AMG-333
| CAS No. | 1416799-28-4 | Cat. No. | BCP30858 |
| Name | AMG-333 | ||
| Synonyms | AMG 333; AMG333; | ||
| Formula | C20H12F5N3O4 | M. Wt | 453.32 |
| Description | AMG-333 is a potent and selective TRPM8 Antagonist for the Treatment of Migraine with IC50 of 13 nM and 20 nM for hTRPM8 and rTRPM8, respectively. In vitro toxicology profiling showed that AMG-333 was selective over several other TRP channels (IC50 TRPV1, V3, V4 > 20 μM; TRPA1 > 40 μM) and had no hits in off-target-activity panels (CEREP, 144 targets at 10 μM, POC > 45%; Ambit kinase, 100 at 1 μM, POC > 50%). AMG-333 was well-tolerated in 28 day rat and dog preclinical safety studies and advanced to Phase 1 human clinical trials. | ||
| Pathways | Ion Channel/Membrane Transporter | ||
| Targets | TRP Channel | ||
Structure
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