2. Apoptosis PI3K/Akt/mTOR Metabolic Enzyme/Protease Immunology/Inflammation NF-κB Anti-infection
  3. Apoptosis Akt mTOR Reactive Oxygen Species (ROS) Caspase Bacterial Fungal
  4. Guaiazulene

Guaiazulene is a bicyclic sesquiterpene that can cross the blood-brain barrier. Guaiazulene exhibits various biological activities such as anti-inflammatory, antioxidant, hepatoprotective, antibacterial, and anti-tumor properties. Guaiazulene is also commonly used as a colorant in cosmetics. Guaiazulene shows in vitro cytotoxicity to rat neuronal cells and N2a neuroblastoma cells at high concentrations.

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Guaiazulene

Guaiazulene Chemical Structure

CAS No. : 489-84-9

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Based on 1 publication(s) in Google Scholar

Other Forms of Guaiazulene:

Guaiazulene Related Antibodies

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  • Biological Activity

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  • Customer Review

Description

Guaiazulene is a bicyclic sesquiterpene that can cross the blood-brain barrier. Guaiazulene exhibits various biological activities such as anti-inflammatory, antioxidant, hepatoprotective, antibacterial, and anti-tumor properties. Guaiazulene is also commonly used as a colorant in cosmetics. Guaiazulene shows in vitro cytotoxicity to rat neuronal cells and N2a neuroblastoma cells at high concentrations[1][2][3][4].

In Vitro

Guaiazulene (≥150 μg/mL; 24 h) can reduce the cell viability, inhibit the total antioxidant capacity, but has no obvious DNA damage in N2a and rat neurons[1].
Guaiazulene (5-20 μM; 0-45 min) significantly inhibits lipid peroxidation in rat liver microsomes with an IC50 of 9.8 μM[2].
Guaiazulene (0-250 μM; 48 h) can inhibit the proliferation, reduce clone formation, and induce ROS accumulation and cell apoptosis of non-small cell lung cancer cell lines[3].
Guaiazulene (0-150 μM; 24-48 h) triggers a complete autophagic flux in non-small cell lung cancer cell lines A549 and H1975 by inhibiting the Akt/mTOR signaling pathway[3].

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

Guaiazulene Related Antibodies

Cell Viability Assay[2]

Cell Line: Primary rat neurons and N2a NB cells
Concentration: 10, 25, 50, 75, 100, 150, 200, and 400 μg/mL
Incubation Time: 24 h
Result: Did not affect cell viability at 10, 25, 50, 75, and 100 μg/mL
Inhibited the cell viability at 150, 200, and 400 μg/mL.

Cell Viability Assay[3]

Cell Line: Non-small cell lung cancer cell lines
Concentration: 0, 50, 100, 150, 200, and 250 μM
Incubation Time: 48 h
Result: Inhibited the cell growth, with IC50 values of 135.0, 144.7, 148.9, 109.5, 152.8, and 207.0 μM for A549, PC9, HCC827, H1975, H1299 and 16HBE, respectively.
In Vivo

Guaiazulene (250 mg/kg; intraperitoneal injection; single dose) exerts a protective effect in a rat model of liver injury[2].
Guaiazulene (25 mg/kg; intraperitoneal injection; 3 weeks) exhibits anti-tumor activity in a nude mouse model of A549 xenograft[3].

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

Animal Model: Female Fischer-344 rats (180-200 g) treated Acetaminophen (Paracetamol; HY-66005) to induc liver injury[2]
Dosage: 250 mg/kg
Administration: Intraperitoneal injection; single dose
Result: Restored the paracetamol-decreased hepatic glutathione level, and normalized other parameters including hepatic weight, cytosolic protein content, glutathione transferase activity, and glutathione reductase activity, which were affected by paracetamol.
Did not cause any macroscopic toxic symptoms, and its administration alone has no effect on all tested indices.
Animal Model: Female nude mice (BALB/c, 17-19 g) aged 5 weeks old treated A549 cells[3]
Dosage: 25 mg/kg
Administration: Intraperitoneal injection; 3 weeks
Result: Caused smaller size and lighter weight of tumors.
Reduced Ki67 staining intensity, while cleaved-caspase 3 intensity was increased; LC3 staining was stronger and p-Akt levels were decreased in tumor tissues.
Caused no significant changes in mouse weight or pathologic features of major organs (heart, lung, liver, spleen, kidney)
Molecular Weight

198.30

Formula

C15H18
CAS No.
Appearance

Solid-Liquid Mixture

SMILES

CC(C1=CC2=C(C)C=CC2=C(C)C=C1)C
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (252.14 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 5.0429 mL 25.2143 mL 50.4286 mL
5 mM 1.0086 mL 5.0429 mL 10.0857 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)

Mass
=
Concentration
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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: ≥ 6.25 mg/mL (31.52 mM); Clear solution

    This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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: ≥ 6.25 mg/mL (31.52 mM); Clear solution

    This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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).
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: 99.26%

SDS (392 KB)

COA (257 KB) RP-HPLC (215 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. 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 5.0429 mL 25.2143 mL 50.4286 mL 126.0716 mL
5 mM 1.0086 mL 5.0429 mL 10.0857 mL 25.2143 mL
10 mM 0.5043 mL 2.5214 mL 5.0429 mL 12.6072 mL
15 mM 0.3362 mL 1.6810 mL 3.3619 mL 8.4048 mL
20 mM 0.2521 mL 1.2607 mL 2.5214 mL 6.3036 mL
25 mM 0.2017 mL 1.0086 mL 2.0171 mL 5.0429 mL
30 mM 0.1681 mL 0.8405 mL 1.6810 mL 4.2024 mL
40 mM 0.1261 mL 0.6304 mL 1.2607 mL 3.1518 mL
50 mM 0.1009 mL 0.5043 mL 1.0086 mL 2.5214 mL
60 mM 0.0840 mL 0.4202 mL 0.8405 mL 2.1012 mL
80 mM 0.0630 mL 0.3152 mL 0.6304 mL 1.5759 mL
100 mM 0.0504 mL 0.2521 mL 0.5043 mL 1.2607 mL
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Guaiazulene 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:

Guaiazulene489-84-9ApoptosisAktmTORReactive Oxygen Species (ROS)CaspaseBacterialFungalPKBProtein kinase BMammalian target of RapamycinA549liver injury modelN2aPC9HCC827H1975H129916HBEInhibitorinhibitorinhibit

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