Tifenazoxide (C09-1183-433)

Tifenazoxide (NN414) is a potent, orally active and SUR1/Kir6.2 selective K ATP channels opener. Tifenazoxide has antidiabetic effect, can inhibit glucose stimulated insulin release in vitro and in vivo, and has a beneficial effect on glucose homeostasisIn VitroTifenazoxide (NN414) hyperpolarises βTC3 cell membranes, and inhibits insulin release from βTC6, from isolated rat islets and from human islets at least a 100-fold more potent than Diazoxide. The EC 50 values for Tifenazoxide and diazoxide are 0.45 and 31 µM, respectively in the patch-clamp assay. Tifenazoxide (100 µM) activates Kir6.2/SUR1 channels, but not Kir6.2/SUR2A or Kir6.2/SUR2 channels, expressed in Xenopus oocytes both in whole-cell and inside-out macropatch recordings. Tifenazoxide is a potent inhibitor of glucose stimulated insulin release from βTC6 cells (IC 50 = 0.15 µM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoTifenazoxide (NN414; 1.5 mg/kg; oral administration; twice daily; for 3 weeks; male VDF Zucker ( fa/fa ) rat) treatment for 3 weeks in VDF rats reduces basal hyperglycemia, improves glucose tolerance, and reduces hyperinsulinemia during an oral glucose tolerance test (OGTT) and improves insulin secretory responsiveness ex vivo . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Vancouver diabetic fatty (VDF) Zucker rat Dosage: 1.5 mg/kg Administration: Oral administration; twice daily; for 3 weeks Result: Basal glucose was significantly reduced with the fall averaging 0.64 mM after 3 weeks of treatment.IC50& Target:K ATP channels. Specifications and Purity: 10mM in DMSO. Molecular Formula: C9H10ClN3O2S2. Molecular Weight: 291.78.