| Description | VU0134992 is an Kir4.1 blocker with an IC50 value of 0.97 μM |
| In vitro | VU0134992 inhibits Kir4.1 with an IC50 value of 0.97 μM and is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50 = 9 μM) at -120 mV.?In thallium (Tl+) flux assays, 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 vivo | VU0134992 displayed a large free unbound fraction (fu) in rat plasma (fu = 0.213).?Consistent with the known role of Kir4.1 in renal function, oral dosing of VU0134992 led to a dose-dependent diuresis, natriuresis, and kaliuresis in rats. |
| Target activity | KIR4.1:0.97 µM |
| Synonyms | VU 0134992 |
| molecular weight | 411.38 |
| Molecular formula | C20H31BrN2O2 |
| CAS | 755002-90-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 60 mg/ml (145.85 mM) |
| 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. |