Name | VU0134992 |
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. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 60 mg/ml (145.85 mM)
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Keywords | whole-cell | VU-0134992 | VU0134992 | selective | Potassium Channel | patch-clamp | oral | natriuresis | Kir4.1 | KcsA | kaliuresis | Inhibitor | inhibit | hypertension | electrophysiology | diuresis |
Inhibitors Related | Minoxidil sulfate | Quinine sulfate dihydrate | Hydrochlorothiazide | (±)-Naringenin | Tolbutamide | Tetraethylammonium bromide | Halothane | Butamben | Ursodeoxycholic acid | Cloperastine hydrochloride | Minoxidil | Indapamide |
Related Compound Libraries | Pain-Related Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Inhibitor Library | NO PAINS Compound Library | Orally Active Compound Library | Bioactive Compounds Library Max | Potassium Channel Targeted Library | Ion Channel Targeted Library | Anti-Cancer Compound Library |