Size | Price | Stock | Qty |
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25mg |
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50mg |
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100mg |
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Other Sizes |
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ln Vitro |
Coptisine has an IC50 value of 6.3 μM and a Ki value of 5.8 μM, making it a highly effective non-competitive IDO inhibitor[1]. The growth of A549, H460, H2170, MDA-MB-231, and HT-29 cells is inhibited by copoxine (0.1-100 μM), with IC50 values of 18.09, 29.50, 21.60, 20.15, and 26.60 μM, in that order. In A549 cells, coptisine (12.5, 25, and 50 μM) concentration-dependently causes G2/M arrest and apoptosis, downregulates the expression of cyclin B1, cdc2, and cdc25C, and increases the expression of pH2AX and p21. In A549 cells, copoposite (12.5, 25, 50 μM) also causes mitochondrial dysfunction and triggers caspase activity. Additionally, ROS levels are raised by coptisine (50 μM) in a time-dependent manner (0.5, 1, 2, 4, 12, and 24 hours) [3].
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ln Vivo |
Mice's LD50 value for coptisine was 880.18 mg/kg, and its toxicity increased with concentration. The dosage of 154 mg/kg/day for 90 days did not cause toxicity in SD rats. In addition to increasing HDL-c content to varied degrees and slowing down the weight gain brought on by the HFHC diet, copoxine (23.35, 46.7, 70.05 mg/kg, po) increased fecal cholesterol and TBA levels in hamsters in a dose-dependent manner. It also reduced TC, TG, and LDL-c levels in the serum of the animals. Inducing the expression of SREBP-2, LDLR, and CYP7A1 proteins involved in cholesterol metabolism, coptisine (70.05 mg/kg, po) lowers the level of HMGCR protein expression [2].
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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 |
Molecular Formula |
C19H14NO4
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Molecular Weight |
320.3188
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CAS # |
3486-66-6
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Related CAS # |
Coptisine Sulfate;1198398-71-8;Coptisine chloride;6020-18-4
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SMILES |
O1C([H])([H])OC2=C1C([H])=C1C(=C2[H])C([H])([H])C([H])([H])[N+]2C([H])=C3C4=C(C([H])=C([H])C3=C([H])C=21)OC([H])([H])O4
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.1219 mL | 15.6094 mL | 31.2188 mL | |
5 mM | 0.6244 mL | 3.1219 mL | 6.2438 mL | |
10 mM | 0.3122 mL | 1.5609 mL | 3.1219 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.