Description
AZD9056 hydrochloride is a selective orally active inhibitor of P2X7 which plays a significant role in inflammation and pain-causing diseases.
Product information
CAS Number: 345303-91-5
Molecular Weight: 455.46
Formula: C24H36Cl2N2O2
Chemical Name: 2-chloro-5-{3-[(3-hydroxypropyl)amino]propyl}-N-{[(3R,5S,7s)-adamantan-1-yl]methyl}benzamide hydrochloride
Smiles: Cl.OCCCNCCCC1C=C(C(=O)NCC23C[C@@H]4C[C@H](C2)C[C@H](C3)C4)C(Cl)=CC=1
InChiKey: LZBBHFRRZLDHLE-GRYNSXGKSA-N
InChi: InChI=1S/C24H35ClN2O2.ClH/c25-22-5-4-17(3-1-6-26-7-2-8-28)12-21(22)23(29)27-16-24-13-18-9-19(14-24)11-20(10-18)15-24;/h4-5,12,18-20,26,28H,1-3,6-11,13-16H2,(H,27,29);1H/t18-,19+,20-,24?;
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 50 mg/mL (109.78 mM; Need ultrasonic). H2O : 1.67 mg/mL (3.67 mM; ultrasonic and warming and heat to 60°C).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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. AZD9056 is an inhibitor of BCRP and weakly inhibits BCRP-mediated transport of methotrexate (IC50=92 μM).
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.
Products are for research use only. Not for human use.
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