| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
| Targets |
Multiple targets have been identified for corynoline. It acts as an acetylcholinesterase inhibitor (EC 3.1.1.7). Corynoline promotes apoptosis and inhibits proliferation via regulating the STAT3/Bcl-2 signaling pathway. It suppresses osteoclastogenesis and attenuates ROS activities by regulating NF-κB/MAPKs and Nrf2 signaling pathways. Corynoline protects chronic pancreatitis via binding to PSMA2 and alleviating pancreatic fibrosis. It alleviates hepatic ischemia-reperfusion injury by inhibiting NLRP3 inflammasome activation through enhancing Nrf2/HO-1 signaling.
|
|---|---|
| ln Vitro |
Corynoline demonstrates diverse biological activities. It acts as an acetylcholinesterase inhibitor. The compound promotes apoptosis and inhibits proliferation of glioblastoma via regulating the STAT3/Bcl-2 signaling pathway. It suppresses osteoclastogenesis and attenuates ROS activities by regulating NF-κB/MAPKs and Nrf2 signaling pathways. Corynoline protects chronic pancreatitis via binding to PSMA2 and alleviating pancreatic fibrosis, dose-dependently reducing collagen I synthesis in pancreatic stellate cells induced by TGF-β1. It inhibits proliferation of acute myeloid leukemia cells, induces apoptosis, and causes G2/M cell cycle arrest.
|
| ln Vivo |
In vivo, corynoline has demonstrated protective effects against hepatic ischemia-reperfusion injury by inhibiting oxidative stress, inflammatory responses, and apoptosis. These effects are associated with inhibiting ROS-induced NLRP3 inflammasome activation by enhancing Nrf2/HO-1 signaling. Corynoline has also shown protective effects in models of chronic pancreatitis by alleviating pancreatic fibrosis. Further in vivo studies are needed to fully characterize its therapeutic potential.
|
| Enzyme Assay |
In vitro enzyme assays for corynoline involve measuring acetylcholinesterase inhibition using Ellman's method or other colorimetric assays. The enzyme is incubated with acetylthiocholine substrate and various concentrations of corynoline, and the production of thiocholine is measured spectrophotometrically. IC50 values are determined from concentration-response curves. These assays confirm the acetylcholinesterase inhibitory activity of corynoline.
|
| Cell Assay |
Cellular assays for corynoline involve treating cancer cell lines (such as glioblastoma, acute myeloid leukemia, or breast cancer cells) with the compound and measuring cell proliferation, apoptosis, and cell cycle distribution. Cell viability is assessed by MTT or other metabolic assays. Apoptosis is measured by flow cytometry using Annexin V staining or caspase activity assays. These assays demonstrate the antiproliferative and pro-apoptotic effects of corynoline on various cancer cell lines.
|
| Animal Protocol |
In vivo animal studies for corynoline typically involve administration to rodent models of disease. In models of hepatic ischemia-reperfusion injury, mice are subjected to hepatic ischemia followed by reperfusion, and corynoline is administered before or after the ischemic event. Liver injury is assessed by measuring serum transaminases (ALT, AST), histopathological examination, and measurement of oxidative stress and inflammatory markers. In models of chronic pancreatitis, corynoline's anti-fibrotic effects are assessed.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for corynoline is limited and primarily derived from preclinical studies. The compound is absorbed following oral or intraperitoneal administration and distributes to various tissues. Metabolism and elimination pathways have not been fully characterized. Further pharmacokinetic studies are needed to support clinical development.
|
| Toxicity/Toxicokinetics |
Preclinical toxicity studies of corynoline are limited. As a natural alkaloid, the compound's safety profile has not been extensively characterized. The compound has demonstrated protective effects against various forms of tissue injury, suggesting a favorable safety profile at therapeutic doses. However, comprehensive toxicological evaluation is needed before clinical development.
|
| References |
|
| Additional Infomation |
Corynoline is a benzophenanthrene alkaloid, a compound in which celandine is substituted with a methyl group at the 13-position. It was isolated from the aerial parts of Corydalis incisa and possesses acetylcholinesterase inhibitory activity, along with antitumor and hepatoprotective effects. It is a metabolite and also an EC 3.1.1.7 (acetylcholinesterase) inhibitor, antitumor drug, and hepatoprotective agent. Corynoline belongs to the isoquinoline class of compounds, and is an organic heterohexacyclic compound, a secondary alcohol, a cyclic acetal, and a benzophenanthrene alkaloid. It is functionally related to celandine. Corynoline has been reported to exist in Corydalis conspersa, Corydalis bungeana, and other organisms with relevant data.
Corynoline is a benzophenanthridine alkaloid with diverse pharmacological activities, including acetylcholinesterase inhibition, anticancer, hepatoprotective, and anti-inflammatory effects. The compound has shown promising activity against various cancers including glioblastoma, acute myeloid leukemia, and breast cancer. It is isolated from Corydalis incisa and has been the subject of increasing research interest. Further preclinical and clinical studies are needed to evaluate its therapeutic potential. |
| Molecular Formula |
C21H21NO5
|
|---|---|
| Molecular Weight |
367.4
|
| Exact Mass |
367.141
|
| CAS # |
18797-79-0
|
| PubChem CID |
177014
|
| Appearance |
White to light yellow solid powder
|
| Density |
1.4±0.1 g/cm3
|
| Boiling Point |
504.2±50.0 °C at 760 mmHg
|
| Melting Point |
217-218ºC
|
| Flash Point |
258.7±30.1 °C
|
| Vapour Pressure |
0.0±1.4 mmHg at 25°C
|
| Index of Refraction |
1.659
|
| LogP |
3.23
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
0
|
| Heavy Atom Count |
27
|
| Complexity |
603
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
C[C@]12[C@H](CC3=CC4=C(C=C3[C@H]1N(CC5=C2C=CC6=C5OCO6)C)OCO4)O
|
| InChi Key |
IQUGPRHKZNCHGC-TYPHKJRUSA-N
|
| InChi Code |
InChI=1S/C21H21NO5/c1-21-14-3-4-15-19(27-10-24-15)13(14)8-22(2)20(21)12-7-17-16(25-9-26-17)5-11(12)6-18(21)23/h3-5,7,18,20,23H,6,8-10H2,1-2H3/t18-,20+,21-/m0/s1
|
| Chemical Name |
(1R,12S,13R)-13,24-dimethyl-5,7,18,20-tetraoxa-24-azahexacyclo[11.11.0.02,10.04,8.014,22.017,21]tetracosa-2,4(8),9,14(22),15,17(21)-hexaen-12-ol
|
| Synonyms |
BT 000613 BT000613 Corynoline
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~41.67 mg/mL (~113.42 mM)
|
|---|---|
| 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7218 mL | 13.6091 mL | 27.2183 mL | |
| 5 mM | 0.5444 mL | 2.7218 mL | 5.4437 mL | |
| 10 mM | 0.2722 mL | 1.3609 mL | 2.7218 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
