C₂₄H₃₆Cl₂N₂O₂

CAS No.

345303-91-5

Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (109.78 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 1.67 mg/mL (3.67 mM; ultrasonic and warming and heat to 60°C)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.49 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.49 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.49 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.82%

Select Batch:

Data Sheet (275 KB) SDS (251 KB)

COA (246 KB) LCMS (256 KB)

Handling Instructions (2659 KB)

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]

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	[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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	2.1956 mL	10.9779 mL	21.9558 mL	54.8896 mL
DMSO	5 mM	0.4391 mL	2.1956 mL	4.3912 mL	10.9779 mL
	10 mM	0.2196 mL	1.0978 mL	2.1956 mL	5.4890 mL
	15 mM	0.1464 mL	0.7319 mL	1.4637 mL	3.6593 mL
	20 mM	0.1098 mL	0.5489 mL	1.0978 mL	2.7445 mL
	25 mM	0.0878 mL	0.4391 mL	0.8782 mL	2.1956 mL
	30 mM	0.0732 mL	0.3659 mL	0.7319 mL	1.8297 mL
	40 mM	0.0549 mL	0.2744 mL	0.5489 mL	1.3722 mL
	50 mM	0.0439 mL	0.2196 mL	0.4391 mL	1.0978 mL
	60 mM	0.0366 mL	0.1830 mL	0.3659 mL	0.9148 mL
	80 mM	0.0274 mL	0.1372 mL	0.2744 mL	0.6861 mL
	100 mM	0.0220 mL	0.1098 mL	0.2196 mL	0.5489 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.