| Stereochemistry | RACEMIC |
| Molecular Formula | C24H21N3O5S |
| Molecular Weight | 463.506 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
[O-][N+](=O)C1=CC(=CC=C1)C2=CC=C(OCC(CCC3=CC=NC=C3)N4C(=O)CSC4=O)C=C2
InChI
InChIKey=VQEHBLGYANQWEA-UHFFFAOYSA-N
InChI=1S/C24H21N3O5S/c28-23-16-33-24(29)26(23)21(7-4-17-10-12-25-13-11-17)15-32-22-8-5-18(6-9-22)19-2-1-3-20(14-19)27(30)31/h1-3,5-6,8-14,21H,4,7,15-16H2
| Molecular Formula | C24H21N3O5S |
| Molecular Weight | 463.506 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | RACEMIC |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Optical Activity | ( + / - ) |
AZ11645373 is a potent and selective antagonist of human P2X7, that was developed by Astra Pharmaceuticals Ltd for treatment pain. AZ11645373 Inhibits BzATP-mediated calcium influx and inhibits ATP-mediated IL-1β release in vitro. AZ11645373 in addition to its well-characterized ability to inhibit the pro-inflammatory action of ATP demonstrates a broad P2X7 receptor-independent anti-inflammatory activity against chemically different types of inflammatory agonists. This type of polypharmacology may be especially effective for treatment of inflammatory disorders due to a combination of P2X7-dependent and P2X7-independent anti-inflammatory mechanisms. In other words, AZ11645373 has a potential to induce several beneficial effects including inhibition of inflammasome-mediated generation of IL-1β and IL-18, inhibition of inflammatory pain.
Originator
Approval Year
PubMed
Patents
Sample Use Guides
Human umbilical vein endothelial cells were used for activity evaluation. Cells were preincubated with a solution of AZ11645373 in EBM-2/2% FCS/20 mM HEPES for 20 min followed by addition of OxPAPC (30 to 40 μg/ml) in the same medium. After incubation for 6 h at 37 °C, the medium was removed and RNAzol®RT (Molecular Research Center Inc.; Cincinnati, OH, USA) was added and total RNA was isolated. Concentrations of RNA were determined using a DS-11+Spectophotometer (DeNovix; Wilmington, DE, USA).
