Cavα2δ1&NET-IN-1

Cavα2δ1&NET-IN-1 (Compound 59S) is a dual inhibitor of the α2δ‑1 subunit of voltage-gated calcium channels (Cavα2δ-1) and the norepinephrine transporter (NET) . Cavα2δ1&NET-IN-1 inhibits Cavα2δ-1 with a Ki of 112 nM. Cavα2δ1&NET-IN-1 inhibits NET with a Ki of 383 nM and IC50 of 67 nM. Cavα2δ1&NET-IN-1 can be used for research of pain[1].

Product Specifications

CAS Number

[2314361-39-0]

UNSPSC

12352005

Target

Calcium Channel; Monoamine Transporter

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/cavα2δ1-net-in-1.html

Solubility

10 mM in DMSO

Smiles

O=C1N(CCN(C2=NC=CC=C21)C)C3=CC(O[C@H](C4=CC=CS4)CCNC)=CC=C3

Molecular Formula

C23H26N4O2S

Molecular Weight

422.54

References & Citations

[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.