那可汀

生物活性靶点体外研究体内研究那可汀试剂级价格

那可汀

CAS号:128-62-1
英文名:Narcotine
中文名:那可汀
CBNumber:CB8468501
分子式:C22H23NO7
分子量:413.42
MOL File:128-62-1.mol

那可汀化学性质

熔点 :174-176 °C(lit.)
比旋光度 :-200 º (c=1 in chloroform)
沸点 :532.6°C (rough estimate)
密度 :1.395
折射率 :1.5614 (estimate)
储存条件 :-20°C Freezer, Under Inert Atmosphere
溶解度 :Practically insoluble in water, soluble in acetone, slightly soluble in ethanol (96 per cent). It dissolves in strong acids; on dilution of the solution with water, the base may be precipitated.
酸度系数(pKa) :7.8(at 25℃)
颜色 :Orthorhombic prisms or stout needles from alc
旋光性 (optical activity) :[α]20/D 200°, c = 1 in chloroform
水溶解性 :302.9mg/L(25 ºC)
Merck :13,6752
NIST化学物质信息 :Narcotine alkaloid(128-62-1)
EPA化学物质信息 :1(3H)-Isobenzofuranone, 6,7-dimethoxy-3-[(5R)-5,6,7,8-tetrahydro-4-methoxy-6-methyl-1,3-dioxolo[4,5-g]isoquinolin-5-yl]-, (3S)- (128-62-1)

安全信息

危险品标志 :Xn
危险类别码 :22
安全说明 :24/25
危险品运输编号 :1544
WGK Germany :3
RTECS号 :RD2625000
危险等级 :6.1(b)
包装类别 :III
海关编码 :29329990
毒害物质数据 :128-62-1(Hazardous Substances Data)
毒性 :cyt-ham:lng 100 mg/L ATSUDG (4),41,80

那可汀性质、用途与生产工艺

生物活性 Noscapine ((S,R)-Noscapine) 是一种具有口服活性的苯酞异喹啉生物碱，具有强效镇咳作用。Noscapine 通过激活 sigma 阿片类受体 (sigma opioid receptors) 发挥镇咳作用，是一种非竞争性 Bradykinin 抑制剂。Noscapine 破坏微管动力学，诱导细胞有丝分裂停滞和凋亡 (apoptosis) 以及活性。Noscapine 具有抗癌，神经保护，抗炎活性，并且可以穿越血脑屏障。
靶点

Sigma opioid receptors Bradykinin Apoptosis

体外研究

Noscapine (0-1000 μM; 0-96 hours; rat C6 glioma cells) treatment inhibits cell viability of rat C6 glioma in vitro in a dose- and time-dependent manner. Noscapine inhibits the viability of rat C6 glioma cells with an IC ₅₀ of 250 μM at 72 hours.
Noscapine exposure causes abnormal S-phase reentry, increases mitotic arrest and results in excessive DNA accumulation.
Cylindromatosis increases the ability of noscapine to induce mitotic arrest and apoptosis. Cylindromatosis enhances the effect of noscapine on microtubule polymerization and promotes noscapine binding to microtubules.

Cell Viability Assay

Cell Line:	Rat C6 glioma cells
Concentration:	0 μM, 0.1 μM, 1 μM, 2 μM, 10 μM, 50 μM, 100 μM, 1000 μM
Incubation Time:	0 hours, 12 hours, 24 hours, 48 hours, 72 hours, 96 hours
Result:	Inhibited cell viability of rat C6 glioma in vitro in a dose- and time-dependent manner.

体内研究

Noscapine (300 mg/kg; oral gavage; daily; for 15 days; athymic female mice) treatment reduces tumor growth in mice.

Animal Model:	Athymic female mice (nu/nu) (8-week-old) injected with rat C6 glioma cells
Dosage:	300 mg/kg
Administration:	Oral gavage; daily; for 15 days
Result:	Revealed a significant reduction of tumor volume.