Englitazone (sodium)

Englitazone sodium is a thiazolidinedione compound. Englitazone sodium selectively activates PPARγ1 and PPARγ2. Englitazone sodium improves insulin sensitivity, induces adipogenesis in preadipocytes and mesenchymal stem cells, and inhibits the channel currents of Kir6.2-SUR1 and Kir6.2D26. Englitazone sodium is applicable to research related to non-insulin-dependent diabetes mellitus^[1][2]. In Vitro:Englitazone (1 nM-10 μM; duration of transfection assay) sodium activates both wild-type PPARγ1 and PPARγ2 subtypes in a dose-dependent manner in CV-1 cells in vitro^[1].
Englitazone sodium (10-100 μM; 15 min) inhibits Kir6.2-SUR1 K_ATP channel currents in azide-activated Xenopus oocytes, with an IC₅₀ of 93.6 μM^[2].
Englitazone (10-50 μM) sodium inhibits Kir6.2-SUR1 K_ATP channel activity in inside-out patches of Xenopus oocytes (without sodium azide), with an inhibition rate of 67.6% at 10 μM and 81.5% at 50 μM^[2].
Englitazone (10-50 μM) sodium inhibits the activity of azide-activated Kir6.2-SUR1 K_ATP channels in inside-out membrane patches of Xenopus oocytes, with an inhibition rate of 47.0% at 10 μM and 88.8% at 50 μM^[2].
Englitazone (10 μM) sodium inhibits Kir6.2Δ26-SUR1 K_ATP channel activity by 79.8% in inside-out membrane patches of HEK 293 cells, and this effect is independent of the SUR1 subunit^[2].
Englitazone (10 μM) sodium inhibits the activity of SUR1-null Kir6.2Δ26 K_ATP channels by 93.8% at a concentration of 10 μM in inside-out membrane patches of HEK 293 cells, confirming that its site of action is the Kir6.2 subunit^[2].