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Coptisine sulfate

CAS# 1198398-71-8

Coptisine sulfate

Catalog No. BCN2286----Order now to get a substantial discount!

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Coptisine sulfate: 5mg $40 In Stock
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Quality Control of Coptisine sulfate

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Chemical structure

Coptisine sulfate

3D structure

Chemical Properties of Coptisine sulfate

Cas No. 1198398-71-8 SDF Download SDF
PubChem ID 131674029 Appearance Powder
Formula C19H15NO8S M.Wt 417.4
Type of Compound Alkaloids Storage Desiccate at -20°C
Solubility Soluble in Chloroform,Dichloromethane,Ethyl Acetate,DMSO,Acetone,etc.
Chemical Name hydrogen sulfate;5,7,17,19-tetraoxa-13-azoniahexacyclo[11.11.0.02,10.04,8.015,23.016,20]tetracosa-1(13),2,4(8),9,14,16(20),21,23-octaene
SMILES C1C[N+]2=C(C=C3C=CC4=C(C3=C2)OCO4)C5=CC6=C(C=C51)OCO6.OS(=O)(=O)[O-]
Standard InChIKey LHNQVPXIJDUPAX-UHFFFAOYSA-M
Standard InChI InChI=1S/C19H14NO4.H2O4S/c1-2-16-19(24-10-21-16)14-8-20-4-3-12-6-17-18(23-9-22-17)7-13(12)15(20)5-11(1)14;1-5(2,3)4/h1-2,5-8H,3-4,9-10H2;(H2,1,2,3,4)/q+1;/p-1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Source of Coptisine sulfate

The roots of Chelidonium majus

Biological Activity of Coptisine sulfate

DescriptionCoptisine sulfate can competitively inhibit CYP2D6(*)1 and CYP2D6(*)10, its Ki values for CYP2D6(*)1 and CYP2D6(*)10 are very close, suggesting that genotype-dependent herb-drug inhibition is similar between the two variants.
TargetsP450 (e.g. CYP17)
In vitro

Inhibitory effects of phytochemicals on metabolic capabilities of CYP2D6(*)1 and CYP2D6(*)10 using cell-based models in vitro.[Pubmed: 24786236 ]

Acta Pharmacol Sin. 2014 May;35(5):685-96.

Herbal products have been widely used, and the safety of herb-drug interactions has aroused intensive concerns. This study aimed to investigate the effects of phytochemicals on the catalytic activities of human CYP2D6(*)1 and CYP2D6(*)10 in vitro.
METHODS AND RESULTS:
HepG2 cells were stably transfected with CYP2D6(*)1 and CYP2D6(*)10 expression vectors. The metabolic kinetics of the enzymes was studied using HPLC and fluorimetry. HepG2-CYP2D6(*)1 and HepG2-CYP2D6(*)10 cell lines were successfully constructed. Among the 63 phytochemicals screened, 6 compounds, including Coptisine sulfate, bilobalide, schizandrin B, luteolin, schizandrin A and puerarin, at 100 μmol/L inhibited CYP2D6(*)1- and CYP2D6(*)10-mediated O-demethylation of a coumarin compound AMMC by more than 50%. Furthermore, the inhibition by these compounds was dose-dependent. Eadie-Hofstee plots demonstrated that these compounds competitively inhibited CYP2D6(*)1 and CYP2D6(*)10. However, their Ki values for CYP2D6(*)1 and CYP2D6(*)10 were very close, suggesting that genotype-dependent herb-drug inhibition was similar between the two variants.
CONCLUSIONS:
Six phytochemicals inhibit CYP2D6(*)1 and CYP2D6(*)10-mediated catalytic activities in a dose-dependent manner in vitro. Thus herbal products containing these phytochemicals may inhibit the in vivo metabolism of co-administered drugs whose primary route of elimination is CYP2D6.

Coptisine sulfate Dilution Calculator

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Coptisine sulfate Molarity Calculator

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Preparing Stock Solutions of Coptisine sulfate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.3958 mL 11.9789 mL 23.9578 mL 47.9157 mL 59.8946 mL
5 mM 0.4792 mL 2.3958 mL 4.7916 mL 9.5831 mL 11.9789 mL
10 mM 0.2396 mL 1.1979 mL 2.3958 mL 4.7916 mL 5.9895 mL
50 mM 0.0479 mL 0.2396 mL 0.4792 mL 0.9583 mL 1.1979 mL
100 mM 0.024 mL 0.1198 mL 0.2396 mL 0.4792 mL 0.5989 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on Coptisine sulfate

Inhibitory effects of phytochemicals on metabolic capabilities of CYP2D6(*)1 and CYP2D6(*)10 using cell-based models in vitro.[Pubmed:24786236]

Acta Pharmacol Sin. 2014 May;35(5):685-96.

AIM: Herbal products have been widely used, and the safety of herb-drug interactions has aroused intensive concerns. This study aimed to investigate the effects of phytochemicals on the catalytic activities of human CYP2D6(*)1 and CYP2D6(*)10 in vitro. METHODS: HepG2 cells were stably transfected with CYP2D6(*)1 and CYP2D6(*)10 expression vectors. The metabolic kinetics of the enzymes was studied using HPLC and fluorimetry. RESULTS: HepG2-CYP2D6(*)1 and HepG2-CYP2D6(*)10 cell lines were successfully constructed. Among the 63 phytochemicals screened, 6 compounds, including Coptisine sulfate, bilobalide, schizandrin B, luteolin, schizandrin A and puerarin, at 100 mumol/L inhibited CYP2D6(*)1- and CYP2D6(*)10-mediated O-demethylation of a coumarin compound AMMC by more than 50%. Furthermore, the inhibition by these compounds was dose-dependent. Eadie-Hofstee plots demonstrated that these compounds competitively inhibited CYP2D6(*)1 and CYP2D6(*)10. However, their Ki values for CYP2D6(*)1 and CYP2D6(*)10 were very close, suggesting that genotype-dependent herb-drug inhibition was similar between the two variants. CONCLUSION: Six phytochemicals inhibit CYP2D6(*)1 and CYP2D6(*)10-mediated catalytic activities in a dose-dependent manner in vitro. Thus herbal products containing these phytochemicals may inhibit the in vivo metabolism of co-administered drugs whose primary route of elimination is CYP2D6.

Description

Coptisine Sulfate 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.

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