7-(4-tert-Butylbenzyl)-1,3-dimethyl-3,7-dihydro-1H-purine-2,6-dione

VU0071063 is a potent and selective activator of the inward-rectifier potassium channel (K_ir) 6.2 and sulfonylurea receptor (SUR) 1 (EC₅₀ = 7 μM using whole cell patch clamp electrophysiology). It is selective for SUR1-containing K_ir6.1 or K_ir6.2 channels over SUR2A, K_ir2.1, K_ir2.2, K_ir2.3, K_ir3.1/3/2, and voltage-gated potassium channel 2.1. VU0071063 inhibits glucose-stimulated calcium entry in isolated mouse pancreatic β-cells.

VU0071063 is a potent and specific Kir6.2/SUR1 opener (EC50=7.44 μM) and can be used for investigating Kir6.2/SUR1 expressed in the pancreas and brain. VU0071063 inhibits insulin secretion by inducing hyperpolarization of β-cell membrane potential. VU0071063 chemotype has a very steep structure-activity relationships[1][2].

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[1] Kharade SV, et al. Structure-Activity Relationships, Pharmacokinetics, and Pharmacodynamics of the Kir6.2/SUR1-Specific Channel Opener VU0071063. J Pharmacol Exp Ther. 2019;370(3):350-359. DOI:10.1124/jpet.119.257204
[2] Raphemot R, et al. Direct activation of β-cell KATP channels with a novel xanthine derivative. Mol Pharmacol. 2014;85(6):858-865. DOI:10.1124/mol.114.091884