Art. -Nr.: HY-N0430A

Coptisine Sulfate

5 Cited Publications

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Based on 5 publication(s) in Google Scholar

Coptisine Sulfate is an orally active and brain-penetrant alkaloid found in Coptis chinensis. Coptisine Sulfate is a reversible, uncompetitive IDO inhibitor with a K_i of 5.8 μM and an IC₅₀ of 6.3 μM. Coptisine Sulfate suppresses neuroinflammation, reduces Aβ plaque burden and shows neuroprotective activity. Coptisine Sulfate shows anti-inflammation activity by blocking NF-κB, MAPK, and PI3K/Akt activation. Coptisine Sulfate inhibits cancer cells proliferation, induces DNA damage, G2/M phase cell cycle arrest, apoptosis, ROS production and mitochondrial dysfunction. Coptisine Sulfate inhibits Rho/ROCK pathway activation, reduces arrhythmia, limits cardiac injury marker release, reduces infarct size, and preserves cardiac function in rat myocardial ischemia/reperfusion models. Coptisine Sulfate downregulates HMGCR and upregulates LDLR and CYP7A1 to modulate cholesterol metabolism, reduces abnormal serum lipid levels, and promotes fecal bile acid excretion. Coptisine Sulfate be used for the research of cancer, hypercholesterolemia, Alzheimer’s disease, inflammatory disorders and cardiovascular disease.

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Reinheit: 99.37%
CAS. Nr.: 1198398-71-8
Formel: C₁₉H₁₅NO₈S
Molecular Weight:417.39

Speicherung:

4°C, sealed storage, away from moisture and light

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

Coptisine Sulfate Chemical Structure

CAS. Nr.: 1198398-71-8

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (5)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 6.3 μM (IDO)^[1]
Ki: 5.8 μM (IDO)^[1]

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

Alle NF-κB Isoform-spezifische Produkte anzeigen :

Alle p38 MAPK Isoform-spezifische Produkte anzeigen :

Alle PI3K Isoform-spezifische Produkte anzeigen :

Alle Akt Isoform-spezifische Produkte anzeigen :

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen :

Alle ROCK Isoform-spezifische Produkte anzeigen :

In Vitro

Coptisine (0.1-100 μM; 48 h) Sulfate potently inhibits proliferation of human lung adenocarcinoma A5499, H460,
and H2170 cells (IC₅₀ = 18.09, 29.50, and 21.60 μM) Sulfate and other tested human cancer cell lines, with moderate selectivity relative to normal human umbilical vein endothelial cells^[1].
Coptisine (12.5-50 μM; 48 h) Sulfate induces concentration-dependent DNA damage in human lung adenocarcinoma A549 cells, as shown by increased γH2AX expression^[1].
Coptisine (12.5-50 μM; 48 h) Sulfate induces concentration-dependent G2/M phase cell cycle arrest in human lung adenocarcinoma A549 cells, mediated by downregulated cyclin B1, cdc2, and cdc25C expression and upregulated p21 expression^[1].
Coptisine (12.5-50 μM; 48 h) Sulfate induces concentration-dependent apoptosis in human lung adenocarcinoma A549 cells, inducing concentration-dependent activation of caspase 3/7, caspase 8, caspase 9, and cleavage of PARP^[1].
Coptisine (12.5-50 μM; 0.5-24 h) Sulfate induces time- and concentration-dependent reactive oxygen species generation in human lung adenocarcinoma A549 cells^[1].
Coptisine (12.5-50 μM; 24 h) Sulfate induces concentration-dependent mitochondrial dysfunction in human lung adenocarcinoma A549 cells, including loss of mitochondrial membrane potential and altered Bax, Bcl-2, and cytochrome c expression^[1].
Coptisine Sulfate potently inhibits recombinant human IDO as a reversible, uncompetitive inhibitor with a K_i of 5.8 μM and an IC₅₀ of 6.3 μM^[4].
Coptisine Sulfate inhibits IDO activity in HEK 293 cells with an IC₅₀ of 7.1 μM^[4].
Coptisine (10 μM; 5 h pre-incubation) Sulfate reverses amyloid-β peptide 1-42 and interferon-γ-induced IDO activation and restores cell viability in PC12 cells^[4].
Coptisine Sulfate inhibits LPS (HY-D1056)-stimulated inflammation by blocking NF-κB, MAPK, and PI3K/Akt activation in
macrophages^[5].

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

Western Blot Analysis^[1]

Cell Line:

human lung adenocarcinoma A549
Concentration:

12.5, 25, 50 μM
Incubation Time:

48 h
Result:

Caused a concentration-dependent upregulation of pH2AX, a marker of DNA double-strand breaks, relative to untreated control cells.

In Vivo

Coptisine (10-30 mg/kg; p.o.; single dose 10 min before ischemia or plus additional dose 4 h after reperfusion) Sulfate exerts pronounced cardioprotective effects against rat myocardial ischemia/reperfusion injury by reducing arrhythmias, infarct size, cardiac enzyme release, and left ventricular dysfunction, while suppressing myocardial apoptosis, inflammation, and Rho/ROCK pathway activation^[2].
Coptisine (23.35-70.05 mg/kg/day; i.g.; daily; 4 weeks) Sulfate dose-dependently improves hypercholesterolemia in HFHC-fed Syrian golden hamsters^[3].
Coptisine (482.5-1728 mg/kg; p.o.; single dose) has low acute toxicity in Kunming mice, with an LD₅₀ of 880.18 mg/kg following a single oral dose^[3].
Coptisine (154 mg/kg/day; p.o.; daily; 90 days) Sulfate is well-tolerated in SD rats with no observable toxicity via daily oral administration for 90 days^[3].
Coptisine (50 mg/kg; p.o.; once daily; 1 month) normalizes serum IDO activity, suppresses neuroinflammation, reduces Aβ plaque burden, restores neuronal integrity, and completely reverses cognitive impairment in A-PPswe/PS1ΔE9 transgenic Alzheimer's disease mice^[4].
Coptisine Sulfate attenuates obesity-related inflammation through LPS/TLR-4-mediated signaling pathway in Syrian golden hamsters^[5].

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

Animal Model:

Sprague-Dawley (male, 280±20 g, left anterior descending coronary artery occlusion for 30 min followed by reperfusion)^[2]
Dosage:

3 mg/kg; 10 mg/kg; 30 mg/kg
Administration:

p.o.; single dose 10 min before ischemia, plus an additional dose 4 h after reperfusion (24 h reperfusion studies); single dose 10 min before ischemia (3 h reperfusion studies)
Result:

Significantly decreased I/R-induced arrhythmia score and reduced incidence of premature ventricular complexes and ventricular tachycardia.
Significantly reduced infarct size compared with I/R controls.
Significantly reduced serum levels of aspartate transaminase, lactate dehydrogenase, and creatine kinase-MB compared with I/R controls.
Significantly attenuated I/R-induced reductions in left ventricular ejection fraction and fractional shortening at 24 h post-reperfusion.
Significantly reduced the percentage of TUNEL-positive apoptotic cardiomyocytes, dose-dependently decreased cleaved caspase-3 expression, and upregulated Bcl-2 protein expression compared with I/R controls.
Reduced DNA fragmentation indicative of apoptosis.
Significantly decreased heart tissue levels of proinflammatory cytokines IL-1β, IL-6, and TNF-α, inhibited NF-κB p65 translocation from cytoplasm to nucleus, reduced Rho, ROCK1, and ROCK2 protein expression, and attenuated phosphorylation of myosin phosphatase targeting subunit-1 compared with I/R controls.

Animal Model:

Syrian golden hamsters (male, 4-week-old, 100±5 g, HFHC diet-induced hypercholesterolemia)^[3]
Dosage:

23.35 mg/kg/day; 46.7 mg/kg/day; 70.05 mg/kg/day
Administration:

I.g.; daily; 4 weeks
Result:

Reduced serum total cholesterol (TC) by 10.9% and increased fecal cholesterol by 29% at 23.35 mg/kg.
Reduced serum TC by 24.3% and low-density lipoprotein cholesterol (LDL-c) by 20.0%, increased high-density lipoprotein cholesterol (HDL-c) by 24.8%, increased fecal cholesterol by 44% and fecal total bile acids (TBA) by 31.6% at 46.7 mg/kg.
Reduced serum TC by 26.7%, LDL-c by 22.2%, and triglycerides (TG) by 15.4%, increased HDL-c by 41.7%, increased fecal cholesterol by 51.5% and fecal TBA by 61.4% at 70.05 mg/kg.
Reduced body weight by 9.2% at 70.05 mg/kg/day after 33 days of treatment versus HFHC group.
Suppressed liver Hmgcr mRNA expression, increased liver Ldlr mRNA expression by 8.5-fold, 9.78-fold, and 11-fold, increased liver Cyp7a1 mRNA expression (21% increase at 70.05 mg/kg), and increased liver Srebp-2 mRNA expression across all doses versus HFHC group.
Reduced liver HMGCR protein expression by 16.4%, increased liver SREBP-2, LDLR, and CYP7A1 protein expression by 46.0%, 51.9%, and 107% at 70.05 mg/kg versus HFHC group.
Increased liver LDLR protein expression by 30.7% and CYP7A1 protein expression at 46.7 mg/kg versus HFHC group.

Animal Model:

B6C3-Tg (APPswe, PSEN1dE9)85Dbo/J (A-PPswe/PS1ΔE9) (8-month-old male)^[4]
Dosage:

50 mg/kg
Administration:

p.o.; once daily; 1 month
Result:

Reduced escape latency to levels indistinguishable from wild-type mice.
Showed significantly shorter latency to first target crossing, increased number of target platform crossings, and increased time spent in the target quadrant, with performance matching wild-type mice.
Normalized serum IDO activity (measured by kynurenine/tryptophan ratio) to wild-type levels, without altering IDO mRNA or protein expression in brain tissue.
Reduced brain expression of GFAP (astrocytic activation marker) and CD11b (microglial activation marker) to wild-type levels.
Restored hippocampal MAP2 (neuronal marker) immunoreactivity in the CA1 region, which was reduced in AD control mice.
Significantly reduced hippocampal Aβ_1-42 plaque burden to near wild-type levels.

Chemical Information

CAS. Nr. 1198398-71-8
Appearance Solid
Molecular Weight 417.39
Formel C₁₉H₁₅NO₈S
Color Yellow to orange
SMILES

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

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture and light

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

Publications (5)

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Journal Impact Factor

Mater Technol (N Y N Y)

2026 Jan 27;41.
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
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:

H₂O : 2 mg/mL (4.79 mM; ultrasonic and warming and heat to 60°C)

DMSO : 1 mg/mL (2.40 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)

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

2.3958 mL

11.9792 mL

23.9584 mL

5 mM

---

10 mM

---

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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (288 KB)
SDS (252 KB)
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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]. 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;39(3):1010428317694565. [Content Brief]

[2]. Guo J, et al. Coptisine protects rat heart against myocardial ischemia/reperfusion injury by suppressing myocardial apoptosis and inflammation. Atherosclerosis. 2013;231(2):384-391. [Content Brief]

[3]. He K, et al. The safety and anti-hypercholesterolemic effect of coptisine in Syrian golden hamsters. Lipids. 2015;50(2):185-194. [Content Brief]

[4]. 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]

[5]. Chen HB, et al. Anti-inflammatory activity of coptisine free base in mice through inhibition of NF-κB and MAPK signaling pathways. Eur J Pharmacol. 2017;811:222-231. [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 / H₂O	1 mM	2.3958 mL	11.9792 mL	23.9584 mL	59.8960 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

Coptisine Sulfate

5 Cited Publications

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Coptisine Sulfate

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