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A 804598
Axon 2182
CAS:
1125758-85-1
- Optical Purity: >99% e.e.
- Soluble in DMSO
- MF: C19H17N5
- MW: 315.37
Description
A 804598 is a potent and selective P2X7 receptor antagonist with reported IC50 values of 10, 9 and 11 nM for rat, mouse and human P2X7 receptors. It blocks agonist-stimulated IL-1β release, Yo-Pro uptake and BZ-ATP-stimulated calcium influx in relevant systems.
P2X7 is an ATP-gated ion channel involved in inflammasome activation, cytokine release, pain signaling and neuroinflammation. A 804598 is relevant for purinergic receptor pharmacology and localization studies in brain and spinal cord.
Key Features
- Potent P2X7 receptor antagonist
- Nanomolar activity across rat, mouse and human receptors
- Blocks IL-1β release and Yo-Pro uptake
- Useful purinergic neuroinflammation tool
Applications
- P2X7 receptor assays
- Inflammasome and cytokine studies
- Neuroinflammation and pain models
- Autoradiographic receptor localization research
More Information
| Parent CAS No. | 1125758-85-1 |
|---|---|
| Chemical Name | (S)-2-cyano-1-(1-phenylethyl)-3-(quinolin-5-yl)guanidine |
| SMILES | N(/C(/N[C@@H](C)C1C=CC=CC=1)=NC#N)C1C=CC=C2C=1C=CC=N2 |&1:3,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C19H17N5/c1-14(15-7-3-2-4-8-15)23-19(22-13-20)24-18-11-5-10-17-16(18)9-6-12-21-17/h2-12,14H,1H3,(H2,22,23,24)/t14-/m0/s1 |
| InChiKey | PQYCRDPLPKGSME-AWEZNQCLSA-N |
| CID | 53325874 |
| Short Description | P2X7 antagonist |
References
- D.L. Donnelly-Roberts et al. [3H]A-804598 ([3H]2-cyano-1-[(1S)-1-phenylethyl]-3-quinolin-5-ylguanidine) is a novel, potent, and selective antagonist radioligand for P2X7 receptors. Neuropharm. 2009, 56, 223–229.
- S.L. Able et al. Receptor localization, native tissue binding and ex vivo occupancy for centrally penetrant P2X7 antagonists in the rat. Br. J. Pharmacol. 2011, 162, 405–414.
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