Formulation: A solid
Formal Name: 2-[2-bromo-4-(1-methylethyl)phenoxy]-N-(2,2,6,6-tetramethyl-4-piperidinyl)-acetamide, hydrochloride
Purity: ≥95%
Formula Markup: C20H31BrN2O2 • XHCl
Formula Weight: 411,4
Shelf life (days): 1460
Notes: VU0134992 is an inhibitor of inward-rectifier potassium channel 4.1 (Kir4.1; IC50 = 5.2 µM in a thallium flux assay).{69304} It is selective for Kir4.1 over Kir2.3, Kir7.1, and SUR1/Kir6.2 (IC50s = 13.2, 34.2, and 11.4 µM, respectively), as well as Kir1.1, Kir2.1, and Kir2.2 at 30 µM, but also inhibits Kir4.2, heteromeric GIRK1/GIRK2, also known as Kir3.1/Kir3.2, and heteromeric GIRK1/GIRK4 (IC50s = 8.1, 2.5, and 3.1 µM, respectively). VU0134992 (5 µM) reduces polymyxin B-induced decreases in cell viability in HK-2 human kidney tubular cells and prevents polymyxin B-induced increases in apoptosis in mouse embryonic kidney explant cultures.{69305} In vivo, VU0134992 (50 and 100 mg/kg) increases urine volume and urinary sodium and potassium levels in rats.{69304}
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