生物活性 靶点 体外研究 体内研究 8-chloro-N-(1-methylcyclopropyl)-2,2-dioxo-2$l^{6},9-dithia-3,5-diazab icyclo[4.3.0]nona-3,7,10-trien-4-amine 试剂级价格
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ChemicalBook  CAS数据库列表  8-chloro-N-(1-methylcyclopropyl)-2,2-dioxo-2$l^{6},9-dithia-3,5-diazab icyclo[4.3.0]nona-3,7,10-trien-4-amine

8-chloro-N-(1-methylcyclopropyl)-2,2-dioxo-2$l^{6},9-dithia-3,5-diazab icyclo[4.3.0]nona-3,7,10-trien-4-amine

生物活性 靶点 体外研究 体内研究 8-chloro-N-(1-methylcyclopropyl)-2,2-dioxo-2$l^{6},9-dithia-3,5-diazab icyclo[4.3.0]nona-3,7,10-trien-4-amine 试剂级价格
8-chloro-N-(1-methylcyclopropyl)-2,2-dioxo-2$l^{6},9-dithia-3,5-diazab icyclo[4.3.0]nona-3,7,10-trien-4-amine,279215-43-9,结构式
8-chloro-N-(1-methylcyclopropyl)-2,2-dioxo-2$l^{6},9-dithia-3,5-diazab icyclo[4.3.0]nona-3,7,10-trien-4-amine
  • CAS号:279215-43-9
  • 英文名:8-chloro-N-(1-methylcyclopropyl)-2,2-dioxo-2$l^{6},9-dithia-3,5-diazab icyclo[4.3.0]nona-3,7,10-trien-4-amine
  • 中文名:8-chloro-N-(1-methylcyclopropyl)-2,2-dioxo-2$l^{6},9-dithia-3,5-diazab icyclo[4.3.0]nona-3,7,10-trien-4-amine
  • CBNumber:CB71261289
  • 分子式:C9H10ClN3O2S2
  • 分子量:291.78
  • MOL File:279215-43-9.mol
8-chloro-N-(1-methylcyclopropyl)-2,2-dioxo-2$l^{6},9-dithia-3,5-diazab icyclo[4.3.0]nona-3,7,10-trien-4-amine化学性质
  • 熔点 :251-252 °C (decomp)(Solv: methanol (67-56-1); water (7732-18-5))
  • 沸点 :448.0±55.0 °C(Predicted)
  • 密度 :1.88±0.1 g/cm3(Predicted)
  • 储存条件 :2-8°C
  • 溶解度 :DMSO: soluble15mg/mL, clear
  • 酸度系数(pKa) :-6.81±0.20(Predicted)
  • 形态 :powder
  • 颜色 :white to beige
安全信息
  • WGK Germany :3

8-chloro-N-(1-methylcyclopropyl)-2,2-dioxo-2$l^{6},9-dithia-3,5-diazab icyclo[4.3.0]nona-3,7,10-trien-4-amine性质、用途与生产工艺

  • 生物活性 Tifenazoxide (NN414) 是一种有效的，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 EC 50 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 (IC 50 = 0.15 µM).

  • 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.
8-chloro-N-(1-methylcyclopropyl)-2,2-dioxo-2$l^{6},9-dithia-3,5-diazab icyclo[4.3.0]nona-3,7,10-trien-4-amine上下游产品信息
上游原料
下游产品
8-chloro-N-(1-methylcyclopropyl)-2,2-dioxo-2$l^{6},9-dithia-3,5-diazab icyclo[4.3.0]nona-3,7,10-trien-4-amine 试剂级价格
  • 更新日期：2025/02/05
  • 产品编号：HY-119322
  • 产品名称：8-chloro-N-(1-methylcyclopropyl)-2,2-dioxo-2$l^{6},9-dithia-3,5-diazab icyclo[4.3.0]nona-3,7,10-trien-4-amine Tifenazoxide
  • CAS编号：279215-43-9
  • 包装：5mg
  • 价格：1750元
  • 更新日期：2025/02/05
  • 产品编号：HY-119322
  • 产品名称：8-chloro-N-(1-methylcyclopropyl)-2,2-dioxo-2$l^{6},9-dithia-3,5-diazab icyclo[4.3.0]nona-3,7,10-trien-4-amine Tifenazoxide
  • CAS编号：279215-43-9
  • 包装：10mM * 1mLin DMSO
  • 价格：1925元
8-chloro-N-(1-methylcyclopropyl)-2,2-dioxo-2$l^{6},9-dithia-3,5-diazab icyclo[4.3.0]nona-3,7,10-trien-4-amine生产厂家
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