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
![8-chloro-N-(1-methylcyclopropyl)-2,2-dioxo-2$l^{6},9-dithia-3,5-diazab icyclo[4.3.0]nona-3,7,10-trien-4-amine 结构式](https://img.chemicalbook.com/CAS/20200515/GIF/279215-43-9.gif)
8-chloro-N-(1-methylcyclopropyl)-2,2-dioxo-2$l^{6},9-dithia-3,5-diazab icyclo[4.3.0]nona-3,7,10-trien-4-amine 性质
| 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：可溶15mg/mL，澄清 |
| 酸度系数(pKa) | -6.81±0.20(Predicted) |
| 形态 | 粉末 |
| 颜色 | 白色至米色 |
8-chloro-N-(1-methylcyclopropyl)-2,2-dioxo-2$l^{6},9-dithia-3,5-diazab icyclo[4.3.0]nona-3,7,10-trien-4-amine 用途与合成方法
K ATP channels
Tifenazoxide (NN414) hyperpolarises βTC3 cell membranes, and inhibits insulin release from βTC6, from isolated rat islets and from human islets at least a 100-fold more potent than Diazoxide.
The EC
50
values for Tifenazoxide and diazoxide are 0.45 and 31 µM, respectively in the patch-clamp assay. Tifenazoxide (100 µM) activates Kir6.2/SUR1 channels, but not Kir6.2/SUR2A or Kir6.2/SUR2 channels, expressed in Xenopus oocytes both in whole-cell and inside-out macropatch recordings.
Tifenazoxide is a potent inhibitor of glucose stimulated insulin release from βTC6 cells (IC
50
= 0.15 µM).
Tifenazoxide (NN414; 1.5 mg/kg; oral administration; twice daily; for 3 weeks; male VDF Zucker ( fa/fa ) rat) treatment for 3 weeks in VDF rats reduces basal hyperglycemia, improves glucose tolerance, and reduces hyperinsulinemia during an oral glucose tolerance test (OGTT) and improves insulin secretory responsiveness ex vivo.
| Animal Model: | Male Vancouver diabetic fatty (VDF) Zucker rat |
| Dosage: | 1.5 mg/kg |
| Administration: | Oral administration; twice daily; for 3 weeks |
| Result: | Basal glucose was significantly reduced with the fall averaging 0.64 mM after 3 weeks of treatment. |
8-chloro-N-(1-methylcyclopropyl)-2,2-dioxo-2$l^{6},9-dithia-3,5-diazab icyclo[4.3.0]nona-3,7,10-trien-4-amine 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2025-02-05 | HY-119322 | 8-chloro-N-(1-methylcyclopropyl)-2,2-dioxo-2$l^{6},9-dithia-3,5-diazab icyclo[4.3.0]nona-3,7,10-trien-4-amine | 279215-43-9 | 5mg | 1750 |
| 2025-02-05 | HY-119322 | 8-chloro-N-(1-methylcyclopropyl)-2,2-dioxo-2$l^{6},9-dithia-3,5-diazab icyclo[4.3.0]nona-3,7,10-trien-4-amine | 279215-43-9 | 10mM * 1mLin DMSO | 1925 |
