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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$l^{6},9-dithia-3,5-diazab icyclo[4.3.0]nona-3,7,10-trien-4-amine, 279215-43-9, 结构式
8-chloro-N-(1-methylcyclopropyl)-2,2-dioxo-2$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$l^{6},9-dithia-3,5-diazab icyclo[4.3.0]nona-3,7,10-trien-4-amine
英文别名:
NN414;tifenazoxide;NN414 >=98% (HPLC);NN 414 - Tifenazoxide;6-Chloro-3-[[1-methylcyclopropyl]amino]-4H-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide;2H-Thieno[3,2-e]-1,2,4-thiadiazin-3-amine, 6-chloro-N-(1-methylcyclopropyl)-, 1,1-dioxide;8-chloro-N-(1-methylcyclopropyl)-2,2-dioxo-2$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
中文别名:
化合物 T17094;6-氯-3-[[1-甲基环丙基]氨基]-4H-噻吩并[3,2-E]-1,2,4-噻二嗪1,1-二氧化物
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

更新日期产品编号产品名称CAS编号包装价格
2024/08/19HY-1193228-chloro-N-(1-methylcyclopropyl)-2,2-dioxo-2$l^{6},9-dithia-3,5-diazab icyclo[4.3.0]nona-3,7,10-trien-4-amine
Tifenazoxide
279215-43-95mg1750元
2024/08/19HY-1193228-chloro-N-(1-methylcyclopropyl)-2,2-dioxo-2$l^{6},9-dithia-3,5-diazab icyclo[4.3.0]nona-3,7,10-trien-4-amine
Tifenazoxide
279215-43-910mM * 1mLin DMSO1925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

供应商联系电话电子邮件国家产品数优势度
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天津普西唐生物医药科技有限公司 010-60605840 15801484223 psaitong@jm-bio.com 中国 29778 58
TargetMol中国(陶术生物) 4008200310 marketing@tsbiochem.com 中国 23963 58
苏州美石生物科技有限公司 1173954148q meishipharma@126.com 中国 20035 58
江苏艾康生物医药研发有限公司 025-66113011 18112977050 cb5@aikonchem.com 中国 10529 58
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279215-43-9, 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 相关搜索:

  • C9H10ClN3O2S2
  • 6-氯-3-[[1-甲基环丙基]氨基]-4H-噻吩并[3,2-E]-1,2,4-噻二嗪1,1-二氧化物
  • 化合物 T17094
  • 279215-43-9
  • NN 414 - Tifenazoxide
  • NN414 >=98% (HPLC)
  • 2H-Thieno[3,2-e]-1,2,4-thiadiazin-3-amine, 6-chloro-N-(1-methylcyclopropyl)-, 1,1-dioxide
  • NN414
  • 6-Chloro-3-[[1-methylcyclopropyl]amino]-4H-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide
  • tifenazoxide
  • 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
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