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Tifenazoxide

目录号: PL09956 纯度: ≥99.0%

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。

CAS No. :279215-43-9

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中文名称	Tifenazoxide
英文名称	Tifenazoxide
英文别名	2H-Thieno[3,2-e]-1,2,4-thiadiazin-3-amine,6-chloro-N-(1-methylcyclopropyl)-, 1,1-dioxide;2H-Thieno(3,2-E)-1,2,4-thiadiazin-3-amine, 6-chloro-N-(1-methylcyclopropyl)-, 1,1-dioxide;6-chloro-N-(1-methylcyclopropyl)-4H-thieno[3,2-e][1,2,4]thiadiazin-3-amine 1,1-dioxide;NN-414;Tifenazoxide;6-Chloro-3-[[1-methylcyclopropyl]amino]-4H-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide
Cas No.	279215-43-9
分子式	C₉H₁₀N₃O₂S₂Cl
分子量	291.78
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	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。

产品详情

生物活性

Tifenazoxide (NN414) is a potent, orally active and SUR1/Kir6.2 selective K 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.

性状

Solid

IC50 & Target[1][2]

K channels

体外研究(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 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). has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Carr RD, et al. NN414, a SUR1/Kir6.2-selective potassium channel opener, reduces blood glucose and improves glucose tolerance in the VDF Zucker rat. Diabetes. 2003 Oct;52(10):2513-8.
[2]. Hansen JB. Towards selective Kir6.2/SUR1 potassium channel openers, medicinal chemistry and therapeutic perspectives. Curr Med Chem. 2006;13(4):361-76.

溶解度数据	In Vitro: DMSO : 100 mg/mL (342.72 mM; Need ultrasonic)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Tifenazoxide

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