VU0134992(hydrochloride)

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VU0134992(hydrochloride) Basic information
Product Name:VU0134992(hydrochloride)
Synonyms:VU0134992(hydrochloride);VU0134992,oral,hypertension,patch-clamp,electrophysiology,Kir4.1,VU 0134992,Inhibitor,natriuresis,inhibit,VU-0134992 hydrochloride,whole-cell,selective,kaliuresis,VU0134992 hydrochloride,Potassium Channel,KcsA,VU-0134992,diuresis;2-(2-Bromo-4-isopropylphenoxy)-N-(2,2,6,6-tetramethylpiperidin-4-yl)acetamide hydrochloride;VU0134992 hydrochloride, 10 mM in DMSO;VU0134992 Hcl
CAS:1052515-91-9
MF:C20H32BrClN2O2
MW:447.84
EINECS:
Product Categories:
Mol File:1052515-91-9.mol
VU0134992(hydrochloride) Structure
VU0134992(hydrochloride) Chemical Properties
storage temp. under inert gas (nitrogen or Argon) at 2-8°C
solubility DMSO: 2mg/mL, clear
form Solid
color White to off-white
InChIKeyQXKQUPCNSXWIDX-UHFFFAOYSA-N
SMILESCC(C)C1=CC(Br)=C(OCC(NC2CC(C)(C)NC(C)(C)C2)=O)C=C1.Cl
Safety Information
WGK Germany WGK 3
Storage Class11 - Combustible Solids
MSDS Information
VU0134992(hydrochloride) Usage And Synthesis
UsesVU0134992 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 ActivityVU0134992 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.
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
VU0134992(hydrochloride) Preparation Products And Raw materials
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