Meglitinide is an ATP-sensitive potassium (KATP) channel inhibitor that selectively targets the SUR1, SUR2A, and SUR2B subunits. It exhibits IC50 values of 0.26 μM, 0.53 μM, and 1.6 μM for these channels, respectively, and demonstrates strong binding affinity with Kd values of 7 μM for SUR1 and SUR2A, and 8 μM for SUR2B. Meglitinide effectively closes KATP channels by binding to a shared site across all SUR subtypes, maintaining its efficacy even with the SUR1 S1237Y mutation. This compound is valuable for research applications centered on type 2 diabetes and the modulation of insulin secretion.
Meglitinide is an ATP-sensitive potassium (KATP) channel inhibitor that selectively targets the SUR1, SUR2A, and SUR2B subunits. It exhibits IC50 values of 0.26 μM, 0.53 μM, and 1.6 μM for these channels, respectively, and demonstrates strong binding affinity with Kd values of 7 μM for SUR1 and SUR2A, and 8 μM for SUR2B. Meglitinide effectively closes KATP channels by binding to a shared site across all SUR subtypes, maintaining its efficacy even with the SUR1 S1237Y mutation. This compound is valuable for research applications centered on type 2 diabetes and the modulation of insulin secretion.
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