Tifenazoxide NN414|cas:279215-43-9|西域试剂

Tifenazoxide NN414,99.0%

产品编号：Bellancom-119322| CAS NO：279215-43-9| 分子式：C₉H₁₀ClN₃O₂S₂| 分子量：291.78

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-119322		￥4800.00	杭州北京（现货）
Bellancom-119322		￥7800.00	杭州北京（现货）

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Tifenazoxide NN414

产品介绍

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。

生物活性

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 homeostasis.

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).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

西域 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.

体内研究

西域 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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (342.72 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.4272 mL	17.1362 mL	34.2724 mL
5 mM	0.6854 mL	3.4272 mL	6.8545 mL
10 mM	0.3427 mL	1.7136 mL	3.4272 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (8.57 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.57 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (8.57 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.57 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (8.57 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.57 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。