Art. -Nr.: HY-N0736

Coptisine chloride

Name: Coptisine chloride
Brand: MedChemExpress
SKU: HY-N0736
Price: 75.00 USD
Availability: InStock
Rating: 5 (13 reviews)

13 Cited Publications

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Based on 13 publication(s) in Google Scholar

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 IC₅₀ value of 6.3 μM. Coptisine chloride is a potent H1N1 neuraminidase (NA-1) inhibitor with an IC₅₀ of 104.6?μg/mL and can be used for influenza A (H1N1) infection.

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Reinheit : 99.73%
CAS. Nr.: 6020-18-4
Formel: C₁₉H₁₄ClNO₄
Molecular Weight:355.77

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Coptisine chloride Chemical Structure

CAS. Nr.: 6020-18-4

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (13)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

IDO

6.3 μM (IC₅₀)

IDO

5.8 μM (Ki)

Alle Indoleamine 2,3-Dioxygenase (IDO) Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A10	GI₅₀	4.49 μM Compound: 1	Growth inhibition against rat A10 cells after 72 hrs by MTT assay Growth inhibition against rat A10 cells after 72 hrs by MTT assay	[PMID: 21401114]
A549	IC₅₀	>14.05 μM Compound: 1	Cytotoxicity against human A549 cells assessed as growth inhibition rate after 96 hrs by MTT assay Cytotoxicity against human A549 cells assessed as growth inhibition rate after 96 hrs by MTT assay	[PMID: 25203783]
A549	IC₅₀	23.96 μM Compound: 7	Cytotoxicity against human A549 cells by SRB assay Cytotoxicity against human A549 cells by SRB assay	[PMID: 20594848]
Bel-7402	IC₅₀	>14.05 μM Compound: 1	Cytotoxicity against human Bel7402 cells assessed as growth inhibition rate after 96 hrs by MTT assay Cytotoxicity against human Bel7402 cells assessed as growth inhibition rate after 96 hrs by MTT assay	[PMID: 25203783]
C-33-A	IC₅₀	>14.05 μM Compound: 1	Cytotoxicity against human C33A cells assessed as growth inhibition rate after 96 hrs by MTT assay Cytotoxicity against human C33A cells assessed as growth inhibition rate after 96 hrs by MTT assay	[PMID: 25203783]
G-402	GI₅₀	19.1 μM Compound: 1	Growth inhibition against human G402 cells after 48 hrs by MTT assay Growth inhibition against human G402 cells after 48 hrs by MTT assay	[PMID: 21401114]
HCT-15	IC₅₀	29.07 μM Compound: 7	Cytotoxicity against human HCT15 cells by SRB assay Cytotoxicity against human HCT15 cells by SRB assay	[PMID: 20594848]
HCT-8	IC₅₀	5.59 μM Compound: 1	Cytotoxicity against human HCT8 cells assessed as growth inhibition rate after 96 hrs by MTT assay Cytotoxicity against human HCT8 cells assessed as growth inhibition rate after 96 hrs by MTT assay	[PMID: 25203783]
SK-MEL-2	IC₅₀	>30 μM Compound: 7	Cytotoxicity against human SK-MEL-2 cells by SRB assay Cytotoxicity against human SK-MEL-2 cells by SRB assay	[PMID: 20594848]
SK-OV-3	IC₅₀	>30 μM Compound: 7	Cytotoxicity against human SKOV3 cells by SRB assay Cytotoxicity against human SKOV3 cells by SRB assay	[PMID: 20594848]
VSMC	GI₅₀	3.3 μM Compound: 1	Antiproliferative activity against rat VSMC assessed as cell growth inhibition Antiproliferative activity against rat VSMC assessed as cell growth inhibition	[PMID: 21401114]
VSMC	GI₅₀	3.35 μM Compound: 1	Growth inhibition against rat VSMC after 72 hrs by MTT assay Growth inhibition against rat VSMC after 72 hrs by MTT assay	[PMID: 21401114]

In Vitro

Coptisine chloride is an efficient uncompetitive IDO inhibitor with a K_i 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)^[3].

MedChemExpress (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 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 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Related Protocols :

Research Protocol for Infectious Diseases

Chemical Information

CAS. Nr. 6020-18-4
Appearance Solid
Molecular Weight 355.77
Formel C₁₉H₁₄ClNO₄
Color Orange to reddish brown
SMILES

C1(C(CC[N+]2=C1C=C(C=C3)C(C4=C3OCO4)=C2)=C5)=CC6=C5OCO6.[Cl-]
Structure Classification
- Alkaloids
- Isoquinoline Alkaloids
Initial Source
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (13)

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Journal Impact Factor

Phytomedicine

Jiao-tai-wan and its component coptisine attenuate PCOS by regulating mitochondrial cholesterol import through suppression of SIRT1 ubiquitination. [Abstract]

2025 Nov 25:148:157446. PMID: 41145090

Coptisine chloride purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 Nov 25:148:157446. [Abstract]

Coptisine chloride (10 μM). Western blot analysis of StAR in the cytoplasm and mitochondria of theca cells.

Coptisine chloride purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 Nov 25:148:157446. [Abstract]

Coptisine chloride (10 μM). Confocal imaging of COXIV/Filipin III/PI and colocalization analysis of COXIV and Filipin III in ovarian theca cells.

Coptisine chloride purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 Nov 25:148:157446. [Abstract]

Western blot analysis of SIRT1 in theca cells treated with coptisine chloride (10 μM), MG132, and bafilomycin A1.

Coptisine chloride purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 Nov 25:148:157446. [Abstract]

SPR results for coptisine chloride and the SIRT1 protein.
J Med Chem

2026 Aug 13;69(15):19338-19354. PMID: 42593899
Int Immunopharmacol

Coptisine inhibits aggressive and proliferative actions of fibroblast like synoviocytes and exerts a therapeutic potential for rheumatoid arthritis. [Abstract]

2024 Feb 15:128:111433. PMID: 38181676
Molecules

Discovery of Nine Dipeptidyl Peptidase-4 Inhibitors from Coptis chinensis Using Virtual Screening, Bioactivity Evaluation, and Binding Studies. [Abstract]

2024 May 14;29(10):2304. PMID: 38792165
Food Sci Nutr

2026 Jul 15;14(7):e72107. PMID: 42460425
Mater Technol (N Y N Y)

2026 Jan 27;41.
Naunyn Schmiedebergs Arch Pharmacol

Coptisine inhibits lipid accumulation in high glucose- and palmitic acid-induced HK-2 cells by regulating the AMPK/ACC/CPT-1 signaling pathway. [Abstract]

2025 May;398(5):5465-5474. PMID: 39560754
Vet Microbiol

The Chinese medicine monomer Schisandrin C inhibits PRRSV infection by regulating the OGT-PI3K/AKT/mTOR signaling pathway. [Abstract]

2026 May:316:110992. PMID: 41865607
DNA Cell Biol

Coptisine Blocks Secretion of Exosomal circCCT3 from Cancer-Associated Fibroblasts to Reprogram Glucose Metabolism in Hepatocellular Carcinoma. [Abstract]

2020 Oct 2. PMID: 33001706
Biochem Biophys Res Commun

Coptisine alleviates insulin resistance by suppressing SMARCE1-mediated glycolysis. [Abstract]

2026 Mar 26:806:153415. PMID: 41662796
Planta Med

Novel Approaches for the Analysis and Isolation of Benzylisoquinoline Alkaloids in Chelidonium majus. [Abstract]

2024 Jun;90(7-08):523-533. PMID: 38843792
SSRN

2024 Apr 1.
J Oncol

Pseudogene MSTO2P Interacts with miR-128-3p to Regulate Coptisine Sensitivity of Non-Small-Cell Lung Cancer (NSCLC) through TGF- β Signaling and VEGFC. [Abstract]

2022 Jun 26:2022:9864411. PMID: 35794983

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 7.94 mg/mL (22.32 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 0.8 mg/mL (2.25 mM); Clear solution

This protocol yields a clear solution of ≥ 0.8 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 0.8 mg/mL (2.25 mM); Clear solution

This protocol yields a clear solution of ≥ 0.8 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

[2]. He K, et al. The safety and anti-hypercholesterolemic effect of coptisine in Syrian golden hamsters. Lipids. 2015 Feb;50(2):185-94. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.8108 mL	14.0540 mL	28.1080 mL	70.2701 mL
	5 mM	0.5622 mL	2.8108 mL	5.6216 mL	14.0540 mL
	10 mM	0.2811 mL	1.4054 mL	2.8108 mL	7.0270 mL
	15 mM	0.1874 mL	0.9369 mL	1.8739 mL	4.6847 mL
	20 mM	0.1405 mL	0.7027 mL	1.4054 mL	3.5135 mL

Bioz

Keywords

Coptisine chloride

13 Cited Publications

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Coptisine chloride

Publications Citing Use of MedChemExpress (MCE) Coptisine chloride

Alle Indoleamine 2,3-Dioxygenase (IDO) Isoform-spezifische Produkte anzeigen