Uses
VU0134992 hydrochloride is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC50 of 0.97 μM. VU0134992 hydrochloride is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 μM) at -120 mV[1].
Biological Activity
VU0134992 is an orally available, potent and selective modulator of the inward rectifier potassium (Kir) channel Kir4.1 (KCNJ10) th at induces diuresis, natriuresis, and kaliuresis in rats.
in vivo
VU0134992 hydrochloride (50-100 mg/kg; oral gavage) statistically significantly increased urinary Na+ as well as K+ excretion[1].
| Animal Model: | Male Sprague-Dawley rats (250-300 g)[1] |
| Dosage: | Oral gavage |
| Administration: | 50 and 100 mg/kg |
| Result: | Statistically significantly increased urinary Na+ as well as K+ excretion.
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References
[1] Kharade SV, et al. Discovery, Characterization, and Effects on Renal Fluid and Electrolyte Excretion of the Kir4.1 Potassium Channel Pore Blocker, VU0134992. Mol Pharmacol. 2018 Aug;94(2):926-937. DOI:
10.1124/mol.118.112359
