TRPV1 antagonist CX-3 is a first-in-class highly selective TRPV1 antagonist with an IC50 value of 26.2 nM. CX-3 exhibited equivalent TRPV1 antagonistic activity with classical TRPV1 antagonist BCTC in vitro, and exerted better analgesic activity in vivo than that of BCTC in the formalin induced inflammatory pain model without hyperthermia risk. Moreover, CX-3 exhibited robust glucose-lowering effects and showed high selectivity over other ion channels.

Keywords: TRPV1 antagonist CX-3 | Supplier | TRPV1 antagonist | CX3 | CX 3 | CAS [2998942-96-2] | Non Selective (Cations) | TRPV1 | Antagonist | Ion Channels | Analgesia | Hypoglycemia | Diabetes | Neuropathic pain