1. Neuronal Signaling NF-κB Metabolic Enzyme/Protease Immunology/Inflammation MAPK/ERK Pathway Apoptosis JAK/STAT Signaling Stem Cell/Wnt
  2. Cholinesterase (ChE) Keap1-Nrf2 Heme Oxygenase (HO) COX NO Synthase p38 MAPK JNK Apoptosis Bcl-2 Family Caspase STAT Interleukin Related
  3. Corynoline

Corynoline is an orally active acetylcholinesterase (AChE) inhibitor with an IC50 of 30.6 μM. Corynoline exhibits multiple activities including anti-inflammatory, antinociceptive, antitumor and analgesic effects. Corynoline can be used in the research of diseases such as tumors and inflammatory pain.

For research use only. We do not sell to patients.

Corynoline

Corynoline Chemical Structure

CAS No. : 18797-79-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Corynoline:

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Corynoline is an orally active acetylcholinesterase (AChE) inhibitor with an IC50 of 30.6 μM. Corynoline exhibits multiple activities including anti-inflammatory, antinociceptive, antitumor and analgesic effects. Corynoline can be used in the research of diseases such as tumors and inflammatory pain[1][2][3][4].

IC50 & Target[1][2][3]

AChE

 

HO-1

 

IL-1β

 

Caspase 3

 

Caspase 9

 

p-STAT3

 

Bcl-2

 

COX-2

 

Cellular Effect
Cell Line Type Value Description References
RAW264.7 IC50
2.51 μM
Compound: 6
Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS induced nitric oxide production preincubated for 2 hrs followed by LPS challenge measured after 24 hrs by Griess reagent based assay
Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS induced nitric oxide production preincubated for 2 hrs followed by LPS challenge measured after 24 hrs by Griess reagent based assay
[PMID: 29853329]
In Vitro

Corynoline (1-4 μM; 24 h) inhibits LPS (HY-D1056)-induced NO production in RAW264.7 cells, upregulates the levels of Nrf2, HO-1 and NQO1, and downregulates the expression of iNOS and COX-2[1].
Corynoline (1-4 μM; 24 h) downregulates LPS-induced IL-1β and TNF-α expression at both mRNA and protein levels in RAW264.7 cells in a dose-dependent manner[1].
Corynoline (1 μM; 24 h) inhibits LPS-induced phosphorylation of p38 and JNK in RAW264.7 cells[1].
Corynoline (5-40 μM; 24-48 h) inhibits the proliferation and induces apoptosis of U87 and LN229 glioblastoma cells[2].
Corynoline (10-20 μM; 10-14 days) inhibits the colony-forming ability of U87 glioblastoma cells[2].

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

Western Blot Analysis[1]

Cell Line: RAW264.7 treated LPS (HY-D1056)
Concentration: 1, 2, 4 μM
Incubation Time: 24 h
Result: Upregulated the levels of Nrf2, HO-1 and NQO1, and downregulated the levels of iNOS and COX-2.

Cell Proliferation Assay[2]

Cell Line: U87 glioblastoma cell line, LN229 glioblastoma cell line, human astrocyte (HA) cell line
Concentration: 5, 10, 20, 40 μM
Incubation Time: 24 h, 48 h
Result: Inhibited the viability of U87 and LN229 cells in a dose-dependent manner. Exhibited no significant toxicity towards HA cells.

Immunofluorescence[2]

Cell Line: U87 glioblastoma cell line, LN229 glioblastoma cell line
Concentration: 10, 20 μM
Incubation Time: 48 h
Result: Significantly reduced the percentage of Ki-67-positive cells in both U87 and LN229 cells. Reduced the proportion of Ki-67-positive cells to less than 50% at 20 μM.

Western Blot Analysis[2]

Cell Line: U87 glioblastoma cell line, LN229 glioblastoma cell line
Concentration: 10, 20 μM
Incubation Time: 48 h
Result: Significantly increased the protein levels of cleaved caspase-9 and cleaved caspase-3 in both U87 and LN229 cells.
Inhibited STAT3 phosphorylation and Bcl-2 expression in a concentration-dependent manner in both U87 and LN229 cells. Upregulated the pro-apoptotic proteins Bak and Bax.
In Vivo

Corynoline (50 mg/kg; i.p.; 21 days) exerts antitumor activity in mouse models of glioblastoma[2].
Corynoline (5-20 mg/kg; oral administration; single dose) exerts a significant dose-dependent antinociceptive and anti-inflammatory effect in various nociceptive and inflammatory models of male mice[3].

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

Animal Model: BALB/c nude (6 weeks old, 20-22 g, subcutaneously injected with GBM cells)[2]
Dosage: 50 mg/kg
Administration: i.p.; daily; 21 days
Result: Significantly reduced tumor volume.
Decreased the percentage of Ki-67-positive cells; downregulated phosphorylated STAT3 and Bcl-2 protein levels.
Upregulated Bak, Bax, cleaved caspase-9, and cleaved caspase-3 protein levels in tumor tissues.
Animal Model: Swiss mice (male, 20-30 g)[3]
Dosage: 5, 10, 20 mg/kg
Administration: p.o.; single dose
Result: Significantly increased the latency time of pain response in hot plate and tail immersion tests in a dose-dependent manner.
Reduced the number of abdominal writhing in acetic acid-induced model, the paw licking count in glutamate, capsaicin and formalin-induced models, and inhibited both the neurogenic phase and inflammatory phase of formalin-induced nociception.
Significantly suppressed carrageenan-induced paw edema, reduced the infiltration of leukocytes, mononuclear cells and polymorphonuclear cells in the peritoneal cavity induced by carrageenan, and down-regulated the levels of pro-inflammatory cytokines TNF-α, IL-1β and IL-6 in the air pouch model.
Molecular Weight

367.40

Formula

C21H21NO5

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

C[C@@]1(C(C=CC2=C3OCO2)=C3CN4C)[C@@]4([H])C(C=C(OCO5)C5=C6)=C6C[C@@H]1O

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 40 mg/mL (108.87 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

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

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

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

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: ≥ 4 mg/mL (10.89 mM); Clear solution

    This protocol yields a clear solution of ≥ 4 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (40.0 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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+
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.84%

References

Complete Stock Solution Preparation Table

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

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7218 mL 13.6091 mL 27.2183 mL 68.0457 mL
5 mM 0.5444 mL 2.7218 mL 5.4437 mL 13.6091 mL
10 mM 0.2722 mL 1.3609 mL 2.7218 mL 6.8046 mL
15 mM 0.1815 mL 0.9073 mL 1.8146 mL 4.5364 mL
20 mM 0.1361 mL 0.6805 mL 1.3609 mL 3.4023 mL
25 mM 0.1089 mL 0.5444 mL 1.0887 mL 2.7218 mL
30 mM 0.0907 mL 0.4536 mL 0.9073 mL 2.2682 mL
40 mM 0.0680 mL 0.3402 mL 0.6805 mL 1.7011 mL
50 mM 0.0544 mL 0.2722 mL 0.5444 mL 1.3609 mL
60 mM 0.0454 mL 0.2268 mL 0.4536 mL 1.1341 mL
80 mM 0.0340 mL 0.1701 mL 0.3402 mL 0.8506 mL
100 mM 0.0272 mL 0.1361 mL 0.2722 mL 0.6805 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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