Imeglimin (EMD 387008) Hydrochloride

Imeglimin (EMD 387008, IMEG, PXL 008, RVT-1501) Hydrochloride is a new class of oral glucose-lowering agents. Imeglimin normalizes glucose tolerance and insulin sensitivity by preserving mitochondrial function from oxidative stress and favoring lipid oxidation in liver of HFHSD mice.

Preincubation with Imeglimin (10 mM for 4 h or 100 μM for 24 h) fully prevents tert-butylhydroperoxide (tBH)-induced cell death.^{<a class="sref" href="#s_ref">[2]</a>}

Imeglimin normalizes glucose tolerance and insulin sensitivity by preserving mitochondrial function from oxidative stress and favoring lipid oxidation in liver of high-fat, high-sucrose diet (HFHSD) mice.^{<a class="sref" href="#s_ref">[1]</a>}

• Cell lines

  Human endothelial cells (HMEC-1)

• Concentrations

  100 μM, 10 mM

• Incubation Time

  24 h, 4 h

• Method

  HMEC-1 preincubated with or without Imeglimin (10 mM for 4 h or 100 μM for 24 h) or with CsA (1 μM for 30 min) are ished with PBS before subsequent exposure to 0.5 mM tBH in FBS-free culture medium for 45 min. Cells are then ished with PBS and incubated at 37 °C for 24 h in a complete MCDB medium. Alternatively, cells are exposed to 5.5 mM glucose (control cells) or to 33 mM glucose for 48 h. Cytotoxicity is evaluated with a double-stain system using the Annexin V-Fluoprobes 488 kit combined with propidium iodide.

• Animal Models

  16-week high-fat, high-sucrose diet (HFHSD) mice

• Dosages

  200 mg/kg

• Administration

  o.g.