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Tifenazoxide

CAS No. : 279215-43-9

MCE 站：Tifenazoxide

产品活性：Tifenazoxide (NN414) 是一种有效的，口服活性的 SUR1/Kir6.2 选择性 K^ATP 通道开放剂。Tifenazoxide 具有抗糖尿病作用，可以抑制葡萄糖刺激的胰岛素在体内和体外的释放，并对葡萄糖稳态具有有益作用。

研究领域：Membrane Transporter/Ion Channel

作用靶点：Potassium Channel

In Vitro: Tifenazoxide (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 EC₅₀ values for Tifenazoxide and diazoxide are 0.45 and 31 ?M, respectively in the patch-clamp assay. Tifenazoxide (100 ?M) 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 (IC₅₀ = 0.15 ?M).

In Vivo: Tifenazoxide (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.

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