A 839977
A-839977 is a novel and selective P2X7 antagonist. It blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors with IC50 values 20, 42 and 150 nM respectively. It also potently blocked agonist-evoked YO-PRO uptake and IL-1beta release from differentiated human THP-1 cells. It also produced robust antihyperalgesia in the CFA model of inflammatory pain in wild-type mice. It has been exhibited to reduce CFA-induced thermal hyperalgesia in a dose-dependent fashion with the ED50 value of 100μmol/kg.
| Supplier | BOC Sciences |
|---|---|
| Product # | 870061-27-1 |
| Pricing | Inquire |
| Cas | 870061-27-1 |
| Molecular Weight | 413.26 |
| Molecular Formula | C19H14Cl2N6O |
| Canonical SMILES | C1=CC=C(C(=C1)CNC2=NN=NN2C3=C(C(=CC=C3)Cl)Cl)OC4=CC=CC=N4 |