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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 availablepotent and selective modulator of the inward rectifier potassium (Kir) channel Kir4.1 (KCNJ10) th at induces diuresisnatriuresisand 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 |
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