产品
编 号：F303291
分子式：C9H10ClN3O2S2
分子量：291.78
分子式：C9H10ClN3O2S2
分子量：291.78
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 279215-43-9
产品详情
生物活性：
Tifenazoxide (NN414) is a potent, orally active and SUR1/Kir6.2 selective KATP channels opener. Tifenazoxide has antidiabetic effect, can inhibit glucose stimulated insulin release in vitro and in vivo, and has a beneficial effect on glucose homeostasis.
体内研究：
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.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.
体外研究：
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 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 (IC50 = 0.15 μM).
Tifenazoxide (NN414) is a potent, orally active and SUR1/Kir6.2 selective KATP channels opener. Tifenazoxide has antidiabetic effect, can inhibit glucose stimulated insulin release in vitro and in vivo, and has a beneficial effect on glucose homeostasis.
体内研究：
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.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.
体外研究：
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 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 (IC50 = 0.15 μM).
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