Darbufelone
Based on 1 Customer Validation
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.
- Purity : 98.0%
- CAS No.: 139226-28-1
- Formula: C18H24N2O2S
- Molecular Weight:332.46
-
Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
-
HY-112248A
HAMI 3379CysLT2 Receptor Antagonist -
HY-101438A
Darbufelone mesylatePGF2α/LTB5 Inhibitor -
HY-107607
FPL-55712 free baseleukotriene Receptor Antagonist -
HY-101438AR
Darbufelone mesylate (Standard)PGF2α/LTB5 Inhibitor -
HY-107608
Leukotriene B4PROTAC linker -
HY-17492
ZafirlukastLeukotriene Receptor Antagonist -
HY-19989
MK-571ABCC1/MRP4 Inhibitor -
HY-101813
LaflunimusImmunomodulator/DHODH Inhibitor -
HY-19193
CP-105696LTB4 Receptor Antagonist -
HY-13628
EtalocibLTB4 Receptor Antagonist -
HY-149589
11(Z),14(Z)-Eicosadienoic acidUnsaturated Fatty Acid -
HY-111212
TomelukastLeukotriene D4/E4 Antagonist
All Leukotriene Receptor Isoforms
More
Biological Activity
Description
IC50 & Target
IC50: 0.19 μM (PGHS-2), 20 μM (PGHS-1)[1]
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| RBL-1 | IC50 |
0.11 μM
Compound: 5d
|
Compound was tested for its inhibitory activity against PGF-2 alpha (CO) formation in RBL-1 cells stimulated with the calcium ionophore A-23187
Compound was tested for its inhibitory activity against PGF-2 alpha (CO) formation in RBL-1 cells stimulated with the calcium ionophore A-23187
|
10.1016/S0960-894X(00)80051-7 |
| RBL-1 | IC50 |
1.2 μM
Compound: 5d
|
Compound was tested for its inhibitory activity against LTB4 (5-LO) formation in RBL-1 cells stimulated with the calcium ionophore A-23187
Compound was tested for its inhibitory activity against LTB4 (5-LO) formation in RBL-1 cells stimulated with the calcium ionophore A-23187
|
10.1016/S0960-894X(00)80051-7 |
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. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 139226-28-1
-
Appearance Solid
-
Molecular Weight 332.46
-
Formula C18H24N2O2S
-
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
-
Synonyms
CI-1004
-
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocols
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
-
Data Sheet (280 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
References
[1]. Johnson AR, et al. Slow-binding inhibition of human prostaglandin endoperoxide synthase-2 with darbufelone, an isoform-selective antiinflammatory di-tert-butyl phenol. Biochemistry. 2001 Jun 26;40(25):7736-45. [Content Brief]
[2]. Ye X, et al. Darbufelone, a novel anti-inflammatory drug, induces growth inhibition of lung cancer cells both in vitro and in vivo. Cancer Chemother Pharmacol. 2010 Jul;66(2):277-85. [Content Brief]
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 |
Darbufelone Related Classifications
HY-101438 Related Classifications
Powered by Bioz