VU0810464

VU0810464 is a potent and selective non-ureaG protein-gated inwardly-rectifying potassium channels (GIRK, Kir3) activator. VU0810464 displays nanomolar potency for neuronal (EC50=165 nM) and GIRK1/4 (EC50=720 nM) channels with improved brain penetration[1][2].

Product Specifications

CAS Number

[2126040-21-7]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Potassium Channel

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/vu0810464.html

Purity

99.29

Solubility

DMSO : ≥ 250 mg/mL

Smiles

O=C(NC1=CC(C)=NN1C2CCCCC2)CC3=CC=C(F)C(Cl)=C3

Molecular Formula

C18H21ClFN3O

Molecular Weight

349.83

Precautions

H302, H315, H319, H335

References & Citations

[1]Vo BN, et al. VU0810464, a non-urea G protein-gated inwardly rectifying K+ (Kir 3/GIRK) channel activator, exhibits enhanced selectivity for neuronal Kir 3 channels and reduces stress-induced hyperthermia in mice.Br J Pharmacol. 2019 Jul;176 (13) :2238-2249.|[2]Wieting JM, et al. Discovery and Characterization of 1H-Pyrazol-5-yl-2-phenylacetamides as Novel, Non-Urea-Containing GIRK1/2 Potassium Channel Activators.ACS Chem Neurosci. 2017 Sep 20;8 (9) :1873-1879.