| Identification | Back Directory | [Name]
5H-Pyrimido[4,5-e][1,4]diazepin-5-one, 2-amino-6,7,8,9-tetrahydro-9-methyl-6-[3-[(1S)-3-(methylamino)-1-(2-thienyl)propoxy]phenyl]- | [CAS]
2143586-17-6 | [Synonyms]
Cavα2δ1&NET-IN-2
5H-Pyrimido[4,5-e][1,4]diazepin-5-one, 2-amino-6,7,8,9-tetrahydro-9-methyl-6-[3-[(1S)-3-(methylamino)-1-(2-thienyl)propoxy]phenyl]- | [Molecular Formula]
C22H26N6O2S | [MOL File]
2143586-17-6.mol | [Molecular Weight]
438.55 |
| Hazard Information | Back Directory | [Uses]
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]. | [References]
[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. DOI:10.1021/acs.jmedchem.0c01867 |
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