产品说明书
Coptisine chloride
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同义名 : | 氯化黄连碱 ;Coptisine (chloride);Q-100696;NSC-119754 |
| CAS号 : | 6020-18-4 | |
| 货号 : | A497811 | |
| 分子式 : | C19H14ClNO4 | |
| 纯度 : | 98% | |
| 分子量 : | 355.772 | |
| MDL号 : | MFCD00016676 | |
| 存储条件： |
粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 9 mg/mL(25.3 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Coptisine chloride is an alkaloid from Chinese goldthread, and acts as an efficient uncompetitive IDO inhibitor with a Ki value of 5.8 μM and an IC50 value of 6.3 μM[1]. Coptisine (0.1-100 μM) inhibits the proliferation of A549, H460, H2170, MDA-MB-231 and HT-29 cells, with IC50s of 18.09, 29.50, 21.60, 20.15 and 26.60 µM, respectively. Coptisine (12.5, 25, 50 μM) upregulates the expression of pH2AX and p21, reduces expression of cyclin B1, cdc2, and cdc25C, and induces G2/M arrest and apoptosis of A549 cells in a concentration-dependent manner. Coptisine (12.5, 25, 50 μM) also induces mitochondrial dysfunction and activates caspases activities in A549 cells. Furthermore, Coptisine (50 μM) increases ROS levels in a time-dependent manner (0.5, 1, 2, 4, 12, and 24 h)[2]. Coptisine shows increased toxicity in mice in a concentration dependent manner, with LD50 value of 880.18 mg/kg. Coptisine (154 mg/kg/day, 90 days) shows no toxicity on SD rats. Coptisine (23.35, 46.7, 70.05 mg/kg, p.o.) dose-dependently decreases the levels of TC, TG, and LDL-c and increases HDL-c content in serum of hamsters to different degree, slows down weight gain induced by the HFHC (high-fat and high-cholesterol diet) diet, and raises the level of cholesterol and TBA (total bile acid) in feces dose-dependently in hamsters. Coptisine (70.05 mg/kg, p.o.) suppresses HMGCR (3-hydroxy-3-methyl-glutaryl-CoA reductase) protein expression level and induces the protein expression of SREBP-2, LDLR(low-density lipoprotein receptor), and CYP7A1 (cholesterol 7α-hydroxylase) involved in cholesterol metabolism[3]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.81mL 0.56mL 0.28mL |
14.05mL 2.81mL 1.41mL |
28.11mL 5.62mL 2.81mL |
| 参考文献 |
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