2. GPCR/G Protein
  3. Prostaglandin Receptor Leukotriene Receptor
  4. Darbufelone

Darbufelone is a dual inhibitor of cellular PGF2α and LTB4 production. Darbufelone potently inhibits PGHS-2 (IC50= 0.19 μM) but is much less potent with PGHS-1 (IC50=20 μM).

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

Darbufelone Chemical Structure

Darbufelone Chemical Structure

CAS No. : 139226-28-1

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Based on 1 publication(s) in Google Scholar

Other Forms of Darbufelone:

Darbufelone Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Darbufelone is a dual inhibitor of cellular PGF2α and LTB4 production. Darbufelone potently inhibits PGHS-2 (IC50= 0.19 μM) but is much less potent with PGHS-1 (IC50=20 μM).

IC50 & Target

IC50: 0.19 μM (PGHS-2), 20 μM (PGHS-1)[1]
In Vitro

Darbufelone is a noncompetitive inhibitor of PGHS-2 (Ki=10±5 μM). Darbufelone quenches the fluorescence of PGHS-2 at 325 nm (lambda(ex)=280 nm) with Kd=0.98±0.03 μM[1].To test the putative anti-proliferative effect of Darbufelone, A549, H520 and H460 cell lines are used, which are established from three distinct pathological subtypes of NSCLC (adenocarcinoma, squamous and large cell lung cancer respectively). Increasing concentrations of Darbufelone, ranging from 5 to 60 μM, are tested for 72 h. The cell growth inhibition of these three cell lines gradually increases with higher drug concentration. The IC50 of A549 and H520 are 20±3.6 and 21±1.8 μM, respectively, while the H460 has much lower IC50 (15±2.7 μM)[2].

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

Darbufelone Related Antibodies
In Vivo

Darbufelone is a dual inhibitor of cellular PGF2R and LTB4 production. Darbufelone is orally active and nonulcerogenic in animal models of inflammation and arthritis[1]. When mice are treated with Darbufelone at dosage of 80 mg/kg/day, the tumor volumes decrease in a time-dependent manner. In contrast, lower dose of Darbufelone (20 or 40 mg/kg/day) dos not show any significant inhibition of tumor weight. At necropsy, the tumor weight in mice treated with Darbufelone (80 mg/kg/day) is reduced by 30.2% in comparison with control group[2].

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

332.46

Formula

C18H24N2O2S
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C1N=C(N)S/C1=C\C2=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (300.79 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 3.0079 mL 15.0394 mL 30.0788 mL
5 mM 0.6016 mL 3.0079 mL 6.0158 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 (sealed storage, away from moisture). 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
×
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 (7.52 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.
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 (sealed storage, away from moisture)

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: 99.49%

SDS (252 KB)

COA (252 KB) HNMR (384 KB) LCMS (96 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[1]

The effect of Darbufelone on the cyclooxygenase activity of PGHS-2 is determined in assays with no enzyme-inhibitor preincubation. HoloPGHS-2 (30 nM final concentration) is added to reaction mixtures that contain 20 mM Tris-HCl buffer (pH 7.4), 100 μM TMPD, and varying levels of Arachidonic acid (0-60 μM) and Darbufelone (0-30 μM). The cyclooxygenase activity is measured by monitoring the oxidation of TMPD at 610 nm using a microplate reader[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[2]

A549 (CCL-185, lung adenocarcinoma cancer cell line), NCI-H520 (HTB-182, lung squamous cancer cell line) and NCI-H460 (HTB-177, lung large cell cancer cell line) cells are cultured in RPMI-1640, supplemented with 10% (v/v) heat-inactivated fetal bovine serum, 2 mM L-glutamine, 100 U/mL Penicillin G, and 100μg/mL Streptomycin. Cells are grown at 37°C in a humidified atmosphere of 95% air and 5% CO2 and routinely passaged using 0.25% trypsin–EDTA. The effect of Darbufelone on human lung carcinoma cell viability is determined by MTT reduction assay. In brief, tumor cells growing in log-phase are trypsinized and seeded at 5×103 cells per well into 96-well plates and allowed to attach overnight. Medium in each well is replaced with fresh medium or medium containing various concentrations of Darbufelone (5-60 μM) in at least triplicate wells. Cells are cultured to another 72 h. After treatment, 1/10 volume of MTT solution (5 mg/mL) is added to each well, and the plate is incubated at 37°C for another 4 h. Two hundred microliters of DMSO is added to each well to solubilize the MTT-formazan product after removal of the medium. Absorbance at 595 nm is measured with a multi-well spectrophotometer. Growth inhibition is calculated as a percentage of the untreated controls[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Mice[2]
C57Bl/6 male mice at 4-5 weeks are used. These mice are housed in air-conditioned quarters and are provided food and water ad libitum. On the day 0, Lewis Lung Carcinoma cells (1×106) are implanted into the left armpit of C57Bl/6 mice. The mice are randomly divided into four treatment groups of ten animals each. The day after inoculation (day 1), control group is treated with CMC-Na, and other groups are administered Darbufelone by gavage at doses of 20, 40, and 80 mg/kg/day. The treatment is continued till the end of the study. On day 14, animals are killed, and tumors are excised, weighed, and fixed in formalin for the further histochemical analysis.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 (sealed storage, away from moisture). 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 3.0079 mL 15.0394 mL 30.0788 mL 75.1970 mL
5 mM 0.6016 mL 3.0079 mL 6.0158 mL 15.0394 mL
10 mM 0.3008 mL 1.5039 mL 3.0079 mL 7.5197 mL
15 mM 0.2005 mL 1.0026 mL 2.0053 mL 5.0131 mL
20 mM 0.1504 mL 0.7520 mL 1.5039 mL 3.7599 mL
25 mM 0.1203 mL 0.6016 mL 1.2032 mL 3.0079 mL
30 mM 0.1003 mL 0.5013 mL 1.0026 mL 2.5066 mL
40 mM 0.0752 mL 0.3760 mL 0.7520 mL 1.8799 mL
50 mM 0.0602 mL 0.3008 mL 0.6016 mL 1.5039 mL
60 mM 0.0501 mL 0.2507 mL 0.5013 mL 1.2533 mL
80 mM 0.0376 mL 0.1880 mL 0.3760 mL 0.9400 mL
100 mM 0.0301 mL 0.1504 mL 0.3008 mL 0.7520 mL
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Darbufelone 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:

Darbufelone139226-28-1CI-1004CI1004CI 1004Prostaglandin ReceptorLeukotriene ReceptorInhibitorinhibitorinhibit

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