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].

Product Specifications

CAS Number

[2143586-17-6]

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-2.html

Solubility

10 mM in DMSO

Smiles

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

Molecular Formula

C22H26N6O2S

Molecular Weight

438.55

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.