AZD9056 hydrochloride
Based on 6 publication(s) in Google Scholar
AZD9056 hydrochloride is a selective orally active inhibitor of P2X7 which plays a significant role in inflammation and pain-causing diseases.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.18%
- CAS. Nr.: 345303-91-5
- Formel: C24H36Cl2N2O2
- Molecular Weight:455.46
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Publications Citing Use of MedChemExpress (MCE) AZD9056 hydrochloride
More- Adv Sci (Weinh). 2025 Nov 6:e14842. [Abstract]
- ACS Appl Mater Interfaces. 2025 Feb 5;17(5):7521-7538. [Abstract]
- Front Immunol. 2021 Jan 8;11:602016. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2024 Jan;1870(1):166895. [Abstract]
- J Pharmacol Sci. 2020 Sep;144(1):43-51. [Abstract]
- Biochem Genet. 2025 Dec 6. [Abstract]
Alle P2X Receptor Isoform-spezifische Produkte anzeigen
More
Biologische Aktivität
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P2X7 Receptor |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
0.23 nM
Compound: 2; AZD9056
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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
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[PMID: 27427902] |
| J774.A1 | IC50 |
11.8 μM
Compound: 5, AZD9056
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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
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[PMID: 25597334] |
| MDA-MB-231 | IC50 |
8.699 μM
Compound: 2; AZD9056
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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
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[PMID: 27427902] |
| THP-1 | IC50 |
0.06 nM
Compound: 2; AZD9056
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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
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[PMID: 27427902] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 345303-91-5
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Appearance Solid
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Molecular Weight 455.46
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Formel C24H36Cl2N2O2
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Color White to off-white
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SMILES
O=C(C1=CC(CCCNCCCO)=CC=C1Cl)NCC2(C[C@H](C3)C4)C[C@H]4C[C@H]3C2.Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications (6)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
2025 Nov 6:e14842. PMID: 41195564 -
ACS Appl Mater Interfaces
The P2X7-Mediated Mitochondrial ROS as an Emerging Core Target of Tuftsin Nanoparticles in Severe Acute Pancreatitis Therapy via Regulating Mitophagy. [Abstract]2025 Feb 5;17(5):7521-7538. PMID: 39854589 -
Front Immunol
Stimulation of Vibratory Urticaria-Associated Adhesion-GPCR, EMR2/ADGRE2, Triggers the NLRP3 Inflammasome Activation Signal in Human Monocytes. [Abstract]2021 Jan 8;11:602016. PMID: 33488598 -
Biochim Biophys Acta Mol Basis Dis
Extracellular ATP (eATP) inhibits the progression of endometriosis and enhances the immune function of macrophages. [Abstract]2024 Jan;1870(1):166895. PMID: 37748566 -
J Pharmacol Sci
2020 Sep;144(1):43-51. PMID: 32653340 -
Biochem Genet
Network Pharmacology and Experimental Validation Reveal Wu Miao Pill's Therapeutic Effects on Acute Gouty Arthritis Through P2X7R Regulation. [Abstract]2025 Dec 6. PMID: 41351812
Lösungsmittel & Löslichkeit
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)
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protokoll
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (275 KB)
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SDS (557 KB)
- English - EN (557 KB)
- Français - FR (557 KB)
- Deutsch - DE (557 KB)
- Norwegian - NO (557 KB)
- Español - ES (557 KB)
- Swedish - SV (557 KB)
- Italian - IT (557 KB)
- Korean - KR (557 KB)
- Portuguese - PT (557 KB)
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Handling Instructions (2659 KB)
Verweise
[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
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.
| 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.
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