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VU6036720 is an inhibitor of heteromeric inward-rectifier potassium channels (Kir) composed of Kir4.1 and Kir5.1 subunits (IC50 = 0.24 µM).1 It is selective for Kir4.1/5.1 channels over a variety of homomeric Kir channels, including Kir4.1 (IC50 = >10 µM), as well as heteromeric Kir3.1/3.2, Kir3.1/3.4, Kir6.2/SUR1, and Kir6.1/SUR2b channels at 30 µM but does inhibit the voltage-gated potassium channel Kv11.1, also known as human ether-a-go-go (hERG; IC50 = 6.4 µM). VU6036720 (30 and 100 mg/kg) does not inhibit diuresis in mice due to low oral bioavailability and high hepatic clearance.
WARNING This product is not for human or veterinary use.
1. VU6036720: The first potent and selective in vitro inhibitor of heteromeric Kir4.1/5.1 inward rectifier potassium channels. Mol. Pharmacol. 101(5), 357-370 (2022).