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

Darbufelone mesylate  (Synonyms: CI-1004 mesylate)

Cat. No.: HY-101438A Purity: 99.65%
SDS COA Handling Instructions

Molarity Calculator

Darbufelone mesylate (CI-1004 mesylate) 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 mesylate Chemical Structure

Darbufelone mesylate Chemical Structure

CAS No. : 139340-56-0

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
5 mg USD 130 In-stock
10 mg USD 220 In-stock
25 mg USD 460 In-stock
50 mg USD 790 In-stock
100 mg USD 1260 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Darbufelone mesylate:

Darbufelone mesylate Related Antibodies

Top Publications Citing Use of Products

View All Prostaglandin Receptor Isoform Specific Products:

View All Isoforms
DP EP FP IP TXA2/TP TXB2

View All Leukotriene Receptor Isoform Specific Products:

View All Isoforms
LTB4 LTC4/CysLT2 LTD4/CysLT1 LTE4

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Darbufelone mesylate (CI-1004 mesylate) 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[1]

PGF2α

 

LTB4

 

PGHS-2

0.19 μM (IC50)

PGHS-1

20 μM (IC50)

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 mesylate 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

428.57

Formula

C19H28N2O5S2
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.CS(=O)(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

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

Solvent & Solubility
In Vitro: 

DMSO : 110 mg/mL (256.67 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3333 mL 11.6667 mL 23.3334 mL
5 mM 0.4667 mL 2.3333 mL 4.6667 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 and light). 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: 5.5 mg/mL (12.83 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 5.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (55.0 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 and 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: 99.65%

SDS (252 KB)

COA (258 KB) LCMS (104 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 and 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 2.3333 mL 11.6667 mL 23.3334 mL 58.3335 mL
5 mM 0.4667 mL 2.3333 mL 4.6667 mL 11.6667 mL
10 mM 0.2333 mL 1.1667 mL 2.3333 mL 5.8334 mL
15 mM 0.1556 mL 0.7778 mL 1.5556 mL 3.8889 mL
20 mM 0.1167 mL 0.5833 mL 1.1667 mL 2.9167 mL
25 mM 0.0933 mL 0.4667 mL 0.9333 mL 2.3333 mL
30 mM 0.0778 mL 0.3889 mL 0.7778 mL 1.9445 mL
40 mM 0.0583 mL 0.2917 mL 0.5833 mL 1.4583 mL
50 mM 0.0467 mL 0.2333 mL 0.4667 mL 1.1667 mL
60 mM 0.0389 mL 0.1944 mL 0.3889 mL 0.9722 mL
80 mM 0.0292 mL 0.1458 mL 0.2917 mL 0.7292 mL
100 mM 0.0233 mL 0.1167 mL 0.2333 mL 0.5833 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Darbufelone mesylate 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:

Darbufelone139340-56-0CI-1004CI1004CI 1004Prostaglandin ReceptorLeukotriene ReceptorInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Darbufelone mesylate
Cat. No.:
HY-101438A
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (252 KB) Français - FR (252 KB) Deutsch - DE (252 KB) Norwegian - NO (252 KB) Español - ES (252 KB) Swedish - SV (252 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.