| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 100mg | |||
| Other Sizes |
| Targets |
The target of (-)-Corynoxidine is acetylcholinesterase (AChE), with an IC50 value of 4.2 μM [1]
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|---|---|
| ln Vitro |
1. Inhibition of acetylcholinesterase (AChE) activity (Reference [1]): (-)-Corynoxidine (0.1-100 μM) was tested for AChE inhibitory activity using a colorimetric assay. It showed concentration-dependent inhibition of AChE: at 1 μM, the inhibition rate was 28%; at 4.2 μM (IC50), the inhibition rate reached 50%; at 10 μM, the inhibition rate was 72%; at 100 μM, the maximum inhibition rate (85%) was achieved. This activity was lower than the positive control tacrine (IC50 = 0.12 μM) but confirmed its AChE inhibitory potential [1]
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| Enzyme Assay |
1. Reaction system preparation (Reference [1]): Prepare a reaction mixture containing 50 mM Tris-HCl buffer (pH 8.0), 0.1 mM 5,5'-dithiobis(2-nitrobenzoic acid) (DTNB), 0.5 mM acetylthiocholine iodide (ATCI, AChE substrate), and (-)-Corynoxidine (0.1-100 μM). The final volume of the mixture is 200 μL [1]
2. Incubation and detection (Reference [1]): Add 10 μL of electric eel AChE solution (0.05 U/mL) to the reaction mixture to initiate the reaction. Incubate the mixture at 37°C for 30 minutes. Measure the absorbance at 412 nm using a microplate reader—DTNB reacts with thiocholine (hydrolyzed product of ATCI by AChE) to form a yellow product, and the absorbance value reflects AChE activity [1] 3. Inhibition rate calculation (Reference [1]): Calculate the AChE inhibition rate using the formula: Inhibition rate (%) = [(Acontrol - Asample)/Acontrol] × 100. Acontrol is the absorbance of the mixture without (-)-Corynoxidine, and Asample is the absorbance of the mixture with (-)-Corynoxidine. The IC50 value is calculated by plotting the inhibition rate against the logarithm of (-)-Corynoxidine concentration and using linear regression [1] |
| References | |
| Additional Infomation |
Colinoxine has reportedly been found in Corydalis balansae, Corydalis speciosa, and Stephania rotunda, and there is relevant data available.
1. Source and structural class: (-)-colinoxine is an isoquinoline alkaloid isolated from the aerial parts of Corydalis speciosa (a traditional Chinese medicine of the Papaveraceae family)[1] 2. Mechanistic significance: (-)-colinoxine's acetylcholinesterase (AChE) inhibitory activity suggests its potential for treating neurodegenerative diseases such as Alzheimer's disease, as excessive AChE activity leads to decreased acetylcholine levels in the brain, which is a key factor in cognitive impairment[1] 3. Structural features: (-)-colinoxine has a tetrahydroisoquinoline core structure, which is a common pharmacophore of AChE. Inhibitor[1] |
| Molecular Formula |
C21H25NO5
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|---|---|
| Molecular Weight |
371.4269
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| Exact Mass |
371.173
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| CAS # |
57906-85-1
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| PubChem CID |
21589010
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
3.347
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
27
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| Complexity |
519
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| Defined Atom Stereocenter Count |
2
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| SMILES |
COC1=C(C2=C(C[C@H]3C4=CC(=C(C=C4CC[N@@+]3(C2)[O-])OC)OC)C=C1)OC
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| InChi Key |
QYEMUDHNCZHUKC-JTSKRJEESA-N
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| InChi Code |
InChI=1S/C21H25NO5/c1-24-18-6-5-13-9-17-15-11-20(26-3)19(25-2)10-14(15)7-8-22(17,23)12-16(13)21(18)27-4/h5-6,10-11,17H,7-9,12H2,1-4H3/t17-,22-/m0/s1
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| Chemical Name |
(7S,13aS)-2,3,9,10-tetramethoxy-7-oxido-6,8,13,13a-tetrahydro-5H-isoquinolino[2,1-b]isoquinolin-7-ium
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 Vitro) |
DMSO : ~25 mg/mL (~67.31 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (3.37 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (3.37 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6923 mL | 13.4615 mL | 26.9230 mL | |
| 5 mM | 0.5385 mL | 2.6923 mL | 5.3846 mL | |
| 10 mM | 0.2692 mL | 1.3461 mL | 2.6923 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.
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