[CAS NO. 345303-91-5] AZD9056hydrochloride
PRODUCTS SPECIFICATIONS [345303-91-5]
DESCRIPTION [345303-91-5]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 455.46 |
| Molecular Formula | C24H36Cl2N2O2 |
| SMILES | O=C(C1=CC(CCCNCCCO)=CC=C1Cl)NCC2(C[C@H](C3)C4)C[C@H]4C[C@H]3C2.Cl |
1 Publications Citing Use of MCE
Summary
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 IC 50 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 (IC 50 =1-3 μM) in mouse microglia BV2 cells [1] . AZD9056 is an inhibitor of BCRP and weakly inhibits BCRP-mediated transport of methotrexate (IC 50 =92 μM) [2] .
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00908934 | AstraZeneca |
Healthy
|
May 2009 | Phase 1 |
| NCT00520572 | AstraZeneca |
Rheumatoid Arthritis
|
August 2007 | Phase 2 |
| NCT00736606 | AstraZeneca |
Healthy Volunteers
|
August 2008 | Phase 1 |
| NCT00920608 | AstraZeneca |
Rheumatoid Arthritis
|
May 2009 | Phase 1 |
| NCT00700986 | AstraZeneca |
Rheumatoid Arthritis
|
June 2008 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 50 mg/mL ( 109.78 mM ; Need ultrasonic)
H 2 O : 1.67 mg/mL ( 3.67 mM ; ultrasonic and warming and heat to 60°C)
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 |
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.
- [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.
- [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.