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#: 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

生物活性靶点体外研究体内研究用途与合成方法 MSDS 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) 上下游产品信息

中文名称	8-chloro-N-(1-methylcyclopropyl)-2,2-dioxo-2$l^{6},9-dithia-3,5-diazab icyclo[4.3.0]nona-3,7,10-trien-4-amine
中文同义词	化合物 T17094;6-氯-3-[[1-甲基环丙基]氨基]-4H-噻吩并[3,2-E]-1,2,4-噻二嗪1,1-二氧化物
英文名称	8-chloro-N-(1-methylcyclopropyl)-2,2-dioxo-2$l^{6},9-dithia-3,5-diazab icyclo[4.3.0]nona-3,7,10-trien-4-amine
英文同义词	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;6-Chloro-3-[[1-methylcyclopropyl]amino]-4H-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide;NN414;2H-Thieno[3,2-e]-1,2,4-thiadiazin-3-amine, 6-chloro-N-(1-methylcyclopropyl)-, 1,1-dioxide;NN414 >=98% (HPLC);NN 414 - Tifenazoxide
CAS号	279215-43-9
分子式	C9H10ClN3O2S2
分子量	291.78
EINECS号
相关类别
Mol文件	279215-43-9.mol
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 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 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

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.

安全信息

WGK Germany	3

MSDS信息

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
2024/04/30	HY-119322	8-chloro-N-(1-methylcyclopropyl)-2,2-dioxo-2$l^{6},9-dithia-3,5-diazab icyclo[4.3.0]nona-3,7,10-trien-4-amine Tifenazoxide	279215-43-9	5mg	1750元
2024/04/30	HY-119322	8-chloro-N-(1-methylcyclopropyl)-2,2-dioxo-2$l^{6},9-dithia-3,5-diazab icyclo[4.3.0]nona-3,7,10-trien-4-amine Tifenazoxide	279215-43-9	10mM * 1mLin DMSO	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