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VU0134992

  Cat. No.:  DC23646   Featured
Chemical Structure
755002-90-5
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More than 5000 active chemicals with high quality for research!
Field of application
VU0134992 (VU 0134992) is a potent, selective blocker of the inward rectifier potassium channel Kir4.1 (KCNJ10) with IC50 of 0.97 uM in whole-cell patch clamp electrophysiology assays; displays 9-fold selectivity for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 uM) at -120 mV; VU0134992 is greater than 30-fold selective for Kir4.1 over Kir1.1, Kir2.1, and Kir2.2, is weakly active toward Kir2.3, Kir6.2/SUR1, and Kir7.1, and is equally active toward Kir3.1/3.2, Kir3.1/3.4, and Kir4.2 in Tl+ flux assays; causes dose-dependent diuresis, natriuresis, and kaliuresis in rats after oral treatment; VU0134992 represents the first in vivo-active tool compound for probing the therapeutic potential of Kir4.1 as a novel diuretic target for the treatment of hypertension.
Cas No.: 755002-90-5
Chemical Name: 2-(2-Bromo-4-iso-propylphenoxy)-N-(2,2,6,6-tetramethylpiperidin-4-yl)acetamide
Synonyms: VU 0134992
SMILES: O=C(NC1CC(C)(C)NC(C)(C)C1)COC2=CC=C(C(C)C)C=C2Br
Formula: C20H31BrN2O2
M.Wt: 411.384
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: 1. Kharade SV, et al. Mol Pharmacol. 2018 Jun 12. pii: mol.118.112359.
Description: VU0134992 is a selective inward rectifier potassium (Kir) channel Kir4.1 blocker with an IC50 of 0.97 µM[1].
Target: IC50: 0.97 µM (Kir4.1)[1]
In Vitro: VU0134992 is greater than 30-fold selective for Kir4.1 over Kir1.1, Kir2.1, and Kir2.2, is weakly active toward Kir2.3, Kir6.2/SUR1, and Kir7.1, and is equally active toward Kir3.1/3.2, Kir3.1/3.4, and Kir4.2[1].
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.
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