Tifenazoxide  ≥98%

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包装规格:5mg in glass bottle
产品描述:基本信息 产品编号: T11138 产品名称: Tifenazoxide CAS: 279215-43-9   储存条件 粉末 -20℃ 四年     分子式: C9H10ClN3O2S2 溶于液体 -80℃ 6个月 分子量: 291.78 -20℃ 1个月 化学名:  6-Chloro-3-[[1-methylcyclopropyl]amino]-4H-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide Solubility (25°C):   体外:   DMSO   Ethanol   Water   体内(现配现用):   <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 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。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 3.4272mL 17.1362mL 34.2724mL 5mM 0.6854mL 3.4272mL 6.8545mL 10mM 0.3427mL 1.7136mL 3.4272mL   生物活性 产品描述 一种有效的,口服活性的SUR1/Kir6.2选择性KATP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。 靶点 K ATP channels   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 31µM,respectively in the patch-clamp assay.Tifenazoxide (100µM) 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=0.1µM). 体内研究 Tifenazoxide (NN414;1.5mg/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: 1.5mg/kg Administration: Oral administration;twice daily;for 3 weeks Result: Basal glucose was significantly reduced with the fall averaging 0.64mM after 3 weeks of treatment.
保存条件:-20℃