2. Metabolic Enzyme/Protease Neuronal Signaling Membrane Transporter/Ion Channel NF-κB
  3. Phosphodiesterase (PDE) Calcium Channel MMP NF-κB
  4. Glaucine

Glaucine  (Synonyms: O,O-Dimethylisoboldine; S-(+)-Glaucine; NSC 34396)

Cat. No.: HY-N3945 Purity: 99.57%
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Glaucine (O,O-Dimethylisoboldine) is an alkaloid extracted from Glaucium flavum that possesses various activities, including cough relief, bronchodilation, anti-inflammatory effects, analgesia, antipyretic properties, and anticancer effects. Glaucine acts as a selective and orally active inhibitor of phosphodiesterase 4 (PDE4), with a Ki of 3.4 µM in human bronchial tissues and polymorphonuclear leukocytes. Glaucine induces relaxation of human isolated bronchi by antagonizing calcium channels. Additionally, Glaucine inhibits the activation of NF-κB, leading to a reduction in the expression of the MMP-9 gene, thereby suppressing the migration and invasion of breast cancer cells. Therefore, Glaucine holds potential for research in asthma and breast cancer.

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

Glaucine Chemical Structure

Glaucine Chemical Structure

CAS No. : 475-81-0

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5 mg USD 115 In-stock
10 mg USD 180 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Glaucine:

Glaucine Related Antibodies

Top Publications Citing Use of Products

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PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

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MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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Description

Glaucine (O,O-Dimethylisoboldine) is an alkaloid extracted from Glaucium flavum that possesses various activities, including cough relief, bronchodilation, anti-inflammatory effects, analgesia, antipyretic properties, and anticancer effects. Glaucine acts as a selective and orally active inhibitor of phosphodiesterase 4 (PDE4), with a Ki of 3.4 µM in human bronchial tissues and polymorphonuclear leukocytes. Glaucine induces relaxation of human isolated bronchi by antagonizing calcium channels. Additionally, Glaucine inhibits the activation of NF-κB, leading to a reduction in the expression of the MMP-9 gene, thereby suppressing the migration and invasion of breast cancer cells. Therefore, Glaucine holds potential for research in asthma and breast cancer[1][2][3][4][5][6].

IC50 & Target

PDE4

 

In Vitro

Glaucine (0.1 μM-1 mM; 30 min) produces a concentration-dependent inhibition of both spontaneous tension and histamine (HY-B1204)-induced tension in isolated human bronchial tissues[1].
Glaucine (10 μM-1 mM; 30 min) concentration-dependently inhibits the concentration of calcium ions in isolated human bronchial tissues induced by potassium depolarization[1].
Glaucine (0.1-3 mM; 120 min) concentration-dependently inhibits the release of peroxidase from human eosinophils[1].
Glaucine (0-50 μM; 24 and 48 h) inhibits the proliferation of MCF-7 cells induced by Phorbol 12-myristate 13-acetate (HY-18739) in a concentration-dependent manner[4].
Glaucine (0-30 μM; 36 h) significantly blocks the expression and activity of MMP-9 in MCF-7 cells induced by Phorbol 12-myristate 13-acetate (HY-18739) in a dose-dependent manner[4].
Glaucine (0-30 μM; 24 h) significantly inhibits the invasion of MDA-MB-231 cells in a dose-dependent manner[4].

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

Glaucine Related Antibodies

Cell Proliferation Assay[4]

Cell Line: PMA-induced MCF-7 cells
Concentration: 0, 1, 3, 15, 30 and 50 µM
Incubation Time: 24 and 48 h
Result: Inhibited PMA-induced colony formation by 48 and 63 % at a dose of 15 and 30 µM.

Western Blot Analysis[4]

Cell Line: PMA-induced MCF-7 cells
Concentration: 0, 15 and 30 µM
Incubation Time: 36 h
Result: Inhibited PMA-induced phosphorylation of IκBα in a dose-dependent manner and decreased nuclear NF-κB p65 subunit levels.
In Vivo

Glaucine (5-10 mg/mL; inhale; 3 min) inhibits acute bronchoconstriction and microvascular leakage at all airway levels induced by inhalation of aerosol antigens in guinea pigs sensitized with ovalbumins (HY-W250978)[5].
Glaucine (10-100 mg/kg; p.o.; 60 min) can effectively inhibit carrageenan (HY-125474)-induced paw edema and LPS (HY-D1056)-induced fever in rats, as well as acetic acid (HY-Y0319)-induced abdominal contraction in mice[6].

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

Animal Model: Ovalbumins (HY-W250978) sensitized guinea pigs to inhaled aerosol antigens[5]
Dosage: 10 mg/mL
Administration: inhale; 10 min
Result: Reduced airway hyperresponsiveness to histamine and lung eosinophil accumulation 30 minutes and 3 hours after inhalation of the antigen.
Increased eosinophil peroxidase activity in bronchoalveolar lavage fluid 24 hours after inhalation of aerosol antigen.
Molecular Weight

355.43

Formula

C21H25NO4
CAS No.
Appearance

Solid

Color

White to light brown

SMILES

CN1CCC2=CC(OC)=C(OC)C3=C2[C@]1([H])CC4=CC(OC)=C(OC)C=C34
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (281.35 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 2.8135 mL 14.0675 mL 28.1349 mL
5 mM 0.5627 mL 2.8135 mL 5.6270 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 2.5 mg/mL (7.03 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.03 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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: 99.57%

SDS (393 KB)

COA (255 KB) HNMR (256 KB) LCMS (256 KB)

Handling Instructions (2659 KB)
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 (protect from light). 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 2.8135 mL 14.0675 mL 28.1349 mL 70.3373 mL
5 mM 0.5627 mL 2.8135 mL 5.6270 mL 14.0675 mL
10 mM 0.2813 mL 1.4067 mL 2.8135 mL 7.0337 mL
15 mM 0.1876 mL 0.9378 mL 1.8757 mL 4.6892 mL
20 mM 0.1407 mL 0.7034 mL 1.4067 mL 3.5169 mL
25 mM 0.1125 mL 0.5627 mL 1.1254 mL 2.8135 mL
30 mM 0.0938 mL 0.4689 mL 0.9378 mL 2.3446 mL
40 mM 0.0703 mL 0.3517 mL 0.7034 mL 1.7584 mL
50 mM 0.0563 mL 0.2813 mL 0.5627 mL 1.4067 mL
60 mM 0.0469 mL 0.2345 mL 0.4689 mL 1.1723 mL
80 mM 0.0352 mL 0.1758 mL 0.3517 mL 0.8792 mL
100 mM 0.0281 mL 0.1407 mL 0.2813 mL 0.7034 mL
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Glaucine Related Classifications

Help & FAQs
  • 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.

Keywords:

Glaucine475-81-0O,O-Dimethylisoboldine S-(+)-Glaucine NSC 34396NSC34396NSC 34396NSC-34396Phosphodiesterase (PDE)Calcium ChannelMMPNF-κBCa2+ channelsCa channelsMatrix metalloproteinasesNuclear factor-κBNuclear factor-kappaBPDE4Ca2+α-adrenoceptoralkaloidanti-arthriticantitussivebronchodilationcAMPanti-inflammatoryantioxidativeantiviralInhibitorinhibitorinhibit

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