货号:A497811
同义名:
氯化黄连碱
/ Coptisine (chloride); Q-100696
Coptisine chloride是从黄连中分离的生物碱,抑制 IDO (Ki = 5.8 μM) 和 H1N1 神经氨酸酶 (IC50 = 104.6 μg/mL),具有抗肝癌和抗流感活性。
HazMat Fee + There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
| Type | HazMat fee for 500 gram (Estimated) |
| Excepted Quantity | USD 0.00 |
| Limited Quantity | USD 15-60 |
| Inaccessible (Haz class 6.1), Domestic | USD 80+ |
| Inaccessible (Haz class 6.1), International | USD 150+ |
| Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
| Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |


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|---|---|---|---|---|---|---|---|
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| 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]. |
| Concentration | Treated Time | Description | References | |
| NCI-H1299 | 10 μM or 20 μM | 24 h | To evaluate the effect of COP on ATF4 mRNA levels, results showed that COP significantly reduced ATF4 expression. | Adv Sci (Weinh). 2024 Sep;11(35):e2401748 |
| NCI-H460 | 10 μM or 20 μM | 24 h | To evaluate the effect of COP on ATF4 mRNA levels, results showed that COP significantly reduced ATF4 expression. | Adv Sci (Weinh). 2024 Sep;11(35):e2401748 |
| Helicobacter pylori clinical isolates | 25-50 μg/mL | 3 days | To evaluate the antibacterial activity of Coptisine against clinical isolates, results showed that the MICs of Coptisine against clinical isolates were either 25 or 50 μg/mL | J Enzyme Inhib Med Chem. 2018 Dec;33(1):1362-1375 |
| Helicobacter pylori standard strain NCTC 11637 | 25 μg/mL | 3 days | To evaluate the antibacterial activity of Coptisine against H. pylori, results showed that the MIC of Coptisine against NCTC 11637 strain was 25 μg/mL | J Enzyme Inhib Med Chem. 2018 Dec;33(1):1362-1375 |
| Hep3B cells | 50 µM | 24 h | To assess the cytotoxic effect of coptisine in Hep3B cells, results showed that coptisine significantly inhibited cell viability and induced apoptosis. | Int J Mol Sci. 2020 Jul 31;21(15):5502 |
| MOLM-13 cells | 0–20 μM | 12 h | Evaluated the effect of Coptisine chloride on m6A modification levels, showing COP dose-dependently decreased m6A levels of mRNAs. | Adv Sci (Weinh). 2024 Jul;11(26):e2308786 |
| A549 cells | 10 μM | 24 h | significantly lowered KRAS mRNA levels | Nat Commun. 2022 Oct 12;13(1):6016 |
| H460 cells | 10 μM | 24 h | significantly lowered KRAS mRNA levels | Nat Commun. 2022 Oct 12;13(1):6016 |
| Administration | Dosage | Frequency | Description | References | ||
| BALB/c nude mice | H460 xenograft tumor model | Intraperitoneal injection | 100 mg/kg | Every other day for two weeks | To evaluate the effect of COP in glutamine restriction therapy, results showed that COP significantly enhanced the inhibitory effect of glutamine-restrictive therapy on tumor growth. | Adv Sci (Weinh). 2024 Sep;11(35):e2401748 |
| Mice | Periodontitis model | Local gingival injection | 20 μM | Daily until endpoint | Assessed the therapeutic effect of Coptisine chloride on periodontitis, showing COP significantly alleviated inflammatory bone loss and reduced IL-1β and GSDMD expression. | Adv Sci (Weinh). 2024 Jul;11(26):e2308786 |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.81mL 0.56mL 0.28mL |
14.05mL 2.81mL 1.41mL |
28.11mL 5.62mL 2.81mL |
|
| CAS号 | 6020-18-4 |
| 分子式 | C19H14ClNO4 |
| 分子量 | 355.77 |
| SMILES Code | C1(C(CC[N+]2=C1C=C(C=C3)C(C4=C3OCO4)=C2)=C5)=CC6=C5OCO6.[Cl-] |
| MDL No. | MFCD00016676 |
| 别名 | 氯化黄连碱 ;Coptisine (chloride); Q-100696; NSC-119754 |
| 运输 | 蓝冰 |
| InChI Key | LUXPUVKJHVUJAV-UHFFFAOYSA-M |
| Pubchem ID | 72321 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Inert atmosphere, 2-8°C |
| 溶解方案 |
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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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