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CAS No. | 1416799-28-4 | Cat. No. | BCP30858 |
Name | AMG-333 | ||
Synonyms | AMG 333; AMG333; | ||
SMILES | C1=CC(=C(N=C1)C(C2=CC(=C(C=C2)OC(F)(F)F)F)NC(=O)C3=NC=C(C=C3)C(=O)O)F | ||
Chemical Name | |||
Formula | C20H12F5N3O4 | M. Wt | 453.32 |
Purity | 98% | Storage | Store at 4-8°C |
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. |
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