VU0134992 (hydrochloride)

VU0134992 is an inhibitor of inward-rectifier potassium channel 4.1 (Kir4.1, IC50 = 5.2 µM in a thallium flux assay). 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. In vivo, VU0134992 (50 and 100 mg/kg) increases urine volume and urinary sodium and potassium levels in rats.Formal Name: 2-[2-bromo-4-(1-methylethyl)phenoxy]-N-(2,2,6,6-tetramethyl-4-piperidinyl)-acetamide, hydrochloride. Molecular Formula: C20H31BrN2O2 . XHCl. Formula Weight: 411.4. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMF: 2 mg/ml, DMSO: 1 mg/ml. SMILES: O=C(COC(C=CC(C(C)C)=C1)=C1Br)NC(CC2(C)C)CC(C)(N2)C.Cl. InChi Code: InChI=1S/C20H31BrN2O2.ClH/c1-13(2)14-7-8-17(16(21)9-14)25-12-18(24)22-15-10-19(3,4)23-20(5,6)11-15,/h7-9,13,15,23H,10-12H2,1-6H3,(H,22,24),1H. InChi Key: QXKQUPCNSXWIDX-UHFFFAOYSA-N.