Cavα2δ1&NET-IN-2

Cavα2δ1&NET-IN-2 (Compound 45CS) is a dual inhibitor of the α2δ‑1 subunit of voltage-gated calcium channels (Cavα2δ-1) and the norepinephrine transporter (NET). Cavα2δ1&NET-IN-2 inhibits Cavα2δ-1 with a Ki of 454 nM. Cavα2δ1&NET-IN-2 inhibits NET with a Ki of 59 nM and IC50 of 7 nM. Cavα2δ1&NET-IN-2 can be used for research of pain[1].

Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Membrane Transporter/Ion Channel >> Monoamine Transporter

Cavα2δ1: 112 nM (Ki); NET: 383 nM (Ki), 67 nM (IC50).

[1]. Díaz JL, et al. Bicyclic Diazepinones as Dual Ligands of the α2δ-1 Subunit of Voltage-Gated Calcium Channels and the Norepinephrine Transporter. J Med Chem. 2021 Feb 25;64(4):2167-2185.