[CAS NO. 6020-18-4] Coptisine chloride
PRODUCTS SPECIFICATIONS [6020-18-4]
DESCRIPTION [6020-18-4]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 355.77 |
| Molecular Formula | C19H14ClNO4 |
| SMILES | C1(C(CC[N+]2=C1C=C(C=C3)C(C4=C3OCO4)=C2)=C5)=CC6=C5OCO6.[Cl-] |
2 Publications Citing Use of MCE
Summary
Coptisine chloride is an alkaloid from Chinese goldthread, and acts as an efficient uncompetitive IDO inhibitor with a K i value of 5.8 μM and an IC 50 value of 6.3 μM. Coptisine chloride is a potent H1N1 neuraminidase (NA-1) inhibitor with an IC 50 of 104.6 μg/mL and can be used for influenza A (H1N1) infection .
IC50 & Target
|
IDO 6.3 μM (IC 50 ) |
IDO 5.8 μM (Ki) |
In Vitro
Coptisine chloride is an efficient uncompetitive IDO inhibitor with a K i value of 5.8 μM and an IC 50 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 IC 50 s 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) [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Coptisine shows increased toxicity in mice in a concentration dependent manner, with LD 50 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 diet, and raises the level of cholesterol and TBA in feces dose-dependently in hamsters. Coptisine (70.05 mg/kg, p.o.) suppresses HMGCR protein expression level and induces the protein expression of SREBP-2, LDLR, and CYP7A1 involved in cholesterol metabolism [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 10.42 mg/mL ( 29.29 mM ; ultrasonic and warming and heat to 60°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.8108 mL | 14.0540 mL | 28.1080 mL |
| 5 mM | 0.5622 mL | 2.8108 mL | 5.6216 mL |
| 10 mM | 0.2811 mL | 1.4054 mL | 2.8108 mL |
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1.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1.04 mg/mL (2.92 mM); Clear solution
-
2.
References
- [1] Yu D, et al. The IDO inhibitor coptisine ameliorates cognitive impairment in a mouse model of Alzheimer's disease. J Alzheimers Dis. 2015;43(1):291-302.
- [2] He K, et al. The safety and anti-hypercholesterolemic effect of coptisine in Syrian golden hamsters. Lipids. 2015 Feb;50(2):185-94.
- [3] Rao PC, et al. Coptisine-induced cell cycle arrest at G2/M phase and reactive oxygen species-dependent mitochondria-mediated apoptosis in non-small-cell lung cancer A549 cells. Tumour Biol. 2017 Mar;39(3):1010428317694565.
- [4] Zhou X, et al. Inhibition activity of a traditional Chinese herbal formula Huang-Lian-Jie-Du-Tang and its major components found in its plasma profile on neuraminidase-1. Sci Rep. 2017 Nov 14;7(1):15549.
Synonyms