COX-1-IN-5 (example 13, compound PS13) is a potent and selective COX-1 inhibitor ( COX-1 IC 50 = 1 nM, COX-2 IC 50 > 0.1 μM) exhibiting >1000-fold selectivity over COX-2 . COX-1-IN-5 possesses strong anti-inflammatory, antipyretic, analgesic, antithrombotic, anti-cancer activities. COX-1-IN-5 can be used for COX-mediated diseases research, such as inflammatory conditions and pain. COX-1-IN-5 radiolabeled with 11 C can be used as a selective PET tracer for whole‑body imaging of COX‑1 distribution and target engagement in vivo.
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