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Chemical Structure : VU0134992
CAS No.: 755002-90-5
Catalog No.: PC-35211Not For Human Use, Lab Use Only.
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.
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|---|---|---|---|
| 10 mg | $108 | In stock | |
| 25 mg | $178 | In stock | |
| 50 mg | $288 | In stock | |
| 100 mg | Get quote |
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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.
VU0134992 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.
VU0134992 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.
| M.Wt | 411.384 | |
| Formula | C20H31BrN2O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
DMSO: 259 mg/mL. H2O: <2 mg/mL. |
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| Chemical Name/SMILES |
2-(2-Bromo-4-iso-propylphenoxy)-N-(2,2,6,6-tetramethylpiperidin-4-yl)acetamide |
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1. Kharade SV, et al. Mol Pharmacol. 2018 Jun 12. pii: mol.118.112359.
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