VU0810464 | Kir3 activator

VU0810464 chemical structure Focus Biomolecules

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VU0810464 (2126040-21-7) is a potent (Kir3.1/3.2; GIRK1/2 EC50 = 165 nM) activator of G protein-gated inwardly-rectifying potassium channels (Kir3; GIRK).1,2 Displays selectivity for Kir3.1/3.2 versus Kir3.1/3.4 as well as selectivity for neuronal versus cardiac Kir3 channels. VU0810464 reduced stress-induced hyperthermia but not anxiety-related behavior in mice.

References/Citations:

  1. Wieting et al. (2017), Discovery and Characterization of 1H-Pyrazol-5-yl-2-phenylacetamides as Novel, Non-Urea-Containing GIRK1/2 Potassium Channel Activators; ACS Chem. Neurosci. 8 1873
  2. Vo et al. (2019), VU0810464, a non-urea G-protein-gated inwardly rectifying K+ (Kir3/GIRK) channel activator, exhibits enhanced selectivity for neuronal Kir 3 channels and reduces stress-induced hyperthermia in mice; Br. J. Pharmacol. 176 2238
2126040-21-7, GIRK activator, Kir3 activator, VU-0810464, VU0810464, VU0810464 supplier

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VU0810464 (2126040-21-7) is a potent (Kir3.1/3.2; GIRK1/2 EC50 = 165 nM) activator of G protein-gated inwardly-rectifying potassium channels (Kir3; GIRK).1,2 Displays selectivity for Kir3.1/3.2 versus Kir3.1/3.4 as well as selectivity for neuronal versus cardiac Kir3 channels. VU0810464 reduced stress-induced hyperthermia but not anxiety-related behavior in mice.

References/Citations:

  1. Wieting et al. (2017), Discovery and Characterization of 1H-Pyrazol-5-yl-2-phenylacetamides as Novel, Non-Urea-Containing GIRK1/2 Potassium Channel Activators; ACS Chem. Neurosci. 8 1873
  2. Vo et al. (2019), VU0810464, a non-urea G-protein-gated inwardly rectifying K+ (Kir3/GIRK) channel activator, exhibits enhanced selectivity for neuronal Kir 3 channels and reduces stress-induced hyperthermia in mice; Br. J. Pharmacol. 176 2238

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